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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: pettibone dj. Bioorg Med Chem. 1994 Sep;2(9):971-85. doi: 10.1016/s0968-0896(00)82046-5. Bioorg Med Chem. 1994. PMID: 7712132
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: pettibone dj. 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. Eur J Pharmacol. 1991 Apr 24;196(3):233-7. doi: 10.1016/0014-2999(91)90435-s. Eur J Pharmacol. 1991. PMID: 1893911
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: pettibone dj. J Med Chem. 1995 Nov 10;38(23):4634-6. doi: 10.1021/jm00023a002. J Med Chem. 1995. PMID: 7473590 No abstract available.
Small molecule ligands for oxytocin and vasopressin receptors.
Freidinger RM, Pettibone DJ. Freidinger RM, et al. Among authors: pettibone dj. Med Res Rev. 1997 Jan;17(1):1-16. doi: 10.1002/(sici)1098-1128(199701)17:1<1::aid-med1>3.0.co;2-5. Med Res Rev. 1997. PMID: 8979247 Review. No abstract available.
Development of orally active oxytocin antagonists: studies on 1-(1-[4-[1-(2-methyl-1-oxidopyridin-3-ylmethyl)piperidin-4-yloxy]-2- methoxybenzoyl]piperidin-4-yl)-1,4-dihydrobenz[d][1,3]oxazin-2-one (L-372,662) and related pyridines.
Bell IM, Erb JM, Freidinger RM, Gallicchio SN, Guare JP, Guidotti MT, Halpin RA, Hobbs DW, Homnick CF, Kuo MS, Lis EV, Mathre DJ, Michelson SR, Pawluczyk JM, Pettibone DJ, Reiss DR, Vickers S, Williams PD, Woyden CJ. Bell IM, et al. Among authors: pettibone dj. J Med Chem. 1998 Jun 4;41(12):2146-63. doi: 10.1021/jm9800797. J Med Chem. 1998. PMID: 9622556
109 results