Synthesis and Biological Evaluation of some Amide Derivatives Bearing Benzothiazole and Piperidine Moieties as Antimicrobial Agents

ALTINTOP M. D., ÖZDEMİR A., KAPLANCIKLI Z. A., Turan-Zitouni G., İŞCAN G., AKALIN ÇİFTÇİ G.

LETTERS IN DRUG DESIGN & DISCOVERY, vol.10, no.5, pp.453-461, 2013 (SCI-Expanded) identifier identifier

  • Publication Type: Article / Article
  • Volume: 10 Issue: 5
  • Publication Date: 2013
  • Doi Number: 10.2174/1570180811310050013
  • Journal Name: LETTERS IN DRUG DESIGN & DISCOVERY
  • Journal Indexes: Science Citation Index Expanded (SCI-EXPANDED), Scopus
  • Page Numbers: pp.453-461
  • Keywords: Amide, Benzothiazole, Piperidine, Antimicrobial activity, Cytotoxicity, ANTI-BACTERIAL, ANTIFUNGAL, CYTOTOXICITY, ANALOGS
  • Anadolu University Affiliated: Yes

Abstract

In this study, N-(benzothiazol-2-yl)-2-(piperidin-1-yl)acetamide derivatives (1-24) were obtained by the reaction of 2-chloro-N-(benzothiazole-2-yl)acetamides with piperidine derivatives. The structures of the compounds were elucidated by H-1-NMR and mass spectral data and elemental analysis. The compounds were screened for their antimicrobial activities against pathogenic bacteria and Candida species. The compounds were also investigated for their cytotoxic properties using MTT assay. The microbiological results revealed that the compounds were more effective against fungi than bacteria. Among Candida species, C. utilis was the most susceptible fungus to compounds 7 and 11. It is apparent that 2,6-dimethylpiperidine group and chloro and methyl substituents on benzothiazole ring have an important impact on anticandidal activity. MTT assay indicated that the effective doses of these derivatives were lower than their cytotoxic doses.