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Discovery of potent, selective, bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model, part I: transformation of selective pyrazolodiazepinone phosphodiesterase 4 (PDE4) inhibitors into selective PDE2 inhibitors.
Plummer MS, Cornicelli J, Roark H, Skalitzky DJ, Stankovic CJ, Bove S, Pandit J, Goodman A, Hicks J, Shahripour A, Beidler D, Lu XK, Sanchez B, Whitehead C, Sarver R, Braden T, Gowan R, Shen XQ, Welch K, Ogden A, Sadagopan N, Baum H, Miller H, Banotai C, Spessard C, Lightle S. Plummer MS, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3438-42. doi: 10.1016/j.bmcl.2013.03.072. Epub 2013 Mar 28. Bioorg Med Chem Lett. 2013. PMID: 23582272
Discovery of potent selective bioavailable phosphodiesterase 2 (PDE2) inhibitors active in an osteoarthritis pain model. Part II: optimization studies and demonstration of in vivo efficacy.
Plummer MS, Cornicelli J, Roark H, Skalitzky DJ, Stankovic CJ, Bove S, Pandit J, Goodman A, Hicks J, Shahripour A, Beidler D, Lu XK, Sanchez B, Whitehead C, Sarver R, Braden T, Gowan R, Shen XQ, Welch K, Ogden A, Sadagopan N, Baum H, Miller H, Banotai C, Spessard C, Lightle S. Plummer MS, et al. Bioorg Med Chem Lett. 2013 Jun 1;23(11):3443-7. doi: 10.1016/j.bmcl.2013.03.082. Epub 2013 Mar 29. Bioorg Med Chem Lett. 2013. PMID: 23597790
Binding thermodynamics of substituted diaminopyrimidine renin inhibitors.
Sarver RW, Peevers J, Cody WL, Ciske FL, Dyer J, Emerson SD, Hagadorn JC, Holsworth DD, Jalaie M, Kaufman M, Mastronardi M, McConnell P, Powell NA, Quin J 3rd, Van Huis CA, Zhang E, Mochalkin I. Sarver RW, et al. Anal Biochem. 2007 Jan 1;360(1):30-40. doi: 10.1016/j.ab.2006.10.017. Epub 2006 Oct 30. Anal Biochem. 2007. PMID: 17113558
Preparation of novel anthranilic acids as antibacterial agents: extensive evaluation of structural and physical properties on antibacterial activity and human serum albumin affinity.
Thorarensen A, Li J, Wakefield BD, Romero DL, Marotti KR, Sweeney MT, Zurenko GE, Sarver RW. Thorarensen A, et al. Among authors: sarver rw. Bioorg Med Chem Lett. 2007 Jun 1;17(11):3113-6. doi: 10.1016/j.bmcl.2007.03.036. Epub 2007 Mar 15. Bioorg Med Chem Lett. 2007. PMID: 17400450
33 results