AJMER S I N G H GREWAL (original) (raw)
Papers by AJMER S I N G H GREWAL
International Journal of Pharmaceutical Sciences Review and Research, Oct 20, 2011
... Suparna kumar Das*, Ajmer singh Grewal, Mrityunjay Banerjee Dept. ... 8. Ghosh Amitava, Chakr... more ... Suparna kumar Das*, Ajmer singh Grewal, Mrityunjay Banerjee Dept. ... 8. Ghosh Amitava, Chakrabarti Piyali, Roy Partha, Bhadury Somnath, Nag Tanushree And Sarkar Simli Bioremediation Of Heavy Metals From Neem (Azadirachta Indica) Leaf Extract By Chelation With ...
Anti-inflammatory & anti-allergy agents in medicinal chemistry, Jan 16, 2017
Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyc... more Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors. The present work involved the synthesis of a series of newer substituted triazole amine derivatives followed by characterization using FTIR and 1H-NMR spectroscopy and their in silico evaluation by docking studies to determine the binding interactions for the best fit conformations in the binding site of PDE4 protein. Based on the results of the in silico studies, the selected compounds were tested for the anti-inflammatory activity using carrageenan-induced paw oedema method. The yields ...
Letters in Drug Design & Discovery, 2016
Current Topics in Medicinal Chemistry, 2016
International Journal of Pharmtech Research, Nov 20, 2014
Some new compounds derived from imidazo [1,2-a]pyridine, The newly synthesized compounds were cha... more Some new compounds derived from imidazo [1,2-a]pyridine, The newly synthesized compounds were characterized by elemental analysis, IR, 1H NMR and mass spectra. All the compounds have been evaluated for their in vitro biological assay like antibacterial activity towards Gram positive and Gram negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40µg/ml. The biological activities of synthesized compounds were compared with standard drugs.
Mini reviews in medicinal chemistry, 2015
Diabetes mellitus occurrence has been associated to the modification of the physiological levels ... more Diabetes mellitus occurrence has been associated to the modification of the physiological levels of glucose and is often accompanied by several long-term complications, namely neuropathy, nephropathy, retinopathy, cataract, and cardiovascular. Aldose reductase (AR) is an enzyme of aldoketo reductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathway of glucose metabolism. In this context, aldose reductase inhibitors (ARIs) have received much attention worldwide. Decreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of major complications of diabetes. The present review article describes a brief overview of the role of aldose reductase in the diabetic complications, advances achieved on ARIs and their potential use in the treatment and management of the major diabetic complications such as cataract, retinopathy, neuropathy, nephropathy and cardiovascular. The ARIs developed vary structurally, and rep...
Applied Clinical Research, Clinical Trials and Regulatory Affairs, 2015
International Journal of Pharmaceutical Sciences and Research, Jul 21, 2012
Three simple sensitive, rapid, accurate and economical methods were developed for simultaneous es... more Three simple sensitive, rapid, accurate and economical methods were developed for simultaneous estimation of Ciprofloxacin & Ornidazole in bulk and its pharmaceutical formulations. First method was based on the simultaneous equation, second method was based on Q-Analysis (Absorbance ratio method) and third method was based on multicomponent mode. The absorption maxima for Ciprofloxacin and Ornidazole were 272 nm and 319 nm in 0.1 N NaOH respectively. The iso-absorptive point for Ciprofloxacin Hydrochloride and Ornidazole was 292 nm. The calibration curve was linear over the concentration range 2.5 to 22.5 µg/ml of Ciprofloxacin & Ornidazole. The methods had been validated statistically and by recovery study. It can be used in the simultaneous estimation of Ciprofloxacin and Ornidazole in bulk drugs and its pharmaceutical preparations in a routine manner.
Mini-Reviews in Medicinal Chemistry, 2015
Diabetes mellitus occurrence has been associated to the modification of the physiological levels ... more Diabetes mellitus occurrence has been associated to the modification of the physiological levels of glucose and is often accompanied by several long-term complications, namely neuropathy, nephropathy, retinopathy, cataract, and cardiovascular. Aldose reductase (AR) is an enzyme of aldoketo reductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathway of glucose metabolism. In this context, aldose reductase inhibitors (ARIs) have received much attention worldwide. Decreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of major complications of diabetes. The present review article describes a brief overview of the role of aldose reductase in the diabetic complications, advances achieved on ARIs and their potential use in the treatment and management of the major diabetic complications such as cataract, retinopathy, neuropathy, nephropathy and cardiovascular. The ARIs developed vary structurally, and representative structural classes of ARIs include i) carboxylic acid derivatives (such as Epalrestat, Alrestatin, Zopalrestat, Zenarestat, Ponalrestat, Lidorestat, and Tolrestat), ii) spirohydantoins and related cyclic amides (such as Sorbinil, Minalrestat, and Fidarestat), and iii) phenolic derivatives (related to Benzopyran-4-one and Chalcone). Among these inhibitors, Epalrestat is the only commercially available inhibitor till date. In addition, some other ARIs such as Sorbinil and Ranirestat had been advanced into late stage of clinical trials and found to be safe for human use. The role of various natural ARIs in management of diabetic complications will be discussed. Adapting ARIs could prevent sepsis complications, prevent angiogenesis, ameliorate mild or asymptomatic diabetic cardiovascular autonomic neuropathy and appear to be a promising strategy for the treatment of endotoxemia and other ROS-induced inflammatory diseases. The role of ARIs in non-diabetic diseases will also be discussed.
Medicinal chemistry (Shariqah (United Arab Emirates)), Jan 24, 2015
Metabolic syndrome is a disorder described by reduced insulin sensitivity, overweight, hyperlipid... more Metabolic syndrome is a disorder described by reduced insulin sensitivity, overweight, hyperlipidaemia, high blood pressure and myocardial disorders, mainly due to high fat diet and lack of physical activity. The peroxisome proliferator activated receptors (PPARs) are type II nuclear hormone receptors that regulate a number of processes in living systems, such as metabolism of carbohydrates and fatty acids, growth and differentiation of cell, and inflammatory reactions. Alpha, gamma and delta are the three distinct isoforms of PPAR. The stimulation of PPARδ alters body's energy fuel preference from glucose to fat. The PPARδ isoform is expressed ubiquitously in all tissues, especially in those tissues which involved in metabolism of lipids like adipose tissue, liver, kidney, and muscle. Currently, PPARδ is an emerging therapeutic target for the pharmacological therapy of disorders associated with metabolic syndrome. Several PPARδ selective agonists had been reported in last ten y...
International Journal of PharmTech Research
In the present article synthesis and evaluation for antibacterial and antifungal activity of a ne... more In the present article synthesis and evaluation for antibacterial and antifungal activity of a new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives is described. 2,5-disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of quinolinyl hydrazone derivatives with dichloromethane. The compounds (6a-h) were characterized by IR, NMR, and mass spectroscopy. All the synthesized compounds were screened for their antimicrobial activity. The antimicrobial results reveal that among the synthesized compounds 6b and 6f showed excellent antibacterial and antifungal activity. The compounds 6c, 6d and 6e did not show antifungal activity against the Colletotrichum capsici.
The pharmaceutical formulations for human use are required to meet standards which relate to thei... more The pharmaceutical formulations for human use are required to meet standards which relate to their safety and efficacy. The evaluation of safety and efficacy of multi-component pharmaceutical formulations is dependent upon the existence of adequate methods for quality control of the product. Simultaneous estimation methods are now being used more frequently for estimation of drugs in multi-component pharmaceutical formulations due to their inherent advantages such as avoid time consuming extraction and separation; and are economical. For the estimation of multi-component formulation, the instrumental techniques, which are commonly employed, are UV spectrophotometry, gas liquid chromatography, high performance thin layer chromatography, and high performance liquid chromatography. These methods are based upon the measurement of specific and non-specific physical properties of the substances. Chromatographic separation techniques are one of the most widely used techniques for analysis ...
The main objective was to develop and validate asimple, accurate, precise and sensitive ion-pair ... more The main objective was to develop and validate asimple, accurate, precise and sensitive ion-pair spectrophotometric extraction method for the assay of Ciprofloxacin (CFX) in pure drug and tablets. The method is based upon the reaction of Ciprofloxacin with methyl orange, forming a yellow colour complex in acidic medium, which is extracted in chloroform and analyzed. The extracted complexes showed absorbance maxima (λmax) found to be at 429 nm. Beer's law was obeyed for a wide concentration range i.e.100-700 µg/mL as the extracted species seemed well defined and stable. Surface or an interphase adsorption phenomenon was not a problem. Optimization of the reaction was carried out with factors such as buffer strength, stability of complex, molar ratio of drug: dye and extraction time. The proposed method was validated as per ICH guidelines Q 2. The recovery studies confirmed the accuracy and precision of the method. The above method was a rapid tool for routine analysis of Ciproflo...
Green Chemistry with its twelve principles would like to see changes in the conventional chemical... more Green Chemistry with its twelve principles would like to see changes in the conventional chemical synthesis and the use of less toxic starting materials. Green Chemistry would like to increases the efficiency of synthetic methods, to use less toxic solvents, reduce the stages of the synthetic routes and minimize waste as far as practically possible. In this way, chemical synthesis will be part of the effort for sustainable development. Microwave assisted synthesis has revolutionized chemical synthesis. Small molecules can be built in a fraction of the time required by conventional methods. In conventional heating methods oil bath or hot plate are used as a source of heat to a chemical reaction Microwave irradiation is widely used as a source of heating in chemical synthesis. The basic mechanisms observed in microwave assisted synthesis are dipolar polarization and conduction. Microwave-assisted synthesis provides clean synthesis with the advantage of enhanced reaction rates, higher ...
International Journal of ChemTech Research
The main objective was to develop and validate a simple, accurate, precise and sensitive ion-pair... more The main objective was to develop and validate a simple, accurate, precise and sensitive ion-pair spectrophotometric extraction method for the assay of Ornidazole in pure drug and tablets. The method is based upon reduction of ornidazole and reaction of reduced ornidazole with orcinol to form yellow coloured ornidazole-orcinol complex. The colored complex obeyed Beer’s law in the concentration range of 10-60 μg/ml at λmax of 420 nm. The proposed method was validated as per ICH guidelines Q 2. The recovery studies confirmed the accuracy and precision of the method. The above method was a rapid tool for routine analysis of Ornidazole in the bulk and pharmaceutical dosage forms.
Mini-Reviews in Medicinal Chemistry, 2014
Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primar... more Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells. Small molecules called glucokinase activators (GKAs) which bind to an allosteric activator site of the GK enzyme have indeed been discovered and developed, and thus hold great promise as new, effective and safe antidiabetic agents. GKAs enhance the catalytic activity of GK and promising clinical trials in humans demonstrated that they are highly useful in the treatment of type 2 diabetes mellitus. Most of the reported GKAs include amide derivatives like benzamides, acrylamides, carboxamides, acetamides and acrylamides. Examples include Piragliatin, AZD1656, AZD6370, R1440 GKA2, GKA 50, YH GKA, PSN 010, and LY2121260. Recent findings on GKAs including lead compounds and overview of current hypothesis on mechanism of GK activation along with summary of the recently published patents as well as the GKAs of natural origin are reported in the present review.
International Journal of Pharmaceutical Sciences Review and Research, Oct 20, 2011
... Suparna kumar Das*, Ajmer singh Grewal, Mrityunjay Banerjee Dept. ... 8. Ghosh Amitava, Chakr... more ... Suparna kumar Das*, Ajmer singh Grewal, Mrityunjay Banerjee Dept. ... 8. Ghosh Amitava, Chakrabarti Piyali, Roy Partha, Bhadury Somnath, Nag Tanushree And Sarkar Simli Bioremediation Of Heavy Metals From Neem (Azadirachta Indica) Leaf Extract By Chelation With ...
Anti-inflammatory & anti-allergy agents in medicinal chemistry, Jan 16, 2017
Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyc... more Phosphodiesterase 4 (PDE4), one of the member of PDE superfamily catalyzes, the hydrolysis of cyclic adenosine monophosphate to adenosine monophosphate in pro-inflammatory and immunomodulatory cells leading to increased inflammatory processes. PDE4 has been reported as an attractive therapeutic target involved in various inflammatory disorders. The present work was designed to synthesize and evaluate the anti-inflammatory activity of some new triazole amine derivatives as potential PDE4 inhibitors. The present work involved the synthesis of a series of newer substituted triazole amine derivatives followed by characterization using FTIR and 1H-NMR spectroscopy and their in silico evaluation by docking studies to determine the binding interactions for the best fit conformations in the binding site of PDE4 protein. Based on the results of the in silico studies, the selected compounds were tested for the anti-inflammatory activity using carrageenan-induced paw oedema method. The yields ...
Letters in Drug Design & Discovery, 2016
Current Topics in Medicinal Chemistry, 2016
International Journal of Pharmtech Research, Nov 20, 2014
Some new compounds derived from imidazo [1,2-a]pyridine, The newly synthesized compounds were cha... more Some new compounds derived from imidazo [1,2-a]pyridine, The newly synthesized compounds were characterized by elemental analysis, IR, 1H NMR and mass spectra. All the compounds have been evaluated for their in vitro biological assay like antibacterial activity towards Gram positive and Gram negative bacterial strains and antifungal activity towards Aspergillus niger at a concentration of 40µg/ml. The biological activities of synthesized compounds were compared with standard drugs.
Mini reviews in medicinal chemistry, 2015
Diabetes mellitus occurrence has been associated to the modification of the physiological levels ... more Diabetes mellitus occurrence has been associated to the modification of the physiological levels of glucose and is often accompanied by several long-term complications, namely neuropathy, nephropathy, retinopathy, cataract, and cardiovascular. Aldose reductase (AR) is an enzyme of aldoketo reductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathway of glucose metabolism. In this context, aldose reductase inhibitors (ARIs) have received much attention worldwide. Decreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of major complications of diabetes. The present review article describes a brief overview of the role of aldose reductase in the diabetic complications, advances achieved on ARIs and their potential use in the treatment and management of the major diabetic complications such as cataract, retinopathy, neuropathy, nephropathy and cardiovascular. The ARIs developed vary structurally, and rep...
Applied Clinical Research, Clinical Trials and Regulatory Affairs, 2015
International Journal of Pharmaceutical Sciences and Research, Jul 21, 2012
Three simple sensitive, rapid, accurate and economical methods were developed for simultaneous es... more Three simple sensitive, rapid, accurate and economical methods were developed for simultaneous estimation of Ciprofloxacin & Ornidazole in bulk and its pharmaceutical formulations. First method was based on the simultaneous equation, second method was based on Q-Analysis (Absorbance ratio method) and third method was based on multicomponent mode. The absorption maxima for Ciprofloxacin and Ornidazole were 272 nm and 319 nm in 0.1 N NaOH respectively. The iso-absorptive point for Ciprofloxacin Hydrochloride and Ornidazole was 292 nm. The calibration curve was linear over the concentration range 2.5 to 22.5 µg/ml of Ciprofloxacin & Ornidazole. The methods had been validated statistically and by recovery study. It can be used in the simultaneous estimation of Ciprofloxacin and Ornidazole in bulk drugs and its pharmaceutical preparations in a routine manner.
Mini-Reviews in Medicinal Chemistry, 2015
Diabetes mellitus occurrence has been associated to the modification of the physiological levels ... more Diabetes mellitus occurrence has been associated to the modification of the physiological levels of glucose and is often accompanied by several long-term complications, namely neuropathy, nephropathy, retinopathy, cataract, and cardiovascular. Aldose reductase (AR) is an enzyme of aldoketo reductase super-family that catalyzes the conversion of glucose to sorbitol in the polyol pathway of glucose metabolism. In this context, aldose reductase inhibitors (ARIs) have received much attention worldwide. Decreased sorbitol flux through polyol pathway by ARIs could be an emerging target for the management of major complications of diabetes. The present review article describes a brief overview of the role of aldose reductase in the diabetic complications, advances achieved on ARIs and their potential use in the treatment and management of the major diabetic complications such as cataract, retinopathy, neuropathy, nephropathy and cardiovascular. The ARIs developed vary structurally, and representative structural classes of ARIs include i) carboxylic acid derivatives (such as Epalrestat, Alrestatin, Zopalrestat, Zenarestat, Ponalrestat, Lidorestat, and Tolrestat), ii) spirohydantoins and related cyclic amides (such as Sorbinil, Minalrestat, and Fidarestat), and iii) phenolic derivatives (related to Benzopyran-4-one and Chalcone). Among these inhibitors, Epalrestat is the only commercially available inhibitor till date. In addition, some other ARIs such as Sorbinil and Ranirestat had been advanced into late stage of clinical trials and found to be safe for human use. The role of various natural ARIs in management of diabetic complications will be discussed. Adapting ARIs could prevent sepsis complications, prevent angiogenesis, ameliorate mild or asymptomatic diabetic cardiovascular autonomic neuropathy and appear to be a promising strategy for the treatment of endotoxemia and other ROS-induced inflammatory diseases. The role of ARIs in non-diabetic diseases will also be discussed.
Medicinal chemistry (Shariqah (United Arab Emirates)), Jan 24, 2015
Metabolic syndrome is a disorder described by reduced insulin sensitivity, overweight, hyperlipid... more Metabolic syndrome is a disorder described by reduced insulin sensitivity, overweight, hyperlipidaemia, high blood pressure and myocardial disorders, mainly due to high fat diet and lack of physical activity. The peroxisome proliferator activated receptors (PPARs) are type II nuclear hormone receptors that regulate a number of processes in living systems, such as metabolism of carbohydrates and fatty acids, growth and differentiation of cell, and inflammatory reactions. Alpha, gamma and delta are the three distinct isoforms of PPAR. The stimulation of PPARδ alters body's energy fuel preference from glucose to fat. The PPARδ isoform is expressed ubiquitously in all tissues, especially in those tissues which involved in metabolism of lipids like adipose tissue, liver, kidney, and muscle. Currently, PPARδ is an emerging therapeutic target for the pharmacological therapy of disorders associated with metabolic syndrome. Several PPARδ selective agonists had been reported in last ten y...
International Journal of PharmTech Research
In the present article synthesis and evaluation for antibacterial and antifungal activity of a ne... more In the present article synthesis and evaluation for antibacterial and antifungal activity of a new series of 2,5-disubstituted-1,3,4-oxadiazole derivatives is described. 2,5-disubstituted-1,3,4-oxadiazole derivatives were synthesized by the reaction of quinolinyl hydrazone derivatives with dichloromethane. The compounds (6a-h) were characterized by IR, NMR, and mass spectroscopy. All the synthesized compounds were screened for their antimicrobial activity. The antimicrobial results reveal that among the synthesized compounds 6b and 6f showed excellent antibacterial and antifungal activity. The compounds 6c, 6d and 6e did not show antifungal activity against the Colletotrichum capsici.
The pharmaceutical formulations for human use are required to meet standards which relate to thei... more The pharmaceutical formulations for human use are required to meet standards which relate to their safety and efficacy. The evaluation of safety and efficacy of multi-component pharmaceutical formulations is dependent upon the existence of adequate methods for quality control of the product. Simultaneous estimation methods are now being used more frequently for estimation of drugs in multi-component pharmaceutical formulations due to their inherent advantages such as avoid time consuming extraction and separation; and are economical. For the estimation of multi-component formulation, the instrumental techniques, which are commonly employed, are UV spectrophotometry, gas liquid chromatography, high performance thin layer chromatography, and high performance liquid chromatography. These methods are based upon the measurement of specific and non-specific physical properties of the substances. Chromatographic separation techniques are one of the most widely used techniques for analysis ...
The main objective was to develop and validate asimple, accurate, precise and sensitive ion-pair ... more The main objective was to develop and validate asimple, accurate, precise and sensitive ion-pair spectrophotometric extraction method for the assay of Ciprofloxacin (CFX) in pure drug and tablets. The method is based upon the reaction of Ciprofloxacin with methyl orange, forming a yellow colour complex in acidic medium, which is extracted in chloroform and analyzed. The extracted complexes showed absorbance maxima (λmax) found to be at 429 nm. Beer's law was obeyed for a wide concentration range i.e.100-700 µg/mL as the extracted species seemed well defined and stable. Surface or an interphase adsorption phenomenon was not a problem. Optimization of the reaction was carried out with factors such as buffer strength, stability of complex, molar ratio of drug: dye and extraction time. The proposed method was validated as per ICH guidelines Q 2. The recovery studies confirmed the accuracy and precision of the method. The above method was a rapid tool for routine analysis of Ciproflo...
Green Chemistry with its twelve principles would like to see changes in the conventional chemical... more Green Chemistry with its twelve principles would like to see changes in the conventional chemical synthesis and the use of less toxic starting materials. Green Chemistry would like to increases the efficiency of synthetic methods, to use less toxic solvents, reduce the stages of the synthetic routes and minimize waste as far as practically possible. In this way, chemical synthesis will be part of the effort for sustainable development. Microwave assisted synthesis has revolutionized chemical synthesis. Small molecules can be built in a fraction of the time required by conventional methods. In conventional heating methods oil bath or hot plate are used as a source of heat to a chemical reaction Microwave irradiation is widely used as a source of heating in chemical synthesis. The basic mechanisms observed in microwave assisted synthesis are dipolar polarization and conduction. Microwave-assisted synthesis provides clean synthesis with the advantage of enhanced reaction rates, higher ...
International Journal of ChemTech Research
The main objective was to develop and validate a simple, accurate, precise and sensitive ion-pair... more The main objective was to develop and validate a simple, accurate, precise and sensitive ion-pair spectrophotometric extraction method for the assay of Ornidazole in pure drug and tablets. The method is based upon reduction of ornidazole and reaction of reduced ornidazole with orcinol to form yellow coloured ornidazole-orcinol complex. The colored complex obeyed Beer’s law in the concentration range of 10-60 μg/ml at λmax of 420 nm. The proposed method was validated as per ICH guidelines Q 2. The recovery studies confirmed the accuracy and precision of the method. The above method was a rapid tool for routine analysis of Ornidazole in the bulk and pharmaceutical dosage forms.
Mini-Reviews in Medicinal Chemistry, 2014
Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primar... more Glucose-phosphorylating enzyme, glucokinase (GK) plays a major role in glucose homeostasis primarily through its regulatory actions in pancreatic β-cells and liver hepatocytes. Conversion of glucose to glucose-6-phosphate by GK promotes glycogen synthesis in liver hepatocytes, and insulin release in the pancreatic β-cells. Small molecules called glucokinase activators (GKAs) which bind to an allosteric activator site of the GK enzyme have indeed been discovered and developed, and thus hold great promise as new, effective and safe antidiabetic agents. GKAs enhance the catalytic activity of GK and promising clinical trials in humans demonstrated that they are highly useful in the treatment of type 2 diabetes mellitus. Most of the reported GKAs include amide derivatives like benzamides, acrylamides, carboxamides, acetamides and acrylamides. Examples include Piragliatin, AZD1656, AZD6370, R1440 GKA2, GKA 50, YH GKA, PSN 010, and LY2121260. Recent findings on GKAs including lead compounds and overview of current hypothesis on mechanism of GK activation along with summary of the recently published patents as well as the GKAs of natural origin are reported in the present review.