(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators

Aranapakam M Venkatesan; George T Grosu; Amedeo A Failli; Peter S Chan; Joseph Coupet; Trina Saunders; Hussain Mazandarani; Xun Ru

doi:10.1016/j.bmcl.2005.08.007

(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators

Bioorg Med Chem Lett. 2005 Nov 15;15(22):5003-6. doi: 10.1016/j.bmcl.2005.08.007.

Authors

Aranapakam M Venkatesan¹, George T Grosu, Amedeo A Failli, Peter S Chan, Joseph Coupet, Trina Saunders, Hussain Mazandarani, Xun Ru

Affiliation

¹ Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. venkata@wyeth.com

PMID: 16153837
DOI: 10.1016/j.bmcl.2005.08.007

Abstract

Synthesis and structure-activity relationships (SAR) of arginine vasopressin (AVP) receptor modulators are described. Potent and selective compounds are prepared when the amide linkage connecting rings A and B of VPA-985 is replaced with a bond, CO, -O-, -S-, or -SO2- bond.

MeSH terms

Antidiuretic Hormone Receptor Antagonists
Benzodiazepines / chemical synthesis*
Benzodiazepines / chemistry
Benzodiazepines / pharmacology*
Blood Platelets / drug effects
Blood Platelets / metabolism
Humans
Inhibitory Concentration 50
Molecular Structure
Pyrroles / chemical synthesis*
Pyrroles / chemistry
Pyrroles / pharmacology*
Receptors, Vasopressin / metabolism*
Sensitivity and Specificity
Structure-Activity Relationship

Substances

Antidiuretic Hormone Receptor Antagonists
Pyrroles
Receptors, Vasopressin
Benzodiazepines