title: Synthesis and antibacterial activity of tert-butyl [1-benzyl-2[(4-aryl-2-thiazolyl)hydrazono]ethyl]carbamate derivatives.
abstract: The increasing clinical importance of drug-resistant fungal and bacterial pathogens has lent additional urgency to microbiological research and new antibacterial compound development. For this purpose, new tert-butyl[1-benzyl-2[(4-aryl-2-thiazolyl)hydrazono]ethyl]carbamate derivatives were synthesized and evaluated for antibacterial activity. The reaction of Boc-L-phenylalaninal with thiosemicarbazide gave the thiosemicarbazone which furnished the title compounds by reaction with phenacyl bromides. The newly synthesized compounds were screened for antibacterial activity and toxicity. While microdilution broth susceptibility assay was used for the antibacterial activity evaluation of the compounds against the strains E. coli (NRRL B-3704), M. luteus (NRRL B-4375), B. cereus (NRRL B-3711), P. aeruginosa (NRRL B-23), and S. fecalis (NRRL B-14617), the Artemia salina 96-well assay was used to determine cytotoxicities of the compounds. Observations obtained from the bioassays showed that some of the compounds are highly active against E. coli, M. luteus, and B. cereus when compared with the control agent and showed low toxicity.
authors.affiliation: Anadolu University, Faculty of Pharmacy, Department of Pharmaceutical Chemistry, Eskisehir, Turkey. gturan@anadolu.edu.tr
authors.forename: Gülhan
authors.initials: G
authors.lastname: Turan-Zitouni
authors.forename: Jean-Alain
authors.initials: JA
authors.lastname: Fehrentz
authors.forename: Pierre
authors.initials: P
authors.lastname: Chevallet
authors.forename: Jean
authors.initials: J
authors.lastname: Martinez
authors.forename: Zafer Asim
authors.initials: ZA
authors.lastname: Kaplancikli
authors.forename: Ahmet
authors.initials: A
authors.lastname: Ozdemir
authors.forename: Muhittin
authors.initials: M
authors.lastname: Arslanyolu
authors.forename: Mehmet Taha
authors.initials: MT
authors.lastname: Yildiz
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D001156:Artemia / Q000187:drug effects; D001409:Bacillus cereus / Q000187:drug effects; D002219:Carbamates / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D013293:Enterococcus faecalis / Q000187:drug effects; D004926:Escherichia coli / Q000187:drug effects; D006835:Hydrazones / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*; D007928:Lethal Dose 50; D008826:Microbial Sensitivity Tests / Q000379:methods; D013844:Thiazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity*
chemical_list: D000900:Anti-Bacterial Agents; D002219:Carbamates; D006835:Hydrazones; D013844:Thiazoles