(4-Substituted-phenyl)-(5H-10,11-dihydro-pyrrolo [2,1-c][1,4] benzodiazepin-10-yl)-methanone derivatives as vasopressin receptor modulators.
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.
Venkatesan
Aranapakam M
AM
Chemical and Screening Sciences, Wyeth Research, Pearl River, NY 10965, USA. venkata@wyeth.com
Grosu
George T
GT
Failli
Amedeo A
AA
Chan
Peter S
PS
Coupet
Joseph
J
Saunders
Trina
T
Mazandarani
Hussain
H
Ru
Xun
X
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
D065092:Antidiuretic Hormone Receptor Antagonists; D011758:Pyrroles; D017483:Receptors, Vasopressin; D001569:Benzodiazepines