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Conformationally constrained o-tolylpiperazine camphorsulfonamide oxytocin antagonists. Structural modifications that provide high receptor affinity and suggest a bioactive conformation.
Williams PD, Ball RG, Clineschmidt BV, Culberson JC, Erb JM, Freidinger RM, Pawluczyk JM, Perlow DS, Pettibone DJ, Veber DF. Williams PD, et al. Among authors: veber df. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
1-(1-[4-[(N-acetyl-4-piperidinyl)oxy]-2-methoxybenzoyl]piperidin-4- yl)-4H-3,1-benzoxazin-2(1H)-one (L-371,257): a new, orally bioavailable, non-peptide oxytocin antagonist.
Williams PD, Clineschmidt BV, Erb JM, Freidinger RM, Guidotti MT, Lis EV, Pawluczyk JM, Pettibone DJ, Reiss DR, Veber DF, et al. Williams PD, et al. Among authors: veber df. J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002. J Med Chem. 1995. PMID: 7473590 No abstract available.
Orally active, nonpeptide oxytocin antagonists.
Evans BE, Leighton JL, Rittle KE, Gilbert KF, Lundell GF, Gould NP, Hobbs DW, DiPardo RM, Veber DF, Pettibone DJ, et al. Evans BE, et al. Among authors: veber df. J Med Chem. 1992 Oct 16;35(21):3919-27. doi: 10.1021/jm00099a020. J Med Chem. 1992. PMID: 1331449
Bradykinin agonist activity of a novel, potent oxytocin antagonist.
Pettibone DJ, Clineschmidt BV, Lis EV, Ransom RW, Totaro JA, Young GS, Bock MG, Freidinger RM, Veber DF, Williams PD. Pettibone DJ, et al. Among authors: veber df. Eur J Pharmacol. 1991 Apr 24;196(3):233-7. doi: 10.1016/0014-2999(91)90435-s. Eur J Pharmacol. 1991. PMID: 1893911
Identification of an orally active, nonpeptidyl oxytocin antagonist.
Pettibone DJ, Clineschmidt BV, Kishel MT, Lis EV, Reiss DR, Woyden CJ, Evans BE, Freidinger RM, Veber DF, Cook MJ, et al. Pettibone DJ, et al. Among authors: veber df. J Pharmacol Exp Ther. 1993 Jan;264(1):308-14. J Pharmacol Exp Ther. 1993. PMID: 8423533
100 results