33344-79-5Relevant academic research and scientific papers
Isothiazolones; Thiol-reactive inhibitors of cysteine protease cathepsin B and histone acetyltransferase PCAF
Wisastra, Rosalina,Ghizzoni, Massimo,Maarsingh, Harm,Minnaard, Adriaan J.,Haisma, Hidde J.,Dekker, Frank J.
experimental part, p. 1817 - 1822 (2011/05/03)
Isothiazolones and 5-chloroisothiazolones react chemoselectively with thiols by cleavage of the weak nitrogen-sulfur bond to form disulfides. They show selectivity for inhibition of the thiol-dependent cysteine protease cathepsin B and the histone acetylt
Synthesis and antibacterial activity of isothiazolyl oxazolidinones and analogous 3(2H)-isothiazolones
Adibpour, Neda,Khalaj, Ali,Rajabalian, Saeed
scheme or table, p. 19 - 24 (2010/03/24)
The synthesis and antibacterial activity of several new 5-((3-oxoisothiazol-2(3H)-yl)methyl)-3-phenyloxazolidin-2-ones 8 and analogous 2-(4-substituted phenyl)-3(2H)-isothiazolones 3 and 4 substituted at 4 and/or 3-positions of the phenyl moiety with different groups of which some have shown to increase the antibacterial activity of both 3-aryl-2-oxazolidinones and 3(2H)-isothiazolones is described. The most active compounds were isothiazolyl oxazolidinones 8a,j with unsubstituted and 8b with 4-F substituted phenyl rings which showed activities higher than analogous 3(2H)-isothiazolones and comparable or superior to linezolid, vancomycin, and ciprofloxacin against some tested microorganisms. The change in position of F and/or the use of larger substituents gave compounds with reduced or no activity. Evaluation of cytotoxicity to mouse fibroblast (NIH/3T3) cells indicated that these compounds exhibit antibacterial activity at non-cytotoxic concentrations.
Synthesis and antibacterial activity of 2-(4-substituted phenyl)-3(2H)-isothiazolones
Khalaj, Ali,Adibpour, Neda,Shahverdi, Ahmad Reza,Daneshtalab, Mohsen
, p. 699 - 705 (2007/10/03)
Several new and known 2-(4-substituted phenyl)-3(2H)-isothiazolone derivatives with or without chloro substituent at C-5 position were synthesized and their in vitro antibacterial activity against selected Gram-negative and Gram-positive bacteria were eva
Isothiazoles. Part 14: New 3-aminosubstituted isothiazole dioxides and their mono- and dihalogeno derivatives
Clerici, Francesca,Contini, Alessandro,Gelmi, Maria Luisa,Pocar, Donato
, p. 9399 - 9408 (2007/10/03)
3-Alkylamino- and 3-arylamino isothiazole dioxides unsubstituted at C-4 and C-5 were synthesized starting from dithiopropionic amides. Taking advantage of the direct chlorination during the cyclization process or realizing an addition-elimination process with bromine on the final 3-aminoisothiazole dioxide derivatives, the corresponding 5-chloro-, 4,5-dichloro- or the 4-bromoisothiazole dioxides could also be made available.
