DESIGN AND SYNTHESIS OF BENZODIAZEPINES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE AND INDOLE MOIETIES AS A POTENT ANTIMICROBIAL AND ANTIOXIDANT AGENTS


Basavaraj Shivabasappa Naraboli, Biradar Js

Abstract


 

 Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives, namely, 2-((1H-benzo[d] imidazol-2-yl) thio)-N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl) acetamide 3a-d, N-(4-(4-(1H-indol-3-yl)-8-methyl- 1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-((5-methoxy-1H-benzo[d]imidazol-2-yl) thio) acetamide 4a-d and N-(4-(4-(1H-indol-3-yl)-8-methyl-1H-benzo[b][1,4]diazepin-2-yl) phenyl)-2-(benzo[d]thiazol-2-ylthio) acetamide 5a-d.

Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities such as 1,1-diphenyl-2-picrylhydrazyl (DPPH), radical scavenging activity (RSA), ferric ions (Fe3+) reducing antioxidant power (FRAP), and ferrous (Fe2+) metal ion chelating activity.

Result: The structures of all the newly synthesized compounds were characterized by their infrared,1H nuclear magnetic resonance, mass spectral studies, and elemental analysis. Compounds 7a and 7b exhibited good RSA at a concentration 100 μg/ml, compounds 6d, 7a-d and 8a-c displayed good FRAP at a concentration 100 μg/ml, compounds 7b-d and 8b-d showed good Fe2+ ion metal chelating activity. Compounds 6b, 6d, 7a-d, and 8a-d exhibited good activity against all the screened bacteria and fungi.

Conclusion: Some of the compounds have shown potent antimicrobial activity against all the screened bacteria and fungi, and some have exhibited very good antioxidant activity.


Keywords


Benzodiazepine, Indole, Benzimidazole/Benzothiazole, Antimicrobial, Antioxidant.

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About this article

Title

DESIGN AND SYNTHESIS OF BENZODIAZEPINES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE AND INDOLE MOIETIES AS A POTENT ANTIMICROBIAL AND ANTIOXIDANT AGENTS

Keywords

Benzodiazepine, Indole, Benzimidazole/Benzothiazole, Antimicrobial, Antioxidant.

DOI

10.22159/ajpcr.2018.v11i1.21947

Date

01-01-2018

Additional Links

Manuscript Submission

Journal

Asian Journal of Pharmaceutical and Clinical Research
Vol 11 Issue 1 January 2018 Page: 70-77

Print ISSN

0974-2441

Online ISSN

2455-3891

Statistics

39 Views | 126 Downloads

Authors & Affiliations

Basavaraj Shivabasappa Naraboli
Department of Postgraduate Studies and Research in Chemistry, Gulbarga University, Kalaburagi, Karnataka, India.
India

Biradar Js
Department of Postgraduate Studies and Research in Chemistry, Gulbarga University, Kalaburagi, Karnataka, India.
India


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