Future medicinal chemistry · 2026
Design synthesis and evaluation of arylamino propoxyphenyl indoles for potential atypical antipsychotic activity.
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Sharma Tanvi, Kumari Pooja, Bali Alka
Аннотация
INTRODUCTION: A series of substituted indole derivatives have been synthesized and evaluated for their atypical antipsychotic activity Compared to traditional neuroleptics, second-generation or "atypical" antipsychotics offer a more favorable therapeutic profile against both positive and negative symptoms of schizophrenia.
METHODS: The compounds were designed based on their physicochemical similarity studies to standard drugs and in silico (docking studies) with 5-HT2A and D2 receptors. The prepared compounds were evaluated for atypical antipsychotic activity in animal models of dopaminergic (apomorphine-induced mesh climbing behavior and stereotypy) and serotonergic antagonism (1-(2,5-dimethoxy-4-iodophenyl)-2 aminopropane (DOI) induced head twitch assay). All the test compounds showed. 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.
RESULTS: In-silico (docking studies) suggested good binding of the test compounds to the 5-HT2A and D2 receptors and a hypothetical binding model for the target compounds was postulated. The prepared test compounds, designated as 8 to 15, exhibited an atypical antipsychotic profile in the pharmacological assays with a mechanistic profile of combined 5-HT2A and D2 antagonism.
CONCLUSION: The study has afforded novel indole-based lead molecules with potential atypical antipsychotic effect.
METHODS: The compounds were designed based on their physicochemical similarity studies to standard drugs and in silico (docking studies) with 5-HT2A and D2 receptors. The prepared compounds were evaluated for atypical antipsychotic activity in animal models of dopaminergic (apomorphine-induced mesh climbing behavior and stereotypy) and serotonergic antagonism (1-(2,5-dimethoxy-4-iodophenyl)-2 aminopropane (DOI) induced head twitch assay). All the test compounds showed. 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.
RESULTS: In-silico (docking studies) suggested good binding of the test compounds to the 5-HT2A and D2 receptors and a hypothetical binding model for the target compounds was postulated. The prepared test compounds, designated as 8 to 15, exhibited an atypical antipsychotic profile in the pharmacological assays with a mechanistic profile of combined 5-HT2A and D2 antagonism.
CONCLUSION: The study has afforded novel indole-based lead molecules with potential atypical antipsychotic effect.