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Issue 6, 2018
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Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists

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Abstract

We designed and synthesized a new biphenyl amide–tryptamine hybrid molecule 7 utilizing a pharmacophore-based approach as a 5-HT2B antagonist. The hybrid compound 7 was evaluated for its affinity to a panel of seven 5-HT receptors, demonstrating high selectivity for the 5-HT2B receptor. Functional assays revealed potent antagonism of 5-HT2B by 7 with an IC50 value of 14.1 nM. Moreover, compound 7 possessed a desirable in vitro pharmacokinetic profile and maintained its antagonistic potency in the presence of physiological concentrations of serum proteins. The design approach implemented in this investigation would facilitate the development of a second generation of highly selective and potent 5-HT2B antagonists.

Graphical abstract: Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists

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Publication details

The article was received on 16 Apr 2018, accepted on 17 May 2018 and first published on 21 May 2018


Article type: Research Article
DOI: 10.1039/C8MD00204E
Citation: Med. Chem. Commun., 2018,9, 1069-1075
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    Pharmacophore-based tailoring of biphenyl amide derivatives as selective 5-hydroxytryptamine 2B receptor antagonists

    M. T. Gabr and M. S. Abdel-Raziq, Med. Chem. Commun., 2018, 9, 1069
    DOI: 10.1039/C8MD00204E

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