Pub Date : 2021-01-20DOI: 10.56042/ijcb.v60i01.32397
{"title":"Synthesis and evaluation of 2,3,4,9-tetrahydro-1H-carbazole derivatives as selective acetylcholinesterase inhibitors: Potential anti-Alzheimer’s agents","authors":"","doi":"10.56042/ijcb.v60i01.32397","DOIUrl":"https://doi.org/10.56042/ijcb.v60i01.32397","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2021-01-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84125987","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}
Pub Date : 2020-12-16DOI: 10.56042/ijcb.v59i12.30086
P. Kawle, K. Kamble
One-pot four component synthesis of 2,5,6-triaryl pyrazines, 1,2,4,5-tetraaryl imidazoles and 2,2,4,5-tetraaryl imidazoles have been achieved from benzoin, aryl amine, ammonium acetate and aryl ketone /aryl aldehydes using lemon juice ( Citrus limon ) as an ecofriendly catalyst in good yield under mild conditions. The antibacterial action exhibited by the synthesized compounds against clinical isolates obtained from urinary tract catheters of infected patients is close to the standard drug tetracycline. Recovery of lemon juice after completion of reaction eliminates the need to handle side products, making this process more safe and user friendly.
{"title":"Synthesis of pyrazines and imidazoles using lemon juice (Citrus limon) as a recyclable catalyst","authors":"P. Kawle, K. Kamble","doi":"10.56042/ijcb.v59i12.30086","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.30086","url":null,"abstract":"One-pot four component synthesis of 2,5,6-triaryl pyrazines, 1,2,4,5-tetraaryl imidazoles and 2,2,4,5-tetraaryl imidazoles have been achieved from benzoin, aryl amine, ammonium acetate and aryl ketone /aryl aldehydes using lemon juice ( Citrus limon ) as an ecofriendly catalyst in good yield under mild conditions. The antibacterial action exhibited by the synthesized compounds against clinical isolates obtained from urinary tract catheters of infected patients is close to the standard drug tetracycline. Recovery of lemon juice after completion of reaction eliminates the need to handle side products, making this process more safe and user friendly.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"85537705","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}
Pub Date : 2020-12-16DOI: 10.56042/ijcb.v59i12.40244
S. Kotha, Sunil Pulletikurti
Earlier, a simple synthetic approach to cis , syn , cis- triquinanes and propellanes from exo -nadic anhydride through metathesis approach had been demonstrated. In the present work is discussed a distinct course of observations when this methodology has been extended to oxygenated exo -nadic anhydride derivatives and the importance of stereochemistry and the role of hetero atom in the outcome of olefin metathesis has been demonstrated.
{"title":"Synthetic approach to oxa-triquinanes via olefin metathesis as a key step","authors":"S. Kotha, Sunil Pulletikurti","doi":"10.56042/ijcb.v59i12.40244","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.40244","url":null,"abstract":"Earlier, a simple synthetic approach to cis , syn , cis- triquinanes and propellanes from exo -nadic anhydride through metathesis approach had been demonstrated. In the present work is discussed a distinct course of observations when this methodology has been extended to oxygenated exo -nadic anhydride derivatives and the importance of stereochemistry and the role of hetero atom in the outcome of olefin metathesis has been demonstrated.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"84882892","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}
Pub Date : 2020-12-16DOI: 10.56042/ijcb.v59i12.30250
Rahele Bargebid, S. Khabnadideh
Owing to the wide applications and significance of phloroglucide analogues in organic synthesis, pharmacology and industry, there is considerable interest in the synthesis of these compounds. Nevertheless, there are few methods for preparation of these compounds. Here we reported a simple, clean, and highly efficient procedure for the green synthesis of tricyclic polyhydroxyl aromatic compounds. Microwave-assisted alkylation reaction between 4-substituted-2, 6-bis(chloromethyl)phenols and various phenol derivatives, in the presence of zinc oxide (ZnO) in 1-butyl-3methylimidazolium hexaflourophosphate ([Bmim]PF6), affords the title compounds in short duration with high yields. We have synthesized 18 derivatives of the title compounds 3a-3r by this procedure. Chemical structures of all synthesized compounds have been confirmed by spectrophotometric methods such as IR, NMR and mass spectroscopy. Some of the synthesized compounds have been screened for their antimicrobial activities. Antifungal and antibacterial activities have been evaluated against different species of microorganisms including gram positive and gram negative bacteria as well as fungi. Broth microdilution method as recommended by Clinical and Laboratory Standard Institute has been used for this purpose. The results show compounds 3i, 3k and 3m have the best antibacterial and antifungal activity against most of the examined species. Compounds 3b, 3f, 3o, 3p and 3q also show good activity against some species.
{"title":"ZnO in ionic liquid under microwave irradiation: A novel medium for synthesis of phloroglucide derivatives as antimicrobial agents","authors":"Rahele Bargebid, S. Khabnadideh","doi":"10.56042/ijcb.v59i12.30250","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.30250","url":null,"abstract":"Owing to the wide applications and significance of phloroglucide analogues in organic synthesis, pharmacology and industry, there is considerable interest in the synthesis of these compounds. Nevertheless, there are few methods for preparation of these compounds. Here we reported a simple, clean, and highly efficient procedure for the green synthesis of tricyclic polyhydroxyl aromatic compounds. Microwave-assisted alkylation reaction between 4-substituted-2, 6-bis(chloromethyl)phenols and various phenol derivatives, in the presence of zinc oxide (ZnO) in 1-butyl-3methylimidazolium hexaflourophosphate ([Bmim]PF6), affords the title compounds in short duration with high yields. We have synthesized 18 derivatives of the title compounds 3a-3r by this procedure. Chemical structures of all synthesized compounds have been confirmed by spectrophotometric methods such as IR, NMR and mass spectroscopy. Some of the synthesized compounds have been screened for their antimicrobial activities. Antifungal and antibacterial activities have been evaluated against different species of microorganisms including gram positive and gram negative bacteria as well as fungi. Broth microdilution method as recommended by Clinical and Laboratory Standard Institute has been used for this purpose. The results show compounds 3i, 3k and 3m have the best antibacterial and antifungal activity against most of the examined species. Compounds 3b, 3f, 3o, 3p and 3q also show good activity against some species.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"79916384","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}
Pub Date : 2020-12-16DOI: 10.56042/ijcb.v59i12.41816
S. Kotha, Sunil Pulletikurti
Herein is reported a concise synthesis of spiro-annulated cyclobutane tetracyclic and pentacyclic derivatives by ketene addition, and ring-rearrangement metathesis (RRM) as key steps, starting with commercially available norbornadiene and dicyclopentadiene. The tetracyclic spiro-derivative contains a [5/5/4] core unit, which is the key building block to angular triquinanes synthesis. Whereas, the pentacyclic spiro-derivative contains a basic core skeleton of presilphiperfolanes, and other sesquiterpenoids.
{"title":"Synthesis of spiro-annulated cyclobutane derivatives through ketene [2+2] cycloaddition and ring-rearrangement metathesis","authors":"S. Kotha, Sunil Pulletikurti","doi":"10.56042/ijcb.v59i12.41816","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.41816","url":null,"abstract":"Herein is reported a concise synthesis of spiro-annulated cyclobutane tetracyclic and pentacyclic derivatives by ketene addition, and ring-rearrangement metathesis (RRM) as key steps, starting with commercially available norbornadiene and dicyclopentadiene. The tetracyclic spiro-derivative contains a [5/5/4] core unit, which is the key building block to angular triquinanes synthesis. Whereas, the pentacyclic spiro-derivative contains a basic core skeleton of presilphiperfolanes, and other sesquiterpenoids.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"72903399","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}
Pub Date : 2020-12-16DOI: 10.56042/ijcb.v59i12.37312
{"title":"QSAR of 1,3,5-triazine compounds towards inhibition of toxoplasmosis utilizing computed molecular descriptors","authors":"","doi":"10.56042/ijcb.v59i12.37312","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.37312","url":null,"abstract":"","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"86605435","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}
Pub Date : 2020-12-14DOI: 10.56042/ijcb.v59i12.29562
Rupali G. Kalshetti, Ram D. Mandle, Sanjay P. Kamble, A. Sudalai
P 2 O 5 has been found to be a highly efficient and environmental friendly catalyst for the liquid-phase acylation of activated aromatic substrates giving aromatic ketones (45-93%) in a regioselective manner. Both aromatic and aliphatic carboxylic acids can be employed as acylating source. The process is particularly demonstrated at 100 g scale in the case of anisole and acetic acid to produce 4-methoxyacetophenone.
{"title":"P2O5-mediated Friedel-Crafts acylation of activated arenes with carboxylic acid as acylating agent","authors":"Rupali G. Kalshetti, Ram D. Mandle, Sanjay P. Kamble, A. Sudalai","doi":"10.56042/ijcb.v59i12.29562","DOIUrl":"https://doi.org/10.56042/ijcb.v59i12.29562","url":null,"abstract":"P 2 O 5 has been found to be a highly efficient and environmental friendly catalyst for the liquid-phase acylation of activated aromatic substrates giving aromatic ketones (45-93%) in a regioselective manner. Both aromatic and aliphatic carboxylic acids can be employed as acylating source. The process is particularly demonstrated at 100 g scale in the case of anisole and acetic acid to produce 4-methoxyacetophenone.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-12-14","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"80881487","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}
Pub Date : 2020-11-19DOI: 10.56042/ijcb.v59i11.30111
P. P. Deohate, Roshani S. Mulani
The synthesis of (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted phenyl/ H -pyrazol-3-yl)- amines and (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted benzoyl/isonicotinoyl/cinnamoyl-pyrazol-3-yl)-amines by conventional heating and microwave irradiative cyclocondensation have been achieved by the cyclisation of N-(4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-3-oxo butyramide with substituted hydrazines and acid hydrazides. The required butyramide has been synthesized by the reaction of 2,4-diamino-6-methyl-[1,3,5]-triazine with benzaldehyde followed by the condensation with ethyl acetoacetate. Structural elucidation of synthesized compounds has been performed by IR, 1 H NMR and mass spectral studies besides chemical transformation and elemental analysis. The title compounds have been evaluated for their antitubercular and antimicrobial potential against some selected microorganisms to establish the structure activity relationship.
{"title":"Synthesis of triazine linked pyrazole heterocyclics by conventional heating and microwave irradiative cyclocondensation and evaluation of antitubercular and antimicrobial potential","authors":"P. P. Deohate, Roshani S. Mulani","doi":"10.56042/ijcb.v59i11.30111","DOIUrl":"https://doi.org/10.56042/ijcb.v59i11.30111","url":null,"abstract":"The synthesis of (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted phenyl/ H -pyrazol-3-yl)- amines and (4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-(5-methyl-2-substituted benzoyl/isonicotinoyl/cinnamoyl-pyrazol-3-yl)-amines by conventional heating and microwave irradiative cyclocondensation have been achieved by the cyclisation of N-(4-benzylideneamino-6-methyl-[1,3,5]-triazin-2-yl)-3-oxo butyramide with substituted hydrazines and acid hydrazides. The required butyramide has been synthesized by the reaction of 2,4-diamino-6-methyl-[1,3,5]-triazine with benzaldehyde followed by the condensation with ethyl acetoacetate. Structural elucidation of synthesized compounds has been performed by IR, 1 H NMR and mass spectral studies besides chemical transformation and elemental analysis. The title compounds have been evaluated for their antitubercular and antimicrobial potential against some selected microorganisms to establish the structure activity relationship.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78234888","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}
Pub Date : 2020-11-19DOI: 10.56042/ijcb.v59i11.30667
N. Patel, Nilesh B. Chauhan, Sabir S Pathan, V. M. Patel, B. Mistry
Navin B Patel, Nilesh B Chauhan, Sabir S Pathan, Vatsal M Patel* & Bhupendra M Mistry a Department of Chemistry, Veer Narmad South Gujarat University, Surat 395 007, India b Department of Chemistry, Jamanaben Narottambhai Motiram Patel Science College, Bharthana (Vesu), Surat 395 017, India c Department of Food Science and Biotechnology, College of Life and Biotechnology, Dongguk University, Biomedical Campus, 32 Dongguk-ro, Ilsandong-gu, Goyang-si, Gyeonggi-do, Republic of Korea
Navin B Patel, Nilesh B Chauhan, Sabir S Pathan, Vatsal M Patel* & Bhupendra M ministry a Veer Narmad South Gujarat大学化学系，印度，Surat 395 007 B Jamanaben Narottambhai Motiram Patel科学学院化学系，Bharthana (Vesu)，印度，Surat 395 017 c东国大学生命与生物技术学院食品科学与生物技术系，韩国，京畿道高阳市，一山东区，东国路32号，生物医学校区
{"title":"Pyridine clubbed coumarin analogues: Their synthesis and biological studies as antimicrobials and antioxidants","authors":"N. Patel, Nilesh B. Chauhan, Sabir S Pathan, V. M. Patel, B. Mistry","doi":"10.56042/ijcb.v59i11.30667","DOIUrl":"https://doi.org/10.56042/ijcb.v59i11.30667","url":null,"abstract":"Navin B Patel, Nilesh B Chauhan, Sabir S Pathan, Vatsal M Patel* & Bhupendra M Mistry a Department of Chemistry, Veer Narmad South Gujarat University, Surat 395 007, India b Department of Chemistry, Jamanaben Narottambhai Motiram Patel Science College, Bharthana (Vesu), Surat 395 017, India c Department of Food Science and Biotechnology, College of Life and Biotechnology, Dongguk University, Biomedical Campus, 32 Dongguk-ro, Ilsandong-gu, Goyang-si, Gyeonggi-do, Republic of Korea","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"88403551","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}
Pub Date : 2020-11-19DOI: 10.56042/ijcb.v59i11.28918
W. A. Bawazir, R. M. Abdel-Rahman
A few fluorinated 3-hydrazino-1,2,4-triazino[5,6-b] indoles ( 5 - 8 ) have been synthesized and screened for their herbicidal effect. Treatment of 3-hydrazino-8H/8-fluoro-1,2,4-triazino[5,6-b] indoles ( 3 and 4 ) with fluorinated acyl derivatives ( A and B ) yielded the rich fluorine 1,2,4-triazino indole. Structure of the products have been established by elemental analysis and spectral measurements. The presence and position of fluorine atoms have been deduced from 19 F NMR. The novel fluorinated hydrazino-1,2,4-triazino[5,6-b] indoles have been tested for post-emergent herbicidal activity against grass weed species and broadleaf weed species.
{"title":"Synthesis of fluorinated 3-hydrazino-1,2,4-triazino[5,6-b] indoles as novel herbicidal systems","authors":"W. A. Bawazir, R. M. Abdel-Rahman","doi":"10.56042/ijcb.v59i11.28918","DOIUrl":"https://doi.org/10.56042/ijcb.v59i11.28918","url":null,"abstract":"A few fluorinated 3-hydrazino-1,2,4-triazino[5,6-b] indoles ( 5 - 8 ) have been synthesized and screened for their herbicidal effect. Treatment of 3-hydrazino-8H/8-fluoro-1,2,4-triazino[5,6-b] indoles ( 3 and 4 ) with fluorinated acyl derivatives ( A and B ) yielded the rich fluorine 1,2,4-triazino indole. Structure of the products have been established by elemental analysis and spectral measurements. The presence and position of fluorine atoms have been deduced from 19 F NMR. The novel fluorinated hydrazino-1,2,4-triazino[5,6-b] indoles have been tested for post-emergent herbicidal activity against grass weed species and broadleaf weed species.","PeriodicalId":13458,"journal":{"name":"Indian Journal of Chemistry Section B-organic Chemistry Including Medicinal Chemistry","volume":null,"pages":null},"PeriodicalIF":0.5,"publicationDate":"2020-11-19","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":null,"resultStr":null,"platform":"Semanticscholar","paperid":"78470991","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}
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