Abstract:
:Synthesis and structure-activity relationships (SAR) of a novel series of vasopressin V(1b) (V(3)) antagonists are described. 2-(4-Oxo-2-aryl-quinazolin-3(4H)-yl)acetamides have been identified with low nanomolar affinity for the V(1b) receptor and good selectivity with respect to related receptors V(1a), V(2) and oxytocin (OT). Optimised compound 12j demonstrates a good pharmacokinetic profile and activity in a mechanistic model of HPA dysfunction.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Napier SE,Letourneau JJ,Ansari N,Auld DS,Baker J,Best S,Campbell-Wan L,Chan JH,Craighead M,Desai H,Goan KA,Ho KK,Hulskotte EG,MacSweeney CP,Milne R,Morphy JR,Neagu I,Ohlmeyer MH,Peeters AW,Presland J,Riviello C,doi
10.1016/j.bmcl.2010.12.081subject
Has Abstractpub_date
2011-03-15 00:00:00pages
1871-5issue
6eissn
0960-894Xissn
1464-3405pii
S0960-894X(10)01845-7journal_volume
21pub_type
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journal_title:Bioorganic & medicinal chemistry letters
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