Synthesis and In Vitro Activity of Polyhalogenated 2‐phenylbenzimidazoles as a New Class of anti‐MRSA and Anti‐VRE Agents. (31st August 2015)

• Record Type: Journal Article
• Authors: Göker, Hakan; Karaaslan, Cigdem; Püsküllü, Mustafa Orhan; Yildiz, Sulhiye; Duydu, Yalcin; Üstündağ, Aylin; Yalcin, Can Özgür
• Is Part Of: Chemical biology & drug design. Volume 87:Number 1(2016)
• Page Start: 57
• Page End: 68
• Publication Date: 2015-08-31
• Subjects: 2‐phenylbenzimidazoles -- antistaphylococcal activity -- methicillin‐resistant Staphylococcus aureus -- polyhalogenated benzimidazoles -- vancomycin‐resistant Enterococcus faecium; Drugs -- Design -- Periodicals; Pharmaceutical chemistry -- Periodicals; Biochemistry -- Periodicals; 615.19005
• DOI: 10.1111/cbdd.12623
• Languages: English
• ISSNs: 1747-0277

Abstract

Abstract : A series of novel polyhalogenated 2‐phenylbenzimidazoles have been synthesized and evaluated for in vitro antistaphylococcal activity against drug‐resistant bacterial strains (methicillin‐resistant Staphylococcus aureus, and vancomycin‐resistant Enterococcus faecium . Certain compounds inhibit bacterial growth perfectly. 11 was active than vancomycin (0.78 μ g/mL) with the lowest MIC values with 0.19 μ g/mL against methicillin‐resistant Staphylococcus aureus, 8 and 35 exhibited best inhibitory activity against vancomycin‐resistant Enterococcus faecium (1.56 μ g/mL). The mechanism of action for this class of compounds appears to be different than clinically used antibiotics. These polyhalogenated benzimidazoles have potential for further investigation as a new class of potent anti‐methicillin‐resistant Staphylococcus aureus and anti‐vancomycin‐resistant Enterococcus faecium agents. Abstract : A series of novel polyhalogenated 2‐phenylbenzimidazoles have been synthesized and evaluated for their in vitro antibacterial activity against MRSA (Compound 11, MIC values 0.19 μ g/mL) and VRE (Compound 8, MIC values 1.56 μ g/mL)