title: (4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
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.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. venkata@wyeth.com
authors.forename: Aranapakam M
authors.initials: AM
authors.lastname: Venkatesan
authors.forename: George T
authors.initials: GT
authors.lastname: Grosu
authors.forename: Amedeo A
authors.initials: AA
authors.lastname: Failli
authors.forename: Peter S
authors.initials: PS
authors.lastname: Chan
authors.forename: Joseph
authors.initials: J
authors.lastname: Coupet
authors.forename: Trina
authors.initials: T
authors.lastname: Saunders
authors.forename: Hussain
authors.initials: H
authors.lastname: Mazandarani
authors.forename: Xun
authors.initials: X
authors.lastname: Ru
mesh_terms: D065092:Antidiuretic Hormone Receptor Antagonists; D001569:Benzodiazepines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001792:Blood Platelets / Q000187:drug effects / Q000378:metabolism; D006801:Humans; D020128:Inhibitory Concentration 50; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017483:Receptors, Vasopressin / Q000378:metabolism*; D012680:Sensitivity and Specificity; D013329:Structure-Activity Relationship
chemical_list: D065092:Antidiuretic Hormone Receptor Antagonists; D011758:Pyrroles; D017483:Receptors, Vasopressin; D001569:Benzodiazepines