1. Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
- Author
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Nirogi R, Shinde A, Tiriveedhi V, Kota L, Saraf SK, Badange RK, Mohammed AR, Subramanian R, Muddana N, Bhyrapuneni G, and Abraham R
- Subjects
- Administration, Oral, Animals, Benzamides administration & dosage, Benzamides chemistry, Dose-Response Relationship, Drug, Histamine H3 Antagonists administration & dosage, Histamine H3 Antagonists chemistry, Humans, Male, Molecular Structure, Rats, Rats, Wistar, Structure-Activity Relationship, Benzamides pharmacology, Histamine H3 Antagonists pharmacology, Receptors, Histamine H3 metabolism
- 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., (Copyright © 2015 Elsevier Masson SAS. All rights reserved.)
- Published
- 2016
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