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Nonpeptide oxytocin antagonists: analogs of L-371,257 with improved potency.

Abstract：

:Structure-activity studies on the oxytocin antagonist 1 (L-371,257; Ki = 9.3 nM) have led to the identification of a related series of compounds containing an ortho-trifluoroethoxyphenylacetyl core which are orally bioavailable and have significantly improved potency in vitro and in vivo, e.g., compound 8 (L-374,943; Ki = 1.4 nM).

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Williams PD,Bock MG,Evans BE,Freidinger RM,Gallicchio SN,Guidotti MT,Jacobson MA,Kuo MS,Levy MR,Lis EV,Michelson SR,Pawluczyk JM,Perlow DS,Pettibone DJ,Quigley AG,Reiss DR,Salvatore C,Stauffer KJ,Woyden CJ

doi

10.1016/s0960-894x(99)00181-x

subject

Has Abstract

pub_date

1999-05-03 00:00:00

pages

1311-6

issue

9

eissn

0960-894X

issn

1464-3405

pii

S0960894X9900181X

journal_volume

9

pub_type

杂志文章

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