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Indian Journal of Heterocyclic Chemistry最新文献

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Synthesis and In-vivo Bioactivity Studies of Some New Hydrazide Schiff Bases and Mannich Bases of Indole Derivatives 吲哚衍生物中一些新的酰肼席夫碱和曼尼希碱的合成及其体内生物活性研究
4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-09-30 DOI: 10.59467/ijhc.2023.33.289
S. Subramanyam, Ramu Samineni, Sunil Kumar Kadiri, J. P. Yanadaiah, Phaneendranath Jonnalagedda, Krishna Veni Chikkula, Sampath A. Gouru
{"title":"Synthesis and In-vivo Bioactivity Studies of Some New Hydrazide Schiff Bases and Mannich Bases of Indole Derivatives","authors":"S. Subramanyam, Ramu Samineni, Sunil Kumar Kadiri, J. P. Yanadaiah, Phaneendranath Jonnalagedda, Krishna Veni Chikkula, Sampath A. Gouru","doi":"10.59467/ijhc.2023.33.289","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.289","url":null,"abstract":"The anti-inflammatory, analgesic, and antiulcer activities of eight new hydrazide Schiff bases and eight new Mannich bases of indole derivatives were investigated. 2-Methyl-1H-indole-3-carboxylate (III) on hydrazinolysis gave 2-methyl-1H-indole-3-carbohydrazide (IV), which on reaction with aldehydes gave corresponding hydrazide Schiff bases Va–Vh. The reaction of IV with formaldehyde, different aliphatic, aromatic, and heterocyclic amines afforded the Mannich bases of indole derivatives (VIa–VIe). The results of biological studies revealed that Schiff bases with 2,4-dichlorobenzaldehyde (Vh) and 2-chlorobenzaldehyde (Vb) were potent anti-inflammatory, analgesic, and antiulcer activities. Mannich bases (VIh and VIc) having -NO2 and -Cl groups in the paralocation of the heterocyclic nucleus displayed effective anti-inflammatory, analgesic, and antiulcer activities.","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135038088","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Microwave-Assisted Synthesis of 2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones and their Antibacterial, Antitubercular, and In Silico Screening 微波辅助合成2-(芳基烯)-1-噻亚-4-氮杂灵[4.5]decan-3- 1及其抗菌、抗结核和硅筛选
4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-09-30 DOI: 10.59467/ijhc.2023.33.285
Parth P. Patel, Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, Dhanji P. Rajani
{"title":"Microwave-Assisted Synthesis of 2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones and their Antibacterial, Antitubercular, and In Silico Screening","authors":"Parth P. Patel, Navin B. Patel, Manesh S. Tople, Vatsal M. Patel, Dhanji P. Rajani","doi":"10.59467/ijhc.2023.33.285","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.285","url":null,"abstract":"2-(Arylidene)-1-thia-4-azaspiro[4.5]decan-3-ones (3a-e, 4a-e) were synthesized from the 1-thia-4-azaspiro[4.5] decan-3-one through Knoevenagel reaction using the microwave method. In vitro, antibacterial and antitubercular screening of synthetic derivatives 3a-e and 4a-e revealed that compounds 3a and 4b are considerably potent as antibacterial agents against Escherichia coli with MIC = 50 μg/mL and MIC = 50 μg/mL, respectively. Compounds 3e and 4e possessed very good antitubercular activity with MIC = 0.47 μg/mL and MIC = 0.43 μg/mL. The results of molecular docking analysis supported the results of in vitro evaluation as against antibacterial protein compound 3a showed the lowest binding energy and against antitubercular protein, while 3e and 4e were highly attached?","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135038090","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis of Some New 7-(arylidene/heteroylidene imino)-2-(3,4-dimethoxy-phenyl)-5-oxo- 1,5-dihydro-[1,2,4]triazolo[1,5-α]pyridine-6-carbonitrile Derivatives as Potent Antibacterial and Anti-inflammatory Agents 新型7-(芳基/杂酰基亚胺)-2-(3,4-二甲氧基苯基)-5-氧- 1,5-二氢-[1,2,4]三唑[1,5-α]吡啶-6-碳腈衍生物的合成
4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-09-30 DOI: 10.59467/ijhc.2023.33.277
Praneetha Visampalli, Girija Sastry Vedula
{"title":"Synthesis of Some New 7-(arylidene/heteroylidene imino)-2-(3,4-dimethoxy-phenyl)-5-oxo- 1,5-dihydro-[1,2,4]triazolo[1,5-α]pyridine-6-carbonitrile Derivatives as Potent Antibacterial and Anti-inflammatory Agents","authors":"Praneetha Visampalli, Girija Sastry Vedula","doi":"10.59467/ijhc.2023.33.277","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.277","url":null,"abstract":"A new series of 7-(arylidene/heteroylidene imino)-2-(3,4-dimethoxy-phenyl)-5-oxo-1,5-dihydro-[1,2,4] triazolo[1,5-α]pyridine-6-carbonitrile derivatives i.e., Schiff bases (4a-4j) was synthesized from reaction of 7-amino-2-(3,4-dimethoxy-phenyl)-5-oxo-1,5-dihydro-[1,2,4]triazolo[1,5-α]pyridine-6-carbonitrile (3) with substituted benzaldehydes or hetraldehydes in presence of glacial acetic acid. The antibacterial and anti-inflammatory properties of compounds 3, 4a-4j were investigated, and the results showed that some of the synthesized compounds had better activity than the standard reference drugs. The minimum inhibitory concentration of compounds 4b, 4c, 4f, 4g, and 4i was found to be 10 μg/mL, which was lower than that of ciprofloxacin. The compounds were also tested for anti-inflammatory properties in vitro, and compounds 4a and 4f were found to have superior anti-inflammatory action at 100 μg/mL compared to the standard reference drug ibuprofen.","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135038109","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
8-Aryloct-7-en-2,4,6-triones as Useful Precursors for the Regioselective Synthesis of Some New 2-Methyl-5-styryl-7-thioxo-6,7-dihydropyrazolo[1,5-c]pyrimidines 8-芳基-7-en-2,4,6-三酮作为区域选择性合成一些新的2-甲基-5-苯基-7-硫氧基-6,7-二氢吡唑[1,5-c]嘧啶的有用前体
4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-09-30 DOI: 10.59467/ijhc.2023.33.355
Nisha Sharma, Rashmi Pundeer, Om Prakash
{"title":"8-Aryloct-7-en-2,4,6-triones as Useful Precursors for the Regioselective Synthesis of Some New 2-Methyl-5-styryl-7-thioxo-6,7-dihydropyrazolo[1,5-c]pyrimidines","authors":"Nisha Sharma, Rashmi Pundeer, Om Prakash","doi":"10.59467/ijhc.2023.33.355","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.355","url":null,"abstract":"Dehydroacetic acid, commonly abbreviated as DHA, and its derivatives have been extensively used as important intermediates in organic synthesis particularly for the synthesis of heterocyclic compounds. The reaction of 8-aryloct-7-en-2,4,6-triones (DHA-triones, readily prepared from commercially available DHA by the use of a multistep procedure) with thiosemicarbazide led the formation of some new 2-methyl-5-styryl-7-thioxo-6,7-dihydropyrazolo[1,5-c] pyrimidines.","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135038111","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
New Thiosemicarbazide Analogs as Antagonist of Nicotinic Muscarinic Receptors: Synthesis, In silico, and In vivo Screening 新的硫代氨基脲类似物作为烟碱毒蕈碱受体拮抗剂:合成、硅和体内筛选
4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-09-30 DOI: 10.59467/ijhc.2023.33.321
Varsha Jindaniya, Rakhi Mishra, Rupa Mazumder, Avijit Mazumder, Bhupinder Kapoor, Fahad Khan
{"title":"New Thiosemicarbazide Analogs as Antagonist of Nicotinic Muscarinic Receptors: Synthesis, In silico, and In vivo Screening","authors":"Varsha Jindaniya, Rakhi Mishra, Rupa Mazumder, Avijit Mazumder, Bhupinder Kapoor, Fahad Khan","doi":"10.59467/ijhc.2023.33.321","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.321","url":null,"abstract":"Some new thiosemicarbazide derivatives (5*a-5*b and 6a-6f) were synthesized by multiple steps approaches starting from substituted anilines. The synthesized compounds were evaluated for their muscle relaxant activity by an in silico docking study against nicotinic muscarinic receptor (protein database [PDB] ID: 2XNU) using AutoDock Vina and Biovia discovery studio tools. The rotarod test was also used to evaluate the muscle-relaxing activity of the compounds. The results were compared with generic diazepam to corroborate both research findings. In the in silico test, all the compounds showed 2–4 interactions with the target nicotinic muscarinic receptor (PDB ID- 2XNU) having binding affinities in the range of −5.8–−7.8 Kcal/mol. Among them, the 6a compound demonstrated the most remarkable relaxant activity with four hydrogen bond interactions with amino acids TYRC: 52, ILE C: 88, ALA C:90, and GLN C:119 of the target molecule. In addition, the rotarod test showed that compounds 5*a and 6d also had more muscle-relaxing effects than diazepam.","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.0,"publicationDate":"2023-09-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"135038274","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and In Vitro Antimycobacterial Activity of Some New N-(5-Substituted Phenylthiazol-2-yl) Pyrimidine-5-Carboxamides 新型N-(5-取代苯噻唑-2-酰基)嘧啶-5-羧胺类化合物的合成及体外抑菌活性研究
IF 0.3 4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-06-01 DOI: 10.59467/ijhc.2023.33.221
M. Almehmadi, Ahad Amer Alsaiari, M. Allahyani, A. Aljuaid, S. Saha, M. Asif
{"title":"Synthesis and In Vitro Antimycobacterial Activity of Some New N-(5-Substituted Phenylthiazol-2-yl) Pyrimidine-5-Carboxamides","authors":"M. Almehmadi, Ahad Amer Alsaiari, M. Allahyani, A. Aljuaid, S. Saha, M. Asif","doi":"10.59467/ijhc.2023.33.221","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.221","url":null,"abstract":"","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2023-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42871184","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, Antioxidant, and Antibacterial Potential of New Curcumin-Coumarin Hybrids 姜黄素-香豆素新杂种的合成、抗氧化及抗菌活性研究
IF 0.3 4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-06-01 DOI: 10.59467/ijhc.2023.33.183
Nidhi Negi, G. Chand, R. Gahtori, Santosh K. Upadhyay, Penny Joshi
{"title":"Synthesis, Antioxidant, and Antibacterial Potential of New Curcumin-Coumarin Hybrids","authors":"Nidhi Negi, G. Chand, R. Gahtori, Santosh K. Upadhyay, Penny Joshi","doi":"10.59467/ijhc.2023.33.183","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.183","url":null,"abstract":"","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2023-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47803563","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis, Characterization, Molecular Docking, and Biological Evaluation of 2-Methyl Perlolidine 2-甲基Perlolidine的合成、表征、分子对接及生物学评价
IF 0.3 4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-06-01 DOI: 10.59467/ijhc.2023.33.191
K. Prabakaran, A. Nepolraj, Javid A. Malik, Vasyl I. Shupeniuk
{"title":"Synthesis, Characterization, Molecular Docking, and Biological Evaluation of 2-Methyl Perlolidine","authors":"K. Prabakaran, A. Nepolraj, Javid A. Malik, Vasyl I. Shupeniuk","doi":"10.59467/ijhc.2023.33.191","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.191","url":null,"abstract":"","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2023-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"41553255","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Design, Synthesis, and Anticancer Evaluation of New Coumarin and Pyrazole Derivatives Bearing Benzenesulfonamide Moiety 含苯磺酰胺基团香豆素和吡唑衍生物的设计、合成及抗癌评价
IF 0.3 4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-06-01 DOI: 10.59467/ijhc.2023.33.199
Sameh R. Elgogary, Emad M. El Telbani
{"title":"Design, Synthesis, and Anticancer Evaluation of New Coumarin and Pyrazole Derivatives Bearing Benzenesulfonamide Moiety","authors":"Sameh R. Elgogary, Emad M. El Telbani","doi":"10.59467/ijhc.2023.33.199","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.199","url":null,"abstract":"","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2023-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"42162962","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
Synthesis and Antimicrobial Evaluation of 6-Aryl-3-(pyridin-4-yl)-[1,2,4]triazolo[3,4-b] [1,3,4]thiadiazoles 6-芳基-3-（吡啶-4-基）-[1,2,4]三唑并[3,4-b][1,3,4]噻二唑的合成及抗菌性能评价
IF 0.3 4区 化学
Indian Journal of Heterocyclic Chemistry Pub Date : 2023-06-01 DOI: 10.59467/ijhc.2023.33.173
M. Almehmadi, Ahad Amer Alsaiari, M. Allahyani, A. Aljuaid, Abdulaziz Alsharif, M. Asif
{"title":"Synthesis and Antimicrobial Evaluation of 6-Aryl-3-(pyridin-4-yl)-[1,2,4]triazolo[3,4-b] [1,3,4]thiadiazoles","authors":"M. Almehmadi, Ahad Amer Alsaiari, M. Allahyani, A. Aljuaid, Abdulaziz Alsharif, M. Asif","doi":"10.59467/ijhc.2023.33.173","DOIUrl":"https://doi.org/10.59467/ijhc.2023.33.173","url":null,"abstract":"","PeriodicalId":54993,"journal":{"name":"Indian Journal of Heterocyclic Chemistry","volume":null,"pages":null},"PeriodicalIF":0.3,"publicationDate":"2023-06-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"47444825","PeriodicalName":null,"FirstCategoryId":null,"ListUrlMain":null,"RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":"","EPubDate":null,"PubModel":null,"JCR":null,"JCRName":null,"Score":null,"Total":0}
引用次数: 0
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