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Pyridodiazepine amines are selective therapeutic agents for helicobacter pylori by suppressing growth through inhibition of glutamate racemase but are predicted to require continuous elevated levels in plasma to achieve clinical efficacy.
de Jonge BL, Kutschke A, Newman JV, Rooney MT, Yang W, Cederberg C. de Jonge BL, et al. Among authors: rooney mt. Antimicrob Agents Chemother. 2015 Apr;59(4):2337-42. doi: 10.1128/AAC.04410-14. Epub 2015 Feb 2. Antimicrob Agents Chemother. 2015. PMID: 25645840 Free PMC article.
Pharmacodynamic Profiling of a Siderophore-Conjugated Monocarbam in Pseudomonas aeruginosa: Assessing the Risk for Resistance and Attenuated Efficacy.
Kim A, Kutschke A, Ehmann DE, Patey SA, Crandon JL, Gorseth E, Miller AA, McLaughlin RE, Blinn CM, Chen A, Nayar AS, Dangel B, Tsai AS, Rooney MT, Murphy-Benenato KE, Eakin AE, Nicolau DP. Kim A, et al. Among authors: rooney mt. Antimicrob Agents Chemother. 2015 Dec;59(12):7743-52. doi: 10.1128/AAC.00831-15. Epub 2015 Oct 5. Antimicrob Agents Chemother. 2015. PMID: 26438502 Free PMC article.
Discovery of efficacious Pseudomonas aeruginosa-targeted siderophore-conjugated monocarbams by application of a semi-mechanistic pharmacokinetic/pharmacodynamic model.
Murphy-Benenato KE, Bhagunde PR, Chen A, Davis HE, Durand-Réville TF, Ehmann DE, Galullo V, Harris JJ, Hatoum-Mokdad H, Jahić H, Kim A, Manjunatha MR, Manyak EL, Mueller J, Patey S, Quiroga O, Rooney M, Sha L, Shapiro AB, Sylvester M, Tan B, Tsai AS, Uria-Nickelsen M, Wu Y, Zambrowski M, Zhao SX. Murphy-Benenato KE, et al. J Med Chem. 2015 Mar 12;58(5):2195-205. doi: 10.1021/jm501506f. Epub 2015 Mar 3. J Med Chem. 2015. PMID: 25658376
Identification and Optimization of Benzimidazole Sulfonamides as Orally Bioavailable Sphingosine 1-Phosphate Receptor 1 Antagonists with in Vivo Activity.
Hennessy EJ, Oza V, Adam A, Byth K, Castriotta L, Grewal G, Hamilton GA, Kamhi VM, Lewis P, Li D, Lyne P, Öster L, Rooney MT, Saeh JC, Sha L, Su Q, Wen S, Xue Y, Yang B. Hennessy EJ, et al. Among authors: rooney mt. J Med Chem. 2015 Sep 10;58(17):7057-75. doi: 10.1021/acs.jmedchem.5b01078. Epub 2015 Aug 26. J Med Chem. 2015. PMID: 26291341
Discovery of a novel class of dimeric Smac mimetics as potent IAP antagonists resulting in a clinical candidate for the treatment of cancer (AZD5582).
Hennessy EJ, Adam A, Aquila BM, Castriotta LM, Cook D, Hattersley M, Hird AW, Huntington C, Kamhi VM, Laing NM, Li D, MacIntyre T, Omer CA, Oza V, Patterson T, Repik G, Rooney MT, Saeh JC, Sha L, Vasbinder MM, Wang H, Whitston D. Hennessy EJ, et al. Among authors: rooney mt. J Med Chem. 2013 Dec 27;56(24):9897-919. doi: 10.1021/jm401075x. Epub 2013 Dec 13. J Med Chem. 2013. PMID: 24320998
SAR and Structural Analysis of Siderophore-Conjugated Monocarbam Inhibitors of Pseudomonas aeruginosa PBP3.
Murphy-Benenato KE, Dangel B, Davis HE, Durand-Réville TF, Ferguson AD, Gao N, Jahić H, Mueller JP, Manyak EL, Quiroga O, Rooney M, Sha L, Sylvester M, Wu F, Zambrowski M, Zhao SX. Murphy-Benenato KE, et al. ACS Med Chem Lett. 2015 Mar 22;6(5):537-42. doi: 10.1021/acsmedchemlett.5b00026. eCollection 2015 May 14. ACS Med Chem Lett. 2015. PMID: 26005529 Free PMC article.
Discovery of Potent and Brain-Penetrant Tau Tubulin Kinase 1 (TTBK1) Inhibitors that Lower Tau Phosphorylation In Vivo.
Halkina T, Henderson JL, Lin EY, Himmelbauer MK, Jones JH, Nevalainen M, Feng J, King K, Rooney M, Johnson JL, Marcotte DJ, Chodaparambil JV, Kumar PR, Patterson TA, Murugan P, Schuman E, Wong L, Hesson T, Lamore S, Bao C, Calhoun M, Certo H, Amaral B, Dillon GM, Gilfillan R, de Turiso FG. Halkina T, et al. J Med Chem. 2021 May 13;64(9):6358-6380. doi: 10.1021/acs.jmedchem.1c00382. Epub 2021 May 4. J Med Chem. 2021. PMID: 33944571
35 results