Synthesis and potent antibacterial activity against MRSA of some novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidines.
A series of 28 novel 1,2-disubstituted-1H-benzimidazole-N-alkylated-5-carboxamidine derivatives were synthesized and evaluated for in vitro antibacterial activities against Staphylococcus aureus and methicillin resistant S. aureus (MRSA) by the tube dilution method. The results showed that compounds 45-46 and 55-57, having 3,4-dichloro substituted phenyl at the position C-2, of N-bulky alkyl substituted benzimidazolecarboxamidines exhibited the greatest activity with MIC values of 1.56-0.39 microg/ml.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100 Tandogan, Ankara, Turkey. goker@pharmacy.ankara.edu.tr
Hakan
H
Göker
Seçkin
S
Ozden
Sulhiye
S
Yildiz
David W
DW
Boykin
D000478:Alkylation; D000578:Amidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001554:Benzene / Q000737:chemistry*; D007093:Imidazoles / Q000737:chemistry*; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D016106:Methicillin Resistance; D015394:Molecular Structure; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
D000578:Amidines; D000900:Anti-Bacterial Agents; D007093:Imidazoles; C029899:imidazole; D001554:Benzene