80883-92-7Relevant 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.
Synthesis, carbonic anhydrase I and II inhibition studies of the 1,3,5-trisubstituted-pyrazolines
Gul, Halise Inci,Mete, Ebru,Taslimi, Parham,Gulcin, Ilhami,Supuran, Claudiu T.
, p. 189 - 192 (2017/11/21)
4-(3-(4-Substituted-phenyl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl) benzenesulfonamides (9–16) were successfully synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR, and HRMS spectra. Carbonic anhydrase I and II inhibitory effects of the compounds were investigated. Ki values of the compounds were in the range of 316.7 ± 9.6–533.1 ± 187.8 nM towards hCA I and 412.5 ± 115.4–624.6 ± 168.2 nM towards hCA II isoenzymes. While Ki values of the reference compound Acetazolamide were 278.8 ± 44.3 nM and 293.4 ± 46.4 nM towards hCA I and hCA II izoenzymes, respectively. Compound 14 with bromine and compound 13 with fluorine substituents can be considered as the leader compounds of the series because of the lowest Ki values in series to make further detailed carbonic anhydrase inhibiton studies.
Synthesis, molecular docking study, and cytotoxic activity of 1,3,5-triaryl pyrazole derivatives
Ghasemi, Maryam,Ghadbeighi, Sajad,Amirhamzeh, Amirali,Tabatabai, Seyed Abbas,Ostad, Seyed Nasser,Shafiee, Abbas,Amini, Mohsen
, p. 121 - 128 (2016/03/12)
Synthesis, molecular docking study, and cytotoxic activity of a new group of 1,3,5-triaryl pyrazole derivatives were be studied. The antiproliferative activity of the final compounds were examined in MCF-7, AGS, HT-29 and NIH3T3 cell lines by MTT assay, u
Pyrazole Derivatives with Possible Hypoglycemic Activity
Faid-Allah, Hassan M.,Mokhtar, Hassan M.
, p. 245 - 249 (2007/10/02)
Condensation of p-sulphamylphenylhydrazine hydrochloride with different chalcones, leads either to hydrzones (2) or to pyrazolines (3) depending on the reaction conditions.The hydrazones (2) are readily converted into pyrazolines (3) on heating with hydro
