Literature DB >> 29395980

Synthesis and biological evaluation of a series of novel pyridinecarboxamides as potential multi-receptor antipsychotic drugs.

Mingshuo Xu1, Yu Wang2, Feipu Yang2, Chunhui Wu3, Zhen Wang2, Bin Ye3, Xiangrui Jiang2, Qingjie Zhao2, Jianfeng Li2, Yongjian Liu3, Junchi Zhang2, Guanghui Tian3, Yang He4, Jingshan Shen5, Hualiang Jiang2.   

Abstract

In previous study, a series of benzamides was identified as potent antipsychotic agents. As a continuation of the program to discover novel antipsychotics, herein we reported the evaluation of a series of pyridinecarboxamide derivatives. The most promising compound 7h not only held good activities on dopamine D2, serotonin 5-HT1A and 5-HT2A receptors, but also exhibited low potency for α1A, H1 and 5-HT2C receptors, indicating a low propensity of side effects like orthostatic hypotension and weight gain. Furthermore, 7h exhibited more potent antipsychotic-like effect than aripiprazole in behavioral studies. The preliminary results were promising enough for further research around this scaffold.
Copyright © 2018 Elsevier Ltd. All rights reserved.

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Keywords:  5-HT(1A) receptor; Antipsychotic; Multi-receptor; PCP-induced hyperlocomotion; Pyridinecarboxamide

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Year:  2018        PMID: 29395980     DOI: 10.1016/j.bmcl.2018.01.038

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

1.  Computational approaches for the design of novel dopamine D2 and serotonin 5-HT2A receptor dual antagonist towards schizophrenia.

Authors:  Akash Rathore; Vivek Asati; Mitali Mishra; Ratnesh Das; Varsha Kashaw; Sushil Kumar Kashaw
Journal:  In Silico Pharmacol       Date:  2022-04-08
  1 in total

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