title: Benzamide derivatives and their constrained analogs as histamine H3 receptor antagonists.
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.
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India. Electronic address: nvsrk@suven.com.
authors.forename: Ramakrishna
authors.initials: R
authors.lastname: Nirogi
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Anil
authors.initials: A
authors.lastname: Shinde
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Vinaykumar
authors.initials: V
authors.lastname: Tiriveedhi
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Laxman
authors.initials: L
authors.lastname: Kota
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Sangram Keshari
authors.initials: SK
authors.lastname: Saraf
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Rajesh Kumar
authors.initials: RK
authors.lastname: Badange
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Abdul Rasheed
authors.initials: AR
authors.lastname: Mohammed
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Ramkumar
authors.initials: R
authors.lastname: Subramanian
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Nageshwararao
authors.initials: N
authors.lastname: Muddana
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Gopinadh
authors.initials: G
authors.lastname: Bhyrapuneni
authors.affiliation: Discovery Research, Suven Life Sciences Ltd, Serene Chambers, Road-5, Avenue-7, Banjara Hills, Hyderabad 500 034, India.
authors.forename: Renny
authors.initials: R
authors.lastname: Abraham
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001549:Benzamides / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D004305:Dose-Response Relationship, Drug; D054828:Histamine H3 Antagonists / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D008297:Male; D015394:Molecular Structure; D051381:Rats; D017208:Rats, Wistar; D018100:Receptors, Histamine H3 / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D001549:Benzamides; D054828:Histamine H3 Antagonists; D018100:Receptors, Histamine H3
keywords: Histamine H(3) receptor; Pharmacokinetic profile; Receptor occupancy; SAR