Caspase-3 inhibitory activities of some 1, 2-benzisothiazol-3-one derivatives were modeled by quantitative structure-activity relationship (QSAR) using stepwise-multiple linear regression (SW-MLR) method. The built model was robust and predictive with correlation coefficient (R(2)) of 0.91 and 0.59 for training and test groups, respectively. The quality of the model was evaluated by leave-one o...

Saccharin Chem. Abstr. Serv. Reg. No.: 81-07-2 Deleted CAS Reg. Nos: 474-91-9; 61255-27-4; 126987-83-5 Chem. Abstr. Name: 1,2-Benzisothiazol-3(2H)-one, 1,1-dioxide IUPAC Systematic Name: 1,2-Benzisothiazolin-3-one, 1,1-dioxide Synonyms: Acid saccharin; anhydro-ortho-sulfaminebenzoic acid; 3-benzisothiazolinone 1,1-dioxide; benzoic sulfimide; benzoic sulphinide; benzosulfimide; benzosulfinide; o...

A number of 1,2-benzisothiazol-3-one derivatives were prepared through structural modification of the original compound from high-throughput screening. Some analogues (e.g., 6b, 6r, 6s and 6w) were identified as novel and potent caspase inhibitors with IC50 of nanomolar. Structure-activity relationship (SAR) studies for caspase-3 inhibition were evaluated in vitro. Molecular modeling studies pr...

The synthesis of saccharin (1,2-benzisothiazol-3-one-1,1-dioxide) derivatives substituted on the benzene ring has seen limited development despite the longevity of this compound's use as an artificial sweetener. This type of saccharin derivative would however present attractive properties for the development of new bioactive, drug-like small molecule compounds. Here we report the derivatisation...

Ziprasidone Capsules contain a monohydrochloride, monohydrate salt of ziprasidone. Chemically, ziprasidone hydrochloride monohydrate is 5-[2-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]ethyl]-6chloro-1,3-dihydro-2H-indol-2-one, monohydrochloride, monohydrate The empirical formula is C21H21ClN4OS · HCl · H2O and its molecular weight is 467.42. Ziprasidone hydrochloride monohydrate is a white to s...