Antimicrobial activity and a SAR study of some novel benzimidazole derivatives bearing hydrazone moiety.
In this study 12 novel benzimidazole compounds bearing hydrazone moiety were synthesized in order to investigate their possible antibacterial and antifungal activity. Structures of the synthesized compounds were elucidated by spectral data. Six different gram-negative and four different gram-positive bacterial strains were used in antibacterial activity tests. Antifungal activity tests were also performed against three different fungal strains. Most of the test compounds found to be significantly effective against Proteus vulgaris, Staphylococcus typhimurium, Klebsiella pneumoniae and Pseudomonas aeruginosa gram-negative bacterial strains. A structure-activity relationship (SAR) study including some electronic parameters was carried out and a connection between antibacterial activity and electronic properties of the target compounds was determined. Toxicity of the most effective compounds was established by performing Brine-Shrimp lethality assay.
Ozkay
Yusuf
Y
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Anadolu University, 26470 Eskişehir, Turkey. yozkay@anadolu.edu.tr
Tunali
Yağmur
Y
Karaca
Hülya
H
Işikdağ
Ilhan
I
D000818:Animals; D000890:Anti-Infective Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D001156:Artemia / Q000187:drug effects; D001419:Bacteria / Q000187:drug effects*; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000633:toxicity; D005658:Fungi / Q000187:drug effects*; D006835:Hydrazones / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
D000890:Anti-Infective Agents; D001562:Benzimidazoles; D006835:Hydrazones; C031000:benzimidazole