363604-04-0Relevant articles and documents
Pyrazolylbenzo[d]imidazoles as new potent and selective inhibitors of carbonic anhydrase isoforms hCA IX and XII
Kumar, Satish,Ceruso, Mariangela,Tuccinardi, Tiziano,Supuran, Claudiu T.,Sharma, Pawan K.
, p. 2907 - 2913 (2016/06/13)
Novel pyrazolylbenzo[d]imidazole derivatives (2a-2f) were designed, synthesized and evaluated against four human carbonic anhydrase isoforms belonging to α family comprising of two cytosolic isoforms hCA I and II as well as two transmembrane tumor associated isoforms hCA IX and XII. Starting from these derivatives that showed high potency but low selectivity in favor of tumor associated isoforms hCA IX and XII, we investigated the impact of removing the sulfonamide group. Thus, analogs 3a-3f without sulfonamide moiety were synthesized and biological assay revealed a good activity as well as an excellent selectivity as inhibitors for tumor associated hCA IX and hCA XII and the same was analyzed by molecular docking studies.
Synthesis of 4-(2-substituted hydrazinyl)benzenesulfonamides and their carbonic anhydrase inhibitory effects
Gul, Halise Inci,Kucukoglu, Kaan,Yamali, Cem,Bilginer, Sinan,Yuca, Hafize,Ozturk, Iknur,Taslimi, Parham,Gulcin, Ilhami,Supuran, Claudiu T.
, p. 568 - 573 (2016/05/09)
In this study, 4-(2-substituted hydrazinyl)benzenesulfonamides were synthesized by microwave irradiation and their chemical structures were confirmed by 1H NMR, 13CNMR, and HRMS. Ketones used were: Acetophenone (S1), 4-methylacetophe
Synthesis and biological evaluation of some 4-functionalized-pyrazoles as antimicrobial agents
Sharma, Pawan K.,Chandak, Navneet,Kumar, Pawan,Sharma, Chetan,Aneja, Kamal R.
experimental part, p. 1425 - 1432 (2011/04/24)
1,3-Diaryl-4-formylpyrazoles 8 bearing benzenesulfonamide moiety at position-1 were synthesized as important intermediates following Vilsmeier-Haack strategy. Aldehyde moiety of 4-formylpyrazole was then converted into carboxylic acid 9, cyano 10 and carbothioamide 11 using established procedures. Out of these 4-functionalized pyrazoles, pyrazole-4-carboxylic acids 9 and carbothioamides 11 were evaluated for their in vitro antibacterial activity against four pathogenic bacterial strains namely, Staphylococcus aureus, Bacillus subtilis (Gram-positive), Escherichia coli, Pseudomonas aeruginosa (Gram-negative), and in vitro antifungal activity against two pathogenic fungal strains namely, Aspergillus niger and Aspergillus flavus. Three tested compounds, 9e, 11b and 11f exhibited moderate antibacterial activity against Gram-positive bacteria and 9g showed moderate antifungal activity against the tested fungi. However, none of the compounds showed any activity against Gram-negative bacteria.
