Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P169
K. Devi, K. Kumar, G. Krishnaveni
A simple, sensitive, selective, accurate and economical spectrophoto-metric method have been described in the present work for the deter-mination of danazol in bulk drug and pharmaceutical formulations (tablets). Method is based on the formation of yellow coloured ion-association complexes between danazol and alizarine red S in acid medium followed by their extraction with chloroform, exhibiting absorption maxima at 430 nm, and obeying Beer′s law in the concen-tration range of 5-30 μg/mL. Statistical analysis of the results of the proposed methods reveals high accuracy and good precision. The proposed methods could be successfully extended to the commercial pharmaceutical formulations containing danazol.
{"title":"New Extractive Spectrophotometric Method Development and Validation for the Estimation of Danazol in Pharmaceutical Formulations","authors":"K. Devi, K. Kumar, G. Krishnaveni","doi":"10.14233/AJOMC.2019.AJOMC-P169","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P169","url":null,"abstract":"A simple, sensitive, selective, accurate and economical spectrophoto-metric method have been described in the present work for the deter-mination of danazol in bulk drug and pharmaceutical formulations (tablets). Method is based on the formation of yellow coloured ion-association complexes between danazol and alizarine red S in acid medium followed by their extraction with chloroform, exhibiting absorption maxima at 430 nm, and obeying Beer′s law in the concen-tration range of 5-30 μg/mL. Statistical analysis of the results of the proposed methods reveals high accuracy and good precision. The proposed methods could be successfully extended to the commercial pharmaceutical formulations containing danazol.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"2 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78976752","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P168
P. Sharma
8-Substituted-2,5-dihydro-1,5-benzothiazepine derivatives have been synthesized by the reaction of 1-(2-furyl)-3-(3,4-dimethoxyphenyl)-2-propenone with six 5-substiuted-2-minobenzenethiols in dry ethanol saturated with dry HCl gas and also in the presence of aluminium nitrate as catalyst in dry ethanol. All the newly synthesized compounds were characterized by analytical and spectral data comprising IR, 1H NMR, 13C NMR, 19F NMR and mass studies. All these compounds have also been evaluated for their antimicrobial assay against the Gram-positive bacteria, Staphylococcus aureus and the Gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The antifungal activity was found to be more significant than antibacterial activity.
{"title":"Antimicrobial Evaluation and Efficient Green Synthesis of 8-Substituted-2,5-dihydro-1,5-benzothiazepine Derivatives","authors":"P. Sharma","doi":"10.14233/AJOMC.2019.AJOMC-P168","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P168","url":null,"abstract":"8-Substituted-2,5-dihydro-1,5-benzothiazepine derivatives have been synthesized by the reaction of 1-(2-furyl)-3-(3,4-dimethoxyphenyl)-2-propenone with six 5-substiuted-2-minobenzenethiols in dry ethanol saturated with dry HCl gas and also in the presence of aluminium nitrate as catalyst in dry ethanol. All the newly synthesized compounds were characterized by analytical and spectral data comprising IR, 1H NMR, 13C NMR, 19F NMR and mass studies. All these compounds have also been evaluated for their antimicrobial assay against the Gram-positive bacteria, Staphylococcus aureus and the Gram-negative bacteria, Pseudomonas aeruginosa and the fungus, Candida albicans. The antifungal activity was found to be more significant than antibacterial activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88580837","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P164
B. Sujatha, P. Kamala
In the present report, an expeditious green synthetic approach was developed for the synthesis of α-aminophosphonates 5(a-j) in good yields through one-pot three component reaction (Kabachnik-Fields reaction) in solvent-free conditions under microwave irradiation. The newly synthesized compounds were characterized by IR, NMR (1H, 13C and 31P), mass and C, H, N analysis. The synthesized compounds were screened for their anti-inflammatory activity using rat paw edema method. Most of the compounds from the series showed significant (p < 0.05) anti-inflammatory activity.
{"title":"Microwave-Assisted Synthesis and Anti-inflammatory Activity Evaluation of α-Aminophosphonates","authors":"B. Sujatha, P. Kamala","doi":"10.14233/AJOMC.2019.AJOMC-P164","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P164","url":null,"abstract":"In the present report, an expeditious green synthetic approach was developed for the synthesis of α-aminophosphonates 5(a-j) in good yields through one-pot three component reaction (Kabachnik-Fields reaction) in solvent-free conditions under microwave irradiation. The newly synthesized compounds were characterized by IR, NMR (1H, 13C and 31P), mass and C, H, N analysis. The synthesized compounds were screened for their anti-inflammatory activity using rat paw edema method. Most of the compounds from the series showed significant (p < 0.05) anti-inflammatory activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"46 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80857778","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P163
G. Singh, T. Divakar
A novel, simple, precise, accurate stability indicating liquid chromato-graphy method was developed for the separation and simultaneous quantification of bictegravir, emtricitabine, tenofovir in bulk drug and pharmaceutical formulations. Separation was achieved on ProntoSILHypersorb ODS C18 column using mobile phase of 0.1 M sodium perchlorate, methanol in the ratio of 65:35 (v/v), pH 4.8 at a flow rate of 1.0 mL/min and UV detection was monitored at a wavelength of 258 nm. In these conditions, well resolved peaks were observed with acceptable system suitability at a retention time of 4.6 min for bictegravir, 7.0 min for emtricitabine and 10.1 min for tenofovir. Very high correlated linearity range was found to be 5-30 μg/mL for bictegravir, 20-120 μg/mL for emtricitabine and 2.5-15 μg/mL for tenofovir. The method can separate and identify the unknown degradation compounds formed during stress degradation study.
{"title":"A Novel Stability Indicating RP-HPLC Method Development and Validation for Simultaneous Estimation of Bictegravir, Emtricitabine and Tenofovir in Pure and Fixed Dose Combination","authors":"G. Singh, T. Divakar","doi":"10.14233/AJOMC.2019.AJOMC-P163","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P163","url":null,"abstract":"A novel, simple, precise, accurate stability indicating liquid chromato-graphy method was developed for the separation and simultaneous quantification of bictegravir, emtricitabine, tenofovir in bulk drug and pharmaceutical formulations. Separation was achieved on ProntoSILHypersorb ODS C18 column using mobile phase of 0.1 M sodium perchlorate, methanol in the ratio of 65:35 (v/v), pH 4.8 at a flow rate of 1.0 mL/min and UV detection was monitored at a wavelength of 258 nm. In these conditions, well resolved peaks were observed with acceptable system suitability at a retention time of 4.6 min for bictegravir, 7.0 min for emtricitabine and 10.1 min for tenofovir. Very high correlated linearity range was found to be 5-30 μg/mL for bictegravir, 20-120 μg/mL for emtricitabine and 2.5-15 μg/mL for tenofovir. The method can separate and identify the unknown degradation compounds formed during stress degradation study.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"10 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81141654","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P162
B. Sujatha, C. Subramanyam, K. P. Rao
Microwave assisted easy, efficient, and environment friendly process has been devised for the synthesis of phosphonates within minutes via microwave-assisted Michaelis-Arbuzov reaction. The desired products were obtained in excellent yields and in high purity under solvent-free and catalyst-free conditions. The structure of all the synthesized compounds was confirmed by spectral and CHN analysis. in vitro Antibacterial and antifungal activity of these compounds was also analyzed. Majority of the title compounds showed good inhibition towards bacteria and fungi.
{"title":"Microwave Mediated Michaelis-Arbuzov Reaction to Synthesize Bioactive Phenylphosphonate Derivatives Under Solvent Free Condition","authors":"B. Sujatha, C. Subramanyam, K. P. Rao","doi":"10.14233/AJOMC.2019.AJOMC-P162","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P162","url":null,"abstract":"Microwave assisted easy, efficient, and environment friendly process has been devised for the synthesis of phosphonates within minutes via microwave-assisted Michaelis-Arbuzov reaction. The desired products were obtained in excellent yields and in high purity under solvent-free and catalyst-free conditions. The structure of all the synthesized compounds was confirmed by spectral and CHN analysis. in vitro Antibacterial and antifungal activity of these compounds was also analyzed. Majority of the title compounds showed good inhibition towards bacteria and fungi.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"55 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86260593","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P178
P. Priyadarsini, V. Rao, C. Rao
The synthesis of some pyrimidine derivatives was achieved by conden-sation of 2-hydroxyacetophenone and cinnamic acid as starting materials through 1,3-diketones as intermediates. The resulting diketones have been converted into substituted pyrimidines by reaction with urea, thiourea and guanidine in the presence of trace of triethylamine and pyridine in calculated quantity. The synthesized compounds were characterized by their physical properties, NMR and LC-mass spectroscopic studies and also screened for their anti-inflammatory activity.
{"title":"Synthesis, Characterization and Anti-inflammatory Activity of New Pyrimidines","authors":"P. Priyadarsini, V. Rao, C. Rao","doi":"10.14233/AJOMC.2019.AJOMC-P178","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P178","url":null,"abstract":"The synthesis of some pyrimidine derivatives was achieved by conden-sation of 2-hydroxyacetophenone and cinnamic acid as starting materials through 1,3-diketones as intermediates. The resulting diketones have been converted into substituted pyrimidines by reaction with urea, thiourea and guanidine in the presence of trace of triethylamine and pyridine in calculated quantity. The synthesized compounds were characterized by their physical properties, NMR and LC-mass spectroscopic studies and also screened for their anti-inflammatory activity.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"65 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72647316","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P167
P. Subbareddy, T. Divakar
The purpose of the present research was to develop a suitable simple and reproducible RP-HPLC method for a quantification of dapagliflozin propanediol in spiked human plasma samples. The liquidliquid extraction plasma spiked samples of dapagliflozin propanediol were analyzed by using a ODS C18 Prontosil column under isocratic conditions. The extracted plasma spiked samples were carried using methanol, acetonitrile and pH 5.6 acetate buffer in the ratio of 50:20:10 (v/v) with a flow rate of 0.9 mL/min. The detector response was monitored at 228 nm using UV detector. The method was validated as per the ICH guidelines for bio analytical method validation and all the validation parameters were found to be within the acceptance limit The plasma spiked samples shows stability at room temperature over a period of 48 h. Thus, this method would be employed for routine quantification of dapagliflozin in human plasma samples.
{"title":"Bio-analytical Development and Validation of RP-HPLC Liquid Method for Quantification of Dapagliflozin Propanediol in Spiked Human Plasma","authors":"P. Subbareddy, T. Divakar","doi":"10.14233/AJOMC.2019.AJOMC-P167","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P167","url":null,"abstract":"The purpose of the present research was to develop a suitable simple and reproducible RP-HPLC method for a quantification of dapagliflozin propanediol in spiked human plasma samples. The liquidliquid extraction plasma spiked samples of dapagliflozin propanediol were analyzed by using a ODS C18 Prontosil column under isocratic conditions. The extracted plasma spiked samples were carried using methanol, acetonitrile and pH 5.6 acetate buffer in the ratio of 50:20:10 (v/v) with a flow rate of 0.9 mL/min. The detector response was monitored at 228 nm using UV detector. The method was validated as per the ICH guidelines for bio analytical method validation and all the validation parameters\u0000were found to be within the acceptance limit The plasma spiked samples shows stability at room temperature over a period of 48 h. Thus, this method would be employed for routine quantification of dapagliflozin in human plasma samples.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"23 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86945992","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-03-30DOI: 10.14233/AJOMC.2019.AJOMC-P165
M. Rama, B. S. Sundar
The present study deals with the extraction of total essential oils from medicinal plant Ocimum sanctum (Purple) in four different seasons of 2010 calendar year. Extraction of total essential oil content of plant materials was carried out by Soxhlet extraction whereas extraction of volatile oils by steam distillation using Clevenger type apparatus. Total essential oil and volatile oils are more in winter season (November month) whereas very less quantity in summer season (May month). Eugenol is the major constituent present in the plant. The percentage composition of eugenol in four seasons was found from gas chromatography analysis.
{"title":"Seasonal Variation of Essential Oils Composition of A Medicinal Plant - Ocimum sanctum (Purple)","authors":"M. Rama, B. S. Sundar","doi":"10.14233/AJOMC.2019.AJOMC-P165","DOIUrl":"https://doi.org/10.14233/AJOMC.2019.AJOMC-P165","url":null,"abstract":"The present study deals with the extraction of total essential oils from medicinal plant Ocimum sanctum (Purple) in four different seasons of 2010 calendar year. Extraction of total essential oil content of plant materials was carried out by Soxhlet extraction whereas extraction of volatile oils by steam distillation using Clevenger type apparatus. Total essential oil and volatile oils are more in winter season (November month) whereas very less quantity in summer season (May month). Eugenol is the major constituent present in the plant. The percentage composition of eugenol in four seasons was found from gas chromatography analysis.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"1 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-03-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"75468879","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
Pub Date : 2019-01-01DOI: 10.14233/ajomc.2019.ajomc-p239
M. Patra
In present study, the molecular modeling techniques were applied to generate a refined model of a cysteine protease of Leishmania donovani using the crystal structure of a homologous protease and used for lead optimization. The structures of a series of complexes of the protease with the designed inhibitors were predicted using a novel docking technique comprising of repeated cycles of molecular dynamics and energy minimization. Calculation of the free energies of binding of the model with the designed inhibitors suggested that three compounds can form stable complexes with dissociation constants in the nanomolar range (0.038-1.41 nM). Search in the human genome revealed that a number of proteases of the cathepsin family had high homology with the parasite protease with amino acid identity around 45 %. The X-ray structures of all these were available in the protein data bank. The structures of the complexes of the selected inhibitors with a few homologous human proteases of known 3-D structures were also predicted using the same technique of optimization. The electrostatic potentials around the binding sites of the proteases were highly negative, which served as a clue for the introduction of positively charged groups in the designed inhibitors for higher affinity. The comparison of interaction energies and hydrogen bonding patterns among these complexes and similar complexes with homologous human proteases allowed us to short-listed three molecules as effective antileishmanial cysteine protease inhibitors.
{"title":"Rational Lead Optimization Based on the Modeled Structure of\u0000Cysteine Protease of Leishmania donovani","authors":"M. Patra","doi":"10.14233/ajomc.2019.ajomc-p239","DOIUrl":"https://doi.org/10.14233/ajomc.2019.ajomc-p239","url":null,"abstract":"In present study, the molecular modeling techniques were applied to generate a refined model of a cysteine protease of Leishmania donovani using the crystal structure of a homologous protease and used for lead optimization. The structures of a series of complexes of the protease with the designed inhibitors were predicted using a novel docking technique comprising of repeated cycles of molecular dynamics and energy minimization. Calculation of the free energies of binding of the model with the designed inhibitors suggested that three compounds can form stable complexes with dissociation constants in the nanomolar range (0.038-1.41 nM). Search in the human genome revealed that a number of proteases of the cathepsin family had high homology with the parasite protease with amino acid identity around 45 %. The X-ray structures of all these were available in the protein data bank. The structures of the complexes of the selected inhibitors with a few homologous human proteases of known 3-D structures were also predicted using the same technique of optimization. The electrostatic potentials around the binding sites of the proteases were highly negative, which served as a clue for the introduction of positively charged groups in the designed inhibitors for higher affinity. The comparison of interaction energies and hydrogen bonding patterns among these complexes and similar complexes with homologous human proteases allowed us to short-listed three molecules as effective antileishmanial cysteine protease inhibitors.","PeriodicalId":8846,"journal":{"name":"Asian Journal of Organic & Medicinal Chemistry","volume":"86 1","pages":""},"PeriodicalIF":0.0,"publicationDate":"2019-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"81145787","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":0,"RegionCategory":"","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}