Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 74, Issue -, Pages 477-490Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2013.09.020
Keywords
Atypical antipsychotics; Indole derivatives; Log BB; D-2/5-HT2A antagonists; In silico; Docking studies
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Funding
- University Grants Commission
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A series of substituted indole derivatives have been synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced mesh climbing and stereotypy assays in mice. The compounds 11 and 12 have emerged as important lead compounds showing potential atypical antipsychotic profile. In silico (docking studies) have been carried out to postulate a hypothetical binding model for the target compounds with respect to the dopaminergic D-2 and 5-HT2A receptors. Theoretical ADME profiling of the compounds based on selected physicochemical parameters has suggested an excellent compliance with Lipinski's rules. The potential of these compounds to penetrate the blood brain barrier (log BB) was computed through an online software program and the values obtained for the compounds suggest good potential for brain permeation. (C) 2013 Elsevier Masson SAS. All rights reserved.
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