So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic.Abou-Gharbia, Magid; Moyer, John A.; Patel, Usha; Webb, Michael; Schiehser, Guy; Andree, Terrance; Haskins, J. Thomas researched the compound: 2-(tert-Butyl)isothiazol-3(2H)-one 1,1-dioxide( cas:119639-24-6 ).COA of Formula: C7H11NO3S.They published the article 《Synthesis and structure-activity relationship of substituted tetrahydro- and hexahydro-1,2-benzisothiazol-3-one 1,1-dioxides and thiadiazinones: potential anxiolytic agents》 about this compound( cas:119639-24-6 ) in Journal of Medicinal Chemistry. Keywords: piperazinylbutylbenzisothiazolone preparation anxiolytic structure activity; piperazinylbutylthiadiazinone dioxide preparation anxiolytic; benzisothiazolone piperazinylbutyl dioxide preparation anxiolytic; thiadiazinone piperazinylbutyl dioxide preparation anxiolytic. We’ll tell you more about this compound (cas:119639-24-6).
Several novel substituted tetrahydro- and hexahydro-1,2-benzisothiazole-3-one 1,1-dioxides, e.g., I [X = CH:CH, R = 2-pyrimidinyl (II); X = CH2, R = 3-C6H4CF3 (III)], IV (R = 2-pyrazinyl), and thiadiazinones V (R = 2-pyrimidinyl, 6-chloro-2-pyrazinyl) were prepared and examined in a series of in vitro and in vivo tests to determine their pharmacol. profile. Most compounds were orally active in blocking the conditioned avoidance response (CAR) but did not antagonize apomorphine-induced stereotyped behavior. Several compounds demonstrated moderate to high affinity for the 5-HT1A receptor binding site, with II and III containing 2-pyrimidinylpiperazinyl and [3-(trifluoromethyl)phenyl]piperazinyl moieties and IV containing the 2-pyrazinylpiperazinyl moiety displaying the highest affinity (K2 values of 10, 4, and 9 nM, resp. II, buspirone, and ipsapirone showed similarities in their neurochem. and behavioral profiles. They were similar in potency in blocking CAR with AB50 values of 39, 32, and 42 mg/kg, resp. They also demonstrated high affinity and selectivity for the 5-HT1A receptor site (Ki = 10 nM) and exhibited partial agonist/antagonist activity in the serotonin syndrome test. In addition, II inhibited apomorphine-induced climbing behavior much more potently (ED50 of 3.4 mg/kg) than stereotyped behavior (ED50 of 32.2 mg/kg) and will be evaluated further. Structure-activity relationships within this series of compounds are discussed.
Although many compounds look similar to this compound(119639-24-6)COA of Formula: C7H11NO3S, numerous studies have shown that this compound(SMILES:O=C(C=C1)N(C(C)(C)C)S1(=O)=O), has unique advantages. If you want to know more about similar compounds, you can read my other articles.
Reference:
Isothiazole – Wikipedia,
Isothiazole – ScienceDirect.com