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Preclinical evaluation of an inhibitor of cytosolic phospholipase A2α for the treatment of asthma.
Hewson CA, Patel S, Calzetta L, Campwala H, Havard S, Luscombe E, Clarke PA, Peachell PT, Matera MG, Cazzola M, Page C, Abraham WM, Williams CM, Clark JD, Liu WL, Clarke NP, Yeadon M. Hewson CA, et al. Among authors: abraham wm. J Pharmacol Exp Ther. 2012 Mar;340(3):656-65. doi: 10.1124/jpet.111.186379. Epub 2011 Dec 7. J Pharmacol Exp Ther. 2012. PMID: 22160268
Benzenesulfonamide indole inhibitors of cytosolic phospholipase A2alpha: optimization of in vitro potency and rat pharmacokinetics for oral efficacy.
Lee KL, Behnke ML, Foley MA, Chen L, Wang W, Vargas R, Nunez J, Tam S, Mollova N, Xu X, Shen MW, Ramarao MK, Goodwin DG, Nickerson-Nutter CL, Abraham WM, Williams C, Clark JD, McKew JC. Lee KL, et al. Among authors: abraham wm. Bioorg Med Chem. 2008 Feb 1;16(3):1345-58. doi: 10.1016/j.bmc.2007.10.060. Epub 2007 Oct 22. Bioorg Med Chem. 2008. PMID: 17998165
Indole cytosolic phospholipase A2 alpha inhibitors: discovery and in vitro and in vivo characterization of 4-{3-[5-chloro-2-(2-{[(3,4-dichlorobenzyl)sulfonyl]amino}ethyl)-1-(diphenylmethyl)-1H-indol-3-yl]propyl}benzoic acid, efipladib.
McKew JC, Lee KL, Shen MW, Thakker P, Foley MA, Behnke ML, Hu B, Sum FW, Tam S, Hu Y, Chen L, Kirincich SJ, Michalak R, Thomason J, Ipek M, Wu K, Wooder L, Ramarao MK, Murphy EA, Goodwin DG, Albert L, Xu X, Donahue F, Ku MS, Keith J, Nickerson-Nutter CL, Abraham WM, Williams C, Hegen M, Clark JD. McKew JC, et al. Among authors: abraham wm. J Med Chem. 2008 Jun 26;51(12):3388-413. doi: 10.1021/jm701467e. Epub 2008 May 23. J Med Chem. 2008. PMID: 18498150
Potent, nonpeptide inhibitors of human mast cell tryptase. Synthesis and biological evaluation of novel spirocyclic piperidine amide derivatives.
Costanzo MJ, Yabut SC, Zhang HC, White KB, de Garavilla L, Wang Y, Minor LK, Tounge BA, Barnakov AN, Lewandowski F, Milligan C, Spurlino JC, Abraham WM, Boswell-Smith V, Page CP, Maryanoff BE. Costanzo MJ, et al. Among authors: abraham wm. Bioorg Med Chem Lett. 2008 Mar 15;18(6):2114-21. doi: 10.1016/j.bmcl.2008.01.093. Epub 2008 Jan 30. Bioorg Med Chem Lett. 2008. PMID: 18272363
Pharmacological properties of N-(3,5-diamino-6-chloropyrazine-2-carbonyl)-N'-4-[4-(2,3-dihydroxypropoxy)phenyl]butyl-guanidine methanesulfonate (552-02), a novel epithelial sodium channel blocker with potential clinical efficacy for cystic fibrosis lung disease.
Hirsh AJ, Zhang J, Zamurs A, Fleegle J, Thelin WR, Caldwell RA, Sabater JR, Abraham WM, Donowitz M, Cha B, Johnson KB, St George JA, Johnson MR, Boucher RC. Hirsh AJ, et al. Among authors: abraham wm. J Pharmacol Exp Ther. 2008 Apr;325(1):77-88. doi: 10.1124/jpet.107.130443. Epub 2008 Jan 24. J Pharmacol Exp Ther. 2008. PMID: 18218832
220 results