2. Academic Validation
  3. Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents

Synthesis and Evaluation of Selected Benzimidazole Derivatives as Potential Antimicrobial Agents

  • Molecules. 2015 Aug 20;20(8):15206-23. doi: 10.3390/molecules200815206.
Fatmah A S Alasmary 1 2,  Anna M Snelling 3,  Mohammed E Zain 4,  Ahmed M Alafeefy 5,  Amani S Awaad 6,  Nazira Karodia 7 8
Affiliations

Affiliations

  • 1 Chemistry Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia. fasmari@ksu.edu.sa.
  • 2 Centre for Pharmaceutical Engineering Science, Faculty of Life Sciences, University of Bradford, Richmond Road, Bradford BD7 1DP, UK. fasmari@ksu.edu.sa.
  • 3 Centre for Pharmaceutical Engineering Science, Faculty of Life Sciences, University of Bradford, Richmond Road, Bradford BD7 1DP, UK. a.m.snelling@bradford.ac.uk.
  • 4 Botany and Microbiology Department, College of Science, King Saud University, Riyadh 11362, Saudi Arabia. mohamedzain@hotmail.com.
  • 5 Department of Pharmaceutical Chemistry, College of Pharmacy, Sattam bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia. alafeefy@hotmail.com.
  • 6 Pharmacognosy Department, College of Pharmacy, Salman bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia. amaniawaad@hotmail.com.
  • 7 Centre for Pharmaceutical Engineering Science, Faculty of Life Sciences, University of Bradford, Richmond Road, Bradford BD7 1DP, UK. nazira.karodia@wlv.ac.uk.
  • 8 Faculty of Science and Engineering, University of Wolverhampton, Wulfruna Street, Wolverhampton WV1 1LY, UK. nazira.karodia@wlv.ac.uk.
PMID: 26307956 DOI: 10.3390/molecules200815206
Abstract

A library of 53 benzimidazole derivatives, with substituents at positions 1, 2 and 5, were synthesized and screened against a series of reference strains of bacteria and fungi of medical relevance. The SAR analyses of the most promising results showed that the antimicrobial activity of the compounds depended on the substituents attached to the bicyclic heterocycle. In particular, some compounds displayed Antibacterial activity against two methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentrations (MICs) comparable to the widely-used drug ciprofloxacin. The compounds have some common features; three possess 5-halo substituents; two are derivatives of (S)-2-ethanaminebenzimidazole; and the Others are derivatives of one 2-(chloromethyl)-1H-benzo[d]imidazole and (1H-benzo[d]imidazol-2-yl)methanethiol. The results from the Antifungal screening were also very interesting: 23 compounds exhibited potent fungicidal activity against the selected Fungal strains. They displayed equivalent or greater potency in their MIC values than amphotericin B. The 5-halobenzimidazole derivatives could be considered promising broad-spectrum antimicrobial candidates that deserve further study for potential therapeutic applications.

Keywords

Gram-negative; Gram-positive; antibacterial activity; antifungal activity; benzimidazole; heterocycle; resistance.

Figures
Products
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z