The discovery of GSK221149A: A potent and selective oxytocin antagonist

Bioorganic and Medicinal Chemistry Letters

Volumn 18, Issue 1, 2008, Pages 90-94

  Liddle, John ^a   Allen, Michael J ^a   Borthwick, Alan D ^a   Brooks, David P ^b   Davies, David E ^a   Edwards, Richard M ^b   Exall, Anne M ^a   Hamlett, Chris ^a   Irving, Wendy R ^a   Mason, Andrew M ^a   McCafferty, Gerald P ^b   Nerozzi, Fabrizio ^a   Peace, Simon ^a   Philp, Joanne ^a   Pollard, Derek ^a   Pullen, Mark A ^b   Shabbir, Shaila S ^a   Sollis, Steve L ^a   Westfall, Timothy D ^b   Woollard, Pat M ^a   Wu, Charlene ^b   Hickey, Deirdre M B ^a   more..

^a GLAXOSMITHKLINE   (United Kingdom)

^b GLAXOSMITHKLINE   (United States)

Author keywords

Diketopiperazine; Labour; Oxytocin; Tocolytic

Indexed keywords

GSK 221149A; OXAZOLE DERIVATIVE; OXYTOCIN ANTAGONIST; PIPERAZINEDIONE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CONTROLLED STUDY; DRUG EFFECT; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SELECTIVITY; DRUG SYNTHESIS; FEMALE; NONHUMAN; PREMATURE LABOR; RAT; RECEPTOR AFFINITY; SPRAGUE DAWLEY RAT; STRUCTURE ACTIVITY RELATION; UTERUS CONTRACTILITY;

ANIMALS; FEMALE; HUMANS; KINETICS; OXYTOCIN; PIPERAZINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, OXYTOCIN; STRUCTURE-ACTIVITY RELATIONSHIP; UTERINE CONTRACTION;

RATTUS;

EID: 37549041338     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2007.11.008     Document Type: Article

References (16)

1. Vatish M., and Thornton S. Expert Opin. Ther. Patents 12 9 (2002) 1403
2. Schwartz M.K., and Page P. Curr. Med. Chem. 10 (2003) 1441
3. Dawood M.Y. Am. J. Pertinatol. 6 (1989) 167
4. Fuchs A.R., Fuchs F., Husslein P., and Soloff M.S. Am. J. Obstet. Gynaecol. 150 (1984) 734
5. Kimura T., Takemura M., Nomura S., Nobunaga T., Kubota Y., Inoue T., Hashimoto K., Kumazawa I., Ito Y., Ohashi K., Koyama M., Azuma C., Kitamura Y., and Saji F. Endocrinology 137 (1996) 780
6. Freidinger R.M., and Pettibone D.J. Med. Res. Rev. 17 (1997) 1
7. Lundin S., Broeders A., and Melin P. Clin. Endocrinol. 39 (1993) 369
8. Manning M., Stoev S., Cheng L.L., Wo N.C., and Chan W.Y. J. Pept. Sci. 7 (2001) 449
9. Borthwick A.D., Davies D.D., Exall A.M., Livermore D.G., Sollis S.L., Nerozzi F., Allen M.J., Perren M., Shabbir S.S., Woollard P.M., and Wyatt P.G. J. Med. Chem. 28 (2005) 6956
10. The method for the binding assay is described in the following publication. Wyatt P.G., Allen M.J., Chilcott J., Hickin G., Miller N.D., and Woollard P.M. Bioorg. Med. Chem. Lett. 11 (2001) 1301
11. HPLC based measurement of lipophilicity. Valko K., Du C.M., Bevan C., Reynolds D.P., and Abrahams M.H. Curr. Med. Chem. 8 (2001) 1137
12. A human serum albumin coated HPLC column method. Valko K., Nunhuck S., Bevan C., Reynolds D.P., and Abrahams M.H. J. Pharm. Sci. 92 (2003) 2236
13. Wyatt P.G., Allen M.J., Borthwick A.D., Davies D.D., Exall A.M., Hatley R.J.D., Irving W.R., Livermore D.G., Miller N.D., Nerozzi F., Sollis S.L., and Szardenings A.K. Bioorg. Med. Chem. Lett. 15 (2005) 2579
14. Dimethyl, tert-butyl and isopropyl amides are generally equipotent in the binding assay.
15. McCafferty G.P., Pullen M.A., Wu C., Edwards R.M., Allen M.A., Woollard P.M., Borthwick A.D., Liddle J., Hickey D.M.B., Brooks D.P., and Westfall T.D. Am. J. Physiol. (2007) 293
16. Sollis S.L. J. Org. Chem. 70 (2005) 4735