4337-51-3Relevant articles and documents
Synthesis and pharmacological characterization of novel N-(trans-4-(2-(4-(benzo[d]isothiazol-3-yl)piperazin-1-yl)ethyl)cyclohexyl)amides as potential multireceptor atypical antipsychotics
Chen, Xiao-Wen,Sun, Yuan-Yuan,Fu, Lei,Li, Jian-Qi
, p. 332 - 353 (2016/08/04)
A series of novel benzisothiazolylpiperazine derivatives combining potent dopamine D2and D3, and serotonin 5-HT1Aand 5-HT2Areceptor properties were synthesized and evaluated for their potential antipsychotic properties. The most-promising derivative was 9j. The unique pharmacological features of 9j were a high affinity for D2, D3, 5-HT1A, and 5-HT2Areceptors, together with a 20-fold selectivity for the D3versus D2subtype, and a low affinity for muscarinic M1(reducing the risk of anticholinergic side effects), and for hERG channels (reducing incidence of QT interval prolongation). In animal behavioral models, 9j inhibited the locomotor-stimulating effects of phencyclidine, blocked conditioned avoidance response, and improved the cognitive deficit in the novel object recognition tests in rats. 9j exhibited a low potential for catalepsy, consistent with results with risperidone. In addition, favorable brain penetration of 9j in rats was detected. These studies have demonstrated that 9j is a potential atypical antipsychotic candidate.
Selective synthesis of 1,2-benzisothiazol-3-one-1-oxide nitro derivatives
Serebryakov,Kislitsin,Semenov,Zlotin
, p. 1659 - 1664 (2007/10/03)
A new selective synthesis of 1,2-benzisothiazol-3-one-1-oxide nitro derivatives by reaction of 2-benzylthio-4-nitro- and 2-benzylthio-4,6-dinitrobenzamides with gaseous chlorine in wet CH2Cl2 has been developed Reactions of N-unsubstituted 2-benzylthio-4-nitro- and 2-benzylthio-4,6-dinitrobenzamides with gaseous chlorine in 60% AcOH give, instead of the S-oxides, the appropriate 1,2-benzisothiazol-3-one-1,1-dioxide nitro derivatives.
2,2-DICARBAMIDO-5,5-DINITRODIPHENYLDISULFIDES AND
PONCI,GIALDI,BARUFFINI
, p. 254 - 268 (2007/10/08)
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