Medicinal Chemistry articles list

Pyrazole carbaldehyes as antiinflammatory agents-synthesis and in vitro membrane stabilization method

Pyrazole is a nitrogen containing 5-membered heterocyclic compound containing 3 carbons& 2 nitrogen atoms in the adjacent position of ring structure and is chemically known as 1, 2- diazole. Pyrazole nucleus is present in many pharmaceutically important compounds and intermediates . Majority of anti-inflammatory agents currently employed have GI irritation and enhanced acidity as side effects. As part of our efforts to develop newer and effective anti-inflammatory agents , ten newer pyrazole carbaldehydes were synthesized and evaluated for their anti-inflammatory activity using Diclofenac was the standard. Out of ten compounds synthesized, all compounds exhibited comparable activity with that of the standard.Highest percentage of haemolysis was observed for Pyrazole carbaldehydes with methoxy phenyl groups as substituents. These compounds should be considered for developing as leads for newer & safer anti-inflammatory agents.

Vinod B

Synthesis and broad spectrum antibacterial activities of 2-pyrazolines synthesized from chalcones

2-Pyrazolines are well known, and important nitrogen-containing five-membered heterocyclic compounds which belong to the family of azoles and have been found to possess considerable activities, like anticancer, antibacterial, antifungal, immunosuppressant and antiamoebic activity. In the present work, ten novel pyrazolines were prepared from chalcones, characterized and evaluated for their antibacterial activity against Staphylococcus aureus and Escherichia coli using Ciprofloxacin as standard and using DMSO as a solvent. Their activity was evaluated by measuring the zone of inhibition in mm. All the compounds exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli. Among ten derivatives of compounds synthesized, the derivative with 2-chloro and 4-chloro substituted phenyl rings attached to pyrazolines exhibited the highest activity against both types of organisms. The derivatives with an unsubstituted phenyl group attached to pyrazolines exhibited comparatively less activity. Thus it can be concluded that pyrazolines containing substituted phenyl groups are effective broad spectrum antibacterial agents, and they can be developed as effective antibacterial agents.

Vinod B

A comparative study of social and economic aspect of migration

India is a country of immense diversity. It is home to people of many different racial, languages, ethnic, religious, and national backgrounds. Groups of people in India differ from each other not only in physical or demographic characteristics but also in distinctive patterns of behavior and these patterns are determined by social and cultural factors like language, region, religion, and caste. Apart from behaviour, economic development, level of education and political culture of the people in various social segments differ from region to region. More you can say that economy and cultures have been enriched by the contributions of migrants from round the globe. In an increasingly globalised world, migratory movements is continuously shaping the countries all over the world. Some countries like India and Ireland, which set the example of economic development and social integration, have the positive impact of the migration by globalisation and some countries like USA, which recently witness racism, xenophobia and discrimination have the negative impact on the migrants. It does not mean India do not face fragmentation and USA do not have cohesion. USA have many stories which show successful integration process, that facilitated the lives of immigrant communities, but being a developed country it still suffers from cultural alienation. In these countries, borders are built within borders to create cultural divides that do not allow people to integrate. Recently, this problem has become more prominent due to the rise of terrorism, clash of cultures in the world, leading to the glorification of stereotypes. People are becoming less accepting towards anyone who does not belong to their region. Migration does not stop after people move from one place to another place. The main question start after that ‘now what’ they will do. That is why this topic needs to be discussed thoroughly in order to find better solutions. This paper will begin with an analysis of different approaches to Migration, discuss the target groups for integration policies, provide indicators of the current situation of migrants and proceed to an analysis of integration tools: legislation, social policies and participatory processes. It will focus not only on the impact of migration but also on social integration, mix culture like indo-western culture in a comparative basis.

Ekta Meena

A comparative study of social and economic aspect of migration

India is a country of immense diversity. It is home to people of many different racial, languages, ethnic, religious, and national backgrounds. Groups of people in India differ from each other not only in physical or demographic characteristics but also in distinctive patterns of behavior and these patterns are determined by social and cultural factors like language, region, religion, and caste. Apart from behaviour, economic development, level of education and political culture of the people in various social segments differ from region to region. More you can say that economy and cultures have been enriched by the contributions of migrants from round the globe. In an increasingly globalised world, migratory movements is continuously shaping the countries all over the world. Some countries like India and Ireland, which set the example of economic development and social integration, have the positive impact of the migration by globalisation and some countries like USA, which recently witness racism, xenophobia and discrimination have the negative impact on the migrants. It does not mean India do not face fragmentation and USA do not have cohesion. USA have many stories which show successful integration process, that facilitated the lives of immigrant communities, but being a developed country it still suffers from cultural alienation. In these countries, borders are built within borders to create cultural divides that do not allow people to integrate. Recently, this problem has become more prominent due to the rise of terrorism, clash of cultures in the world, leading to the glorification of stereotypes. People are becoming less accepting towards anyone who does not belong to their region. Migration does not stop after people move from one place to another place. The main question start after that ‘now what’ they will do. That is why this topic needs to be discussed thoroughly in order to find better solutions. This paper will begin with an analysis of different approaches to Migration, discuss the target groups for integration policies, provide indicators of the current situation of migrants and proceed to an analysis of integration tools: legislation, social policies and participatory processes. It will focus not only on the impact of migration but also on social integration, mix culture like indo-western culture in a comparative basis.

Ekta Meena

Study of temperature variation in human peripheral region during wound healing process due to plastic surgery

In this paper, investigations are made to analyze the human body temperature during wound healing process due to surgery. Wound is considered after the skin graft. Skin graft is a technique used in plastic surgery. Skin is the first line of defense between the human and environment, it is very susceptible to damage. Internal body or core temperature (Tb) is one of the clinical vital signs along with pulse and respiratory rates. Any disturbance in body temperature will drive complexities in wound healing process. These studies are important in the mechanism of establishing the limits of thermal regulation of human body during the healing process in different situations and conditions. The Finite element method is used to analyze tissues temperature for normal tissues (donor site) and abnormal tissues (tissues after surgery). Appropriate boundary conditions have been framed. Numerical results are obtained using Crank Nicolson Method.

Manisha Jain

Metapuf: a challenge response pair generator

Physically unclonable function (PUF) is a hardware security module preferred for hardware feature based random number and secret key generation. Security of a cryptographic system relies on the quality of the challenge-response pair, it is necessary that the key generation mechanism must unpredictable and its response should constant under different operating condition. Metastable state in CMOS latch is undesirable since it response becomes unpredictable, this feature used in this work to generate a unique response. A feedback mechanism is developed which forces the latch into the metastable region; after metastable state, latch settle to high or state depends on circuit internal condition and noise which cannot be predicted. Obtained inter hamming variation for 8 PUF is 51% and average intra hamming distance is 99.76% with supply voltage variation and 96.22% with temperature variation.

Abhishek Kumar

Intersection of caste and gender based subjugation

One of the unique features of Indian society is prevalence of caste system which was originated thousands of years back to demarcate the people engaged in different occupation or jobs. Initially it was not much rigid but gradually people belonging to upper castes for their own selfish means to maintain their monopoly made this arrangement hereditary and started treating people of lower castes disgracefully. For preservation of this system, people started controlling their women to prevent inter-caste marriages and the concept of endogamy came up. This robbed away many types of freedom from women. For women belonging to lower castes, this situation is worse as they are doubly subjugated on the basis on caste as well as gender. Men belonging to their own caste treat them as secondary beings. This paper throws light on this intersection. How intersection of these two kinds of inequalities place them at the lowest position in Indian society. Dr. B.R. Ambedkar rises as their leader who all his life worked for empowerment of downtrodden section of society. He argues that education is the primary tool for evading these differences among people. He further emphasizes to adopt the concept of exogamy to break the backbone of Indian caste system and to immediately leave a religion or culture which legitimizes such system of inequality among people of the same land.

Swati sharma

Intersection of caste and gender based subjugation

One of the unique features of Indian society is prevalence of caste system which was originated thousands of years back to demarcate the people engaged in different occupation or jobs. Initially it was not much rigid but gradually people belonging to upper castes for their own selfish means to maintain their monopoly made this arrangement hereditary and started treating people of lower castes disgracefully. For preservation of this system, people started controlling their women to prevent inter-caste marriages and the concept of endogamy came up. This robbed away many types of freedom from women. For women belonging to lower castes, this situation is worse as they are doubly subjugated on the basis on caste as well as gender. Men belonging to their own caste treat them as secondary beings. This paper throws light on this intersection. How intersection of these two kinds of inequalities place them at the lowest position in Indian society. Dr. B.R. Ambedkar rises as their leader who all his life worked for empowerment of downtrodden section of society. He argues that education is the primary tool for evading these differences among people. He further emphasizes to adopt the concept of exogamy to break the backbone of Indian caste system and to immediately leave a religion or culture which legitimizes such system of inequality among people of the same land.

Swati sharma

In-silico drug design, synthesis, characterization and biological evaluation of 2-azetidinone derivatives for antileukemic activity

2-Azetidinone shows biological activities like anti-bacterial, anti-microbial activity, anti-tubercular activity, and anti-cancer activity. 2-azetdinone derivatives were synthesized by simple procedures. The first step is synthesis of benzohydrazide through nucleophilic substitution reaction between methyl benzoate and hydrazine hydrate. The above formed compound is then treated with substituted aromatic aldehydes in the presence of catalytic amount of concentrated hydrochloric acid with stirring for one hour to give benzohydrazone which results in the formation of Schiff bases.Schiff bases undergone cyclisation in the presence of chloroacetylchloride and diethylenediamine by using ethanol as a solvent upon stirring for 4 hour’s yielded 2-azetidinone derivatives. The in-silico anti-leukemic activity was determined by using the computational tools i.e. “PASS Online”, “AutoDock4.2” and “ADMET” properties by online software’s. Among these six derivatives compounds (AZT-6) was shown more activity when compared with the other five compounds.

M. Yaswanth

Dimethyl sulfoxide in cryopreservation: an overview

Cryopreservation is a process that preserves intact living cells, tissues or any other biological constructs by cooling and storing the samples to very low temperatures in order to maintain their viability and to save them for future use. At very low temperatures, enzymatic and chemical activities that may cause harm to the biological material are effectively stopped. Cryopreservation methods look to reach very low temperatures without causing further harm caused by the creation of ice crystals during freezing. Cryopreservation human samples for storage including variety of diseases such as cancer, genetic and degenerative disorders and bio-banking. This review aims to describe and highlight dimethyl sulfoxide in cryopreservation. Dimethyl sulfoxide is a non-toxic solvent and is one of the most commonly used pharmaceutical agent with a varied range of pharmacological actions including membrane penetration, anti-inflammatory effects and local analgesia as well as weak bacteriostatic. The main use of dimethyl sulfoxide is a vehicle for some drugs to enhancing the action of the drug and helping penetration of other drugs into the skin. However, dimethyl sulfoxide has been the cryopreservative agent of choice in situation to its exceptional performance in mitigating freezing-related damages. It is frequently used in cell banking applications as a cryoprotectant. When added to media, it prevents intracellular and extracellular crystals from forming in cells during the freezing process. There has been a concern over the toxicity of dimethyl sulfoxide and its potential side effects in different highly concentration after administration to patients. Therefore, there has been growing demand for robust dimethyl sulfoxide for cryopreservation method that can improve safety and maintain potency and efficacy

Mediterranean Journal of Pharmacy and Pharmaceutical Sciences

Improvement of injection conditions for zone electrophoresis of proteins in capillaries coated with n, n-didodecyl-n, n-dimethylammonium bromide

Fused silica capillaries treated with N, N-didodecyl-N, N-dimethylammonium bromide was used in capillary electrophoresis to separate basic proteins using ammonium acetate as BGE at pH 4.0, 70 mM. This surfactant forms a semi-stable coating that provides a strong anodic electroosmosis; however, such coating must regularly be regenerated to maintain efficiency and reproducibility. The temporal stability of the coating was greatly improved by a new procedure as described in previously study by our group. In this study, it is found such experimental conditions that the starting zone could be enriched without loss of sample. The injection of a short plug of the BGE diluted 100 times for 3 sec in 50 µm i.d. capillaries behind the sample zone at 15 kV gave the best performance, whereas, a plug of lower dilution degree (10 times) in 25 µm i.d injected for 3 sec at the same field strength gave the optimum results for this dimension. In conclusion, those conditions were found to effectively decrease the loss of sample and to give a higher separation performance in regard to peak efficiency and resolution compared to injecting the sample without a plug.

Mediterranean Journal of Pharmacy and Pharmaceutical Sciences

Pyrazole carbaldehyes as antiinflammatory agents-synthesis and in vitro membrane stabilization method

Pyrazole is a nitrogen containing 5-membered heterocyclic compound containing 3 carbons& 2 nitrogen atoms in the adjacent position of ring structure and is chemically known as 1, 2- diazole. Pyrazole nucleus is present in many pharmaceutically important compounds and intermediates . Majority of anti-inflammatory agents currently employed have GI irritation and enhanced acidity as side effects. As part of our efforts to develop newer and effective anti-inflammatory agents , ten newer pyrazole carbaldehydes were synthesized and evaluated for their anti-inflammatory activity using Diclofenac was the standard. Out of ten compounds synthesized, all compounds exhibited comparable activity with that of the standard.Highest percentage of haemolysis was observed for Pyrazole carbaldehydes with methoxy phenyl groups as substituents. These compounds should be considered for developing as leads for newer & safer anti-inflammatory agents.

Vinod B

A review on the potential of remdesivir against sars cov2

Covid 19, the pandemic originated in the Chinese city of Wuhan, had the entire world conquered. The structure and transmission of the causative organism, Coronavirus is well studied. Remdesivir, the product of Gilead pharmaceuticals, was effective against many viral infections, including Ebola and SARS. It comes under the category of nucleoside prodrug and has given promising results in the early trials against SARS COV 19. In depth, research is taking place at a rapid pace, so that Remdesivir will be available to the therapeutic community as an effective remedy for the pandemic caused by SARS COV2. If this meets success, the darkest era in the modern history of mankind may become a memory in the near future.

Vinod B

Synthesis and broad spectrum antibacterial activities of 2-pyrazolines synthesized from chalcones

2-Pyrazolines are well known, and important nitrogen-containing five-membered heterocyclic compounds which belong to the family of azoles and have been found to possess considerable activities, like anticancer, antibacterial, antifungal, immunosuppressant and antiamoebic activity. In the present work, ten novel pyrazolines were prepared from chalcones, characterized and evaluated for their antibacterial activity against Staphylococcus aureus and Escherichia coli using Ciprofloxacin as standard and using DMSO as a solvent. Their activity was evaluated by measuring the zone of inhibition in mm. All the compounds exhibited antibacterial activity against Staphylococcus aureus and Escherichia coli. Among ten derivatives of compounds synthesized, the derivative with 2-chloro and 4-chloro substituted phenyl rings attached to pyrazolines exhibited the highest activity against both types of organisms. The derivatives with an unsubstituted phenyl group attached to pyrazolines exhibited comparatively less activity. Thus it can be concluded that pyrazolines containing substituted phenyl groups are effective broad spectrum antibacterial agents, and they can be developed as effective antibacterial agents.

Vinod B

A comparative study of social and economic aspect of migration

India is a country of immense diversity. It is home to people of many different racial, languages, ethnic, religious, and national backgrounds. Groups of people in India differ from each other not only in physical or demographic characteristics but also in distinctive patterns of behavior and these patterns are determined by social and cultural factors like language, region, religion, and caste. Apart from behaviour, economic development, level of education and political culture of the people in various social segments differ from region to region. More you can say that economy and cultures have been enriched by the contributions of migrants from round the globe. In an increasingly globalised world, migratory movements is continuously shaping the countries all over the world. Some countries like India and Ireland, which set the example of economic development and social integration, have the positive impact of the migration by globalisation and some countries like USA, which recently witness racism, xenophobia and discrimination have the negative impact on the migrants. It does not mean India do not face fragmentation and USA do not have cohesion. USA have many stories which show successful integration process, that facilitated the lives of immigrant communities, but being a developed country it still suffers from cultural alienation. In these countries, borders are built within borders to create cultural divides that do not allow people to integrate. Recently, this problem has become more prominent due to the rise of terrorism, clash of cultures in the world, leading to the glorification of stereotypes. People are becoming less accepting towards anyone who does not belong to their region. Migration does not stop after people move from one place to another place. The main question start after that ‘now what’ they will do. That is why this topic needs to be discussed thoroughly in order to find better solutions. This paper will begin with an analysis of different approaches to Migration, discuss the target groups for integration policies, provide indicators of the current situation of migrants and proceed to an analysis of integration tools: legislation, social policies and participatory processes. It will focus not only on the impact of migration but also on social integration, mix culture like indo-western culture in a comparative basis.

Ekta Meena

A comparative study of social and economic aspect of migration

India is a country of immense diversity. It is home to people of many different racial, languages, ethnic, religious, and national backgrounds. Groups of people in India differ from each other not only in physical or demographic characteristics but also in distinctive patterns of behavior and these patterns are determined by social and cultural factors like language, region, religion, and caste. Apart from behaviour, economic development, level of education and political culture of the people in various social segments differ from region to region. More you can say that economy and cultures have been enriched by the contributions of migrants from round the globe. In an increasingly globalised world, migratory movements is continuously shaping the countries all over the world. Some countries like India and Ireland, which set the example of economic development and social integration, have the positive impact of the migration by globalisation and some countries like USA, which recently witness racism, xenophobia and discrimination have the negative impact on the migrants. It does not mean India do not face fragmentation and USA do not have cohesion. USA have many stories which show successful integration process, that facilitated the lives of immigrant communities, but being a developed country it still suffers from cultural alienation. In these countries, borders are built within borders to create cultural divides that do not allow people to integrate. Recently, this problem has become more prominent due to the rise of terrorism, clash of cultures in the world, leading to the glorification of stereotypes. People are becoming less accepting towards anyone who does not belong to their region. Migration does not stop after people move from one place to another place. The main question start after that ‘now what’ they will do. That is why this topic needs to be discussed thoroughly in order to find better solutions. This paper will begin with an analysis of different approaches to Migration, discuss the target groups for integration policies, provide indicators of the current situation of migrants and proceed to an analysis of integration tools: legislation, social policies and participatory processes. It will focus not only on the impact of migration but also on social integration, mix culture like indo-western culture in a comparative basis.

Ekta Meena

Study of temperature variation in human peripheral region during wound healing process due to plastic surgery

In this paper, investigations are made to analyze the human body temperature during wound healing process due to surgery. Wound is considered after the skin graft. Skin graft is a technique used in plastic surgery. Skin is the first line of defense between the human and environment, it is very susceptible to damage. Internal body or core temperature (Tb) is one of the clinical vital signs along with pulse and respiratory rates. Any disturbance in body temperature will drive complexities in wound healing process. These studies are important in the mechanism of establishing the limits of thermal regulation of human body during the healing process in different situations and conditions. The Finite element method is used to analyze tissues temperature for normal tissues (donor site) and abnormal tissues (tissues after surgery). Appropriate boundary conditions have been framed. Numerical results are obtained using Crank Nicolson Method.

Manisha Jain

Metapuf: a challenge response pair generator

Physically unclonable function (PUF) is a hardware security module preferred for hardware feature based random number and secret key generation. Security of a cryptographic system relies on the quality of the challenge-response pair, it is necessary that the key generation mechanism must unpredictable and its response should constant under different operating condition. Metastable state in CMOS latch is undesirable since it response becomes unpredictable, this feature used in this work to generate a unique response. A feedback mechanism is developed which forces the latch into the metastable region; after metastable state, latch settle to high or state depends on circuit internal condition and noise which cannot be predicted. Obtained inter hamming variation for 8 PUF is 51% and average intra hamming distance is 99.76% with supply voltage variation and 96.22% with temperature variation.

Abhishek Kumar

Intersection of caste and gender based subjugation

One of the unique features of Indian society is prevalence of caste system which was originated thousands of years back to demarcate the people engaged in different occupation or jobs. Initially it was not much rigid but gradually people belonging to upper castes for their own selfish means to maintain their monopoly made this arrangement hereditary and started treating people of lower castes disgracefully. For preservation of this system, people started controlling their women to prevent inter-caste marriages and the concept of endogamy came up. This robbed away many types of freedom from women. For women belonging to lower castes, this situation is worse as they are doubly subjugated on the basis on caste as well as gender. Men belonging to their own caste treat them as secondary beings. This paper throws light on this intersection. How intersection of these two kinds of inequalities place them at the lowest position in Indian society. Dr. B.R. Ambedkar rises as their leader who all his life worked for empowerment of downtrodden section of society. He argues that education is the primary tool for evading these differences among people. He further emphasizes to adopt the concept of exogamy to break the backbone of Indian caste system and to immediately leave a religion or culture which legitimizes such system of inequality among people of the same land.

Swati sharma

Intersection of caste and gender based subjugation

One of the unique features of Indian society is prevalence of caste system which was originated thousands of years back to demarcate the people engaged in different occupation or jobs. Initially it was not much rigid but gradually people belonging to upper castes for their own selfish means to maintain their monopoly made this arrangement hereditary and started treating people of lower castes disgracefully. For preservation of this system, people started controlling their women to prevent inter-caste marriages and the concept of endogamy came up. This robbed away many types of freedom from women. For women belonging to lower castes, this situation is worse as they are doubly subjugated on the basis on caste as well as gender. Men belonging to their own caste treat them as secondary beings. This paper throws light on this intersection. How intersection of these two kinds of inequalities place them at the lowest position in Indian society. Dr. B.R. Ambedkar rises as their leader who all his life worked for empowerment of downtrodden section of society. He argues that education is the primary tool for evading these differences among people. He further emphasizes to adopt the concept of exogamy to break the backbone of Indian caste system and to immediately leave a religion or culture which legitimizes such system of inequality among people of the same land.

Swati sharma

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