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Molecules 2016, 21(9), 1156; doi:10.3390/molecules21091156

Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent

1
Department of Chemistry, College of Science, Al-Imam Mohammad Ibn Saud Islamic University (IMSIU), P.O. Box: 90950 Riyadh 11623, Saudi Arabia
2
Photochemistry Department, Heterocyclic & Nucleosides Unit, National Research Centre, Dokki, Giza 12622, Egypt
*
Author to whom correspondence should be addressed.
Academic Editor: Derek J. McPhee
Received: 1 August 2016 / Revised: 21 August 2016 / Accepted: 25 August 2016 / Published: 31 August 2016
View Full-Text   |   Download PDF [1155 KB, uploaded 31 August 2016]   |  

Abstract

A series of novel pyrazole-5-carboxylate containing N-triazole derivatives 3,4; different heterocyclic amines 7ab and 10ab; pyrazolo[4,3-d]pyrimidine containing sulfa drugs 14a,b; and oxypyrazolo[4,3-d]pyrimidine derivatives 17, 19, 21 has been synthesized. The structure of the newly synthesized compounds was elucidated on the basis of analytical and spectral analyses. All compounds have been screened for their in vitro antimicrobial activity against three gram-positive and gram-negative bacteria as well as three fungi. The results revealed that compounds 14b and 17 had more potent antibacterial activity against all bacterial strains than reference drug Cefotaxime. Moreover compounds 4, 7b, and 12b showed excellent antifungal activities against Aspergillus niger and Candida albicans in low inhibitory concentrations but slightly less than the reference drug miconazole against Aspergillus flavus. View Full-Text
Keywords: pyrazole derivatives; pyrazolo[4,3-d]pyrimidine; N-substituted benzenesulfonamides; antimicrobial agent pyrazole derivatives; pyrazolo[4,3-d]pyrimidine; N-substituted benzenesulfonamides; antimicrobial agent
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Hafez, H.N.; El-Gazzar, A.-R.B. Synthesis and Biological Evaluation of N- Pyrazolyl Derivatives and Pyrazolopyrimidine Bearing a Biologically Active Sulfonamide Moiety as Potential Antimicrobial Agent. Molecules 2016, 21, 1156.

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