TY  - JOUR
TI  - Synthesis, characterization and biological evaluation of1,3-thiazolidine-4-ones derived from (2S)-2-benzoylamino 3-methylbutanohydrazide hydrazones
AB  - Novel 2-aryl-5-non-substituted / methyl-1,3-thiazolidine-4-one derivatives 14-33 carrying L-valine core were synthesized by the reaction of acylhydrazones 4-13 with thioglycolic acid / thiolactic acid. Structures of all synthesized compounds 14-33 were confirmed by IR, 1H-NMR and HR-MS analysis and 13C-NMR were recorded for selected compounds 17, 21, 28 and 30. None of the compounds 14-33 showed activity against HIV-1 (strain IIIB) or HIV2 (strain ROD) in an MT-4/MTT based assay. Compounds 14-33 were also screened against Feline Corona Virus (FIPV), Feline Herpes Virus, HSV-1(KOS), HSV-1 (TK-KOS ACVr), HSV-2 (G), Vaccinia virus, Vesicular stomatitis virus, Cytomegalovirus, Varicella-Zoster virus, Respiratory syncytial virus, Coxsackie B4 virus, Parainfluenza-3 virus, Reovirus-1, Sindbis virus and Punta Toro virus, but none of them showed antiviral activity at subtoxic concentrations. Anti-HCV NS5B RdRp activity of some selected compounds from the series 14-33 were found to vary between 4.1-27 % at the concentration of 100 µM. In vitro antibacterial activity evaluation of selected compounds 16-23 and 25-32, against Staphylococcus aureus ATCC 25923, Escherichia coli ATCC 25922, Pseudomonas aeruginosa ATCC 27853, Enterococcus faecalisATCC 29212, Klebsiella pneumoniae ATCC 4352, Bacillus subtilis ATCC 6633, Staphylococcus epidermidis ATCC 12228, MRSA and antifungal activity against Candida albicans ATCC 10231 resulted in the MIC values between 625->5000 µg/ml.
AU  - Bilgin, Merve
AU  - Kaushik-Basu, Neerja
AU  - Ötük, Gülten
AU  - Andrei, Graciela
AU  - Küçükgüzel, İlkay
AU  - Tatar, Esra
AU  - De Clercq, Erik
AU  - Pannecouque, Christophe
AU  - Snoeck, Robert
DO  - 10.29228/jrp.41
PY  - 2021
JO  - Journal of research in pharmacy (online)
VL  - 25
IS  - 4
SN  - 2630-6344
SP  - 507
EP  - 518
DB  - TRDizin
UR  - http://search/yayin/detay/459875
ER  -