1-(((7, 7-Dimethyl-2 (S)-(2 (S)-amino-4-(methylsulfonyl) butyramido) bicyclo [2.2. 1] heptan-1 (S)-yl) methyl) sulfonyl)-4-(2-methylphenyl) piperazine (L-368,899): an …

…, BV Clineschmidt, JC Culberson, JM Erb

Index: Williams; Anderson; Ball; Bock; Carroll; Chiu -; Clineschmidt; Culberson; Erb; Evans; Fitzpatrick; Freidinger; Kaufman; Lundell; Murphy; Pawluczyk; Perlow; Pettibone; Pitzenberger; et al. Journal of Medicinal Chemistry, 1994 , vol. 37, # 5 p. 565 - 571

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Citation Number: 61

Abstract

Modifications to the previously reported spiroindenylpiperidine camphorsulfonamide oxytocin (OT) antagonist L-366,509 have produced a new series of o-tolylpiperazine (TP) camphorsulfonamides. A number of analogues in the TP series that incorporate a modified or unmodified L-methionine sulfone amide at the C2 endo position on the camphor ring exhibit high affinity for OT receptors (ICs0= 1.3-15 nM) and good selectivity for binding to ...