SYNTHESIS, CHARACTERIZATION AND BIOLOGICAL EVALUATION OF INDOLE DERIVATIVES BEARING BENZIMIDAZOLE/BENZOTHIAZOLE MOIETY
| Autor: | Jayaprakash Sharanappa Biradar, Basavaraj S Naraboli |
|---|---|
| Rok vydání: | 2017 |
| Předmět: |
Pharmacology
Indole test Benzimidazole Metal chelating activity 010405 organic chemistry Stereochemistry Pharmaceutical Science Thio 010402 general chemistry 01 natural sciences Chelating Activity Medicinal chemistry 0104 chemical sciences Compound s chemistry.chemical_compound chemistry Benzothiazole Acetamide |
| Zdroj: | International Journal of Pharmacy and Pharmaceutical Sciences. 9:128 |
| ISSN: | 0975-1491 |
| DOI: | 10.22159/ijpps.2017v9i8.19725 |
| Popis: | Objective: The present work deals with the synthesis and characterization of biologically active new indole derivatives viz., 2-((1 H -benzo[d]imidazol-2-yl)thio)- N -(4-(3-(1 H -indol-3-yl)acryloyl)phenyl)acetamide 6a-d, N -(4-(3-(1 H -indol-3-yl)acryloyl)phenyl)-2-((5-methoxy-1 H -benzo[d]imidazol-2-yl)thio)acetamide 7a-d and N -(4-(3-(1 H -indol-3-yl)acryloyl)phenyl)-2-(benzo[d]thiazol-2-ylthio)acetamide 8a-d. Methods: All these newly synthesized compounds were screened for their in vitro antimicrobial activity by an agar plate diffusion method, antioxidant activities: like 1,1-diphenyl-2-picryl hydrazyl (DPPH) radical scavenging activity (RSA), ferric ions (Fe 3+ ) reducing antioxidant power (FRAP), ferrous (Fe 2+ ) metal ion chelating activity. Results: The structures of all the newly synthesized compounds were characterized by their IR, 1 HNMR, mass spectral studies and elemental analysis. Compounds 6b, 7a, 7b, 8a and 8b exhibited good radical scavenging activity (RSA) at a concentration 100 µg/ml, compounds 7b, 7c, 7d and 8b displayed good ferric ions (Fe 3+ ) reducing antioxidant power (FRAP) at a concentration 100 µg/ml, compounds 7b, 7d, 8b and 8d showed good ferrous (Fe 2+ ) ion metal chelating activity. Compounds 7d and 8d exhibited good activity against all the screened bacteria and fungi. Conclusion: The synthesised compounds 7d having methoxy group at 5 positions of benzimidazoles ring, bromo group at 5 positions of indole ring, and 8d having bromo group at position 5 of indole ring, both the compounds have exhibited potent antimicrobial activity. Some compound s have shown very good antioxidant activity. |
| Databáze: | OpenAIRE |
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