Discovery of N-[2-[2-[[3-Methoxy-4-(5-oxazolyl)phenyl]amino]-5-oxazolyl]phenyl]-N-methyl-4- morpholineacetamide as a Novel and Potent Inhibitor of Inosine Monophosphate Dehydrogenase with Excellent in Vivo Activity

Autor: Dhar, T. G. M., Shen, Z., Guo, J., Liu, C., Watterson, S. H., Gu, H. H., Pitts, W. J., Fleener, C. A., Rouleau, K. A., Sherbina, N. Z., McIntyre, K. W., Witmer, M. R., Tredup, J. A., Chen, B.-C., Zhao, R., Bednarz, M. S., Cheney, D. L., MacMaster, J. F., Miller, L. M., Berry, K. K., Harper, T. W., Barrish, J. C., Hollenbaugh, D. L., Iwanowicz, E. J.

Publikováno v: Journal of Medicinal Chemistry; May 2002, Vol. 45 Issue: 11 p2127-2130, 4p

BMS-229724 is a tight-binding inhibitor of cytosolic phospholipase A2 that acts at the lipid/water interface and possesses anti-inflammatory activity in skin inflammation models.

Autor: Burke JR; Dermatology Drug Discovery, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543, USA. james.burke@bms.com, Davern LB, Stanley PL, Gregor KR, Banville J, Remillard R, Russell JW, Brassil PJ, Witmer MR, Johnson G, Tredup JA, Tramposch KM

Publikováno v: The Journal of pharmacology and experimental therapeutics [J Pharmacol Exp Ther] 2001 Jul; Vol. 298 (1), pp. 376-85.

A beta-lactam inhibitor of cytosolic phospholipase A2 which acts in a competitive, reversible manner at the lipid/water interface.

Autor: Burke JR; Department of Dermatology Discovery Research, Buffalo, New York, USA., Gregor KR, Padmanabha R, Banville J, Witmer MR, Davern LB, Manly SP, Tramposch KM

Publikováno v: Journal of enzyme inhibition [J Enzyme Inhib] 1998 Jun; Vol. 13 (3), pp. 195-206.

Cooperativity and binding in the mechanism of cytosolic phospholipase A2.

Autor: Burke JR; Department of Chemistry, Princeton University, New Jersey 08540, USA., Witmer MR, Tredup J, Micanovic R, Gregor KR, Lahiri J, Tramposch KM, Villafranca JJ

Publikováno v: Biochemistry [Biochemistry] 1995 Nov 21; Vol. 34 (46), pp. 15165-74.

Active recombinant human cytosolic phospholipase A2 is expressed in Escherichia coli.

Autor: Witmer MR; Macromolecular Structure Department, Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, New Jersey 08543-4000, USA., Micanovic R, Tredup J, Lin W, Hail M, Villafranca JJ

Publikováno v: Archives of biochemistry and biophysics [Arch Biochem Biophys] 1995 Apr 20; Vol. 318 (2), pp. 430-8.