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Eur J Med Chem. 2016 Jan 27;108:655-662. doi: 10.1016/j.ejmech.2015.12.005. Epub 2015 Dec 10.

Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.

Author information

1
Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India. Electronic address: nvsrk@suven.com.
2
Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.

Abstract

A series of 4-(1-substituted piperidin-4-yloxy) benzamides and 6-(1-substituted piperidin-4-yloxy)-3,4-dihydro-2H-isoquinolin-1-one derivatives have been synthesized and tested for their binding affinity towards H3 receptor. Most of these synthesized compounds have displayed potent binding affinity for H3 receptor when tested in in vitro binding assay. Preliminary SAR studies, functional activity, pharmacokinetic profile and efficacy profile constitute the subject matter of this communication.

KEYWORDS:

Histamine H(3) receptor; Pharmacokinetic profile; Receptor occupancy; SAR

PMID:
26731168
DOI:
10.1016/j.ejmech.2015.12.005
[Indexed for MEDLINE]

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