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Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones

2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously subst...

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Detalles Bibliográficos
Autores principales: Deshmukh, M. B., Patil, S., Patil, S. S., Jadhav, S. D.
Formato: Texto
Lenguaje:English
Publicado: Medknow Publications 2010
Materias:
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013576/
https://www.ncbi.nlm.nih.gov/pubmed/21218064
http://dx.doi.org/10.4103/0250-474X.73934
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author Deshmukh, M. B.
Patil, S.
Patil, S. S.
Jadhav, S. D.
author_facet Deshmukh, M. B.
Patil, S.
Patil, S. S.
Jadhav, S. D.
author_sort Deshmukh, M. B.
collection PubMed
description 2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously substituted aryl aldehydes gave the corresponding hydrazones (3). Further, the cyclization of compound (3) in acetic anhydride gave tricyclic pyrazoloquinazolinones (4). All newly synthesized compounds have been tested for their antibacterial activity against gram +ve bacteria B. substilis, S. aureus and gram –ve bacteria E. coli, P. vulgaris. The species used for antifungal activity are Aspergillus niger and Phytophora. Introduction of -OCH3, -OH and -Cl groups to the heterocyclic frame work enhanced antibacterial and antifungal activities.
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spelling pubmed-30135762011-01-07 Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones Deshmukh, M. B. Patil, S. Patil, S. S. Jadhav, S. D. Indian J Pharm Sci Short Communications 2-thio-3-aryl quinazolin-4(3H)one (1) was synthesized by reacting anthranilic acid with thiocarbamate salts of substituted aniline and carbon disulphide, which on reflux with excess of hydrazine hydrate to form 2-hydrazino quinazolin-4(3H)one derivatives (2). The reaction of (2) with variously substituted aryl aldehydes gave the corresponding hydrazones (3). Further, the cyclization of compound (3) in acetic anhydride gave tricyclic pyrazoloquinazolinones (4). All newly synthesized compounds have been tested for their antibacterial activity against gram +ve bacteria B. substilis, S. aureus and gram –ve bacteria E. coli, P. vulgaris. The species used for antifungal activity are Aspergillus niger and Phytophora. Introduction of -OCH3, -OH and -Cl groups to the heterocyclic frame work enhanced antibacterial and antifungal activities. Medknow Publications 2010 /pmc/articles/PMC3013576/ /pubmed/21218064 http://dx.doi.org/10.4103/0250-474X.73934 Text en © Indian Journal of Pharmaceutical Sciences http://creativecommons.org/licenses/by/2.0/ This is an open-access article distributed under the terms of the Creative Commons Attribution Licence, which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited.
spellingShingle Short Communications
Deshmukh, M. B.
Patil, S.
Patil, S. S.
Jadhav, S. D.
Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title_full Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title_fullStr Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title_full_unstemmed Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title_short Synthesis and Antimicrobial Screening of Pyrazolo-3-Aryl Quinazolin-4(3H)ones
title_sort synthesis and antimicrobial screening of pyrazolo-3-aryl quinazolin-4(3h)ones
topic Short Communications
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3013576/
https://www.ncbi.nlm.nih.gov/pubmed/21218064
http://dx.doi.org/10.4103/0250-474X.73934
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