1415669-39-4Relevant academic research and scientific papers
Synthesis of sulfonamides bearing 1,3,5-triarylpyrazoline and 4-thiazolidinone moieties as novel antimicrobial agents
Thach, Thi-Dan,Le, Thi Tuong-Vi,Nguyen, Huu Thien-An,Dang, Chi-Hien,Dang, Van-Su,Nguyen, Thanh-Danh
, p. 158 - 162 (2020/05/08)
Two series of sulfonamides were synthesized from 4-hydrazinylben-zenesulfonamide as the key starting material. 1,3,5-Triarylpyrazoline sulfonamides (2a-i) were obtained by cyclocondensation of various chalcones in 53-64 % yields, while 4-thiazolidinone derivatives (4a-e) were synthesized by cyclocondensation between mercaptoacetic acid and different phenylhydrazones in 43-62 % yields. The synthesized compounds were characterized based on FTIR, 1H-NMR, 13C-NMR and HRMS data. The sulfonamides were evaluated for their in vitro antimicrobial activities against four bacterial strains (E. coli, P. aeruginosa, B. subtillis and S aureus), two filamentous fungal strains (A. Niger and F. oxysporum) and two yeast strains (C. albicans and S. cerevisiae). Seven pyrazolines, 2a-c and 2e-h, exhibited significant inhibition of different microbial strains. Among them, compound 2b displayed good antifungal activity against A. Niger (MIC value at 12.5 μg mL-1) over the reference drug.
Molecular modeling, synthesis and screening of some new 4-thiazolidinone derivatives with promising selective COX-2 inhibitory activity
Unsal-Tan, Oya,Ozadali, Keriman,Piskin, Kevser,Balkan, Ayla
, p. 59 - 64 (2013/01/15)
In order to develop new selective cyclooxygenase-2 inhibitors, a series of novel 2-aryl-3-(4-sulfamoyl/methylsulfonylphenylamino)-4-thiazolidinones were designed. Molecular modeling studies with COX-2 enzyme were performed by using MOE program. The designed compounds with reasonable binding modes and high docking scores were synthesized. Their COX-1/COX-2 inhibitory activities were evaluated in vitro, using NS-398 and indomethacine as reference compounds. Compounds possessing methyl group (3d and 4d) on the phenyl ring exhibited highly COX-2 inhibitory selectivity and potency.
