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187 results

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Page 1
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Lapointe G, Skepper CK, Holder LM, Armstrong D, Bellamacina C, Blais J, Bussiere D, Bian J, Cepura C, Chan H, Dean CR, De Pascale G, Dhumale B, Fisher LM, Fulsunder M, Kantariya B, Kim J, King S, Kossy L, Kulkarni U, Lakshman J, Leeds JA, Ling X, Lvov A, Ma S, Malekar S, McKenney D, Mergo W, Metzger L, Mhaske K, Moser HE, Mostafavi M, Namballa S, Noeske J, Osborne C, Patel A, Patel D, Patel T, Piechon P, Polyakov V, Prajapati K, Prosen KR, Reck F, Richie DL, Sanderson MR, Satasia S, Savani B, Selvarajah J, Sethuraman V, Shu W, Tashiro K, Thompson KV, Vaarla K, Vala L, Veselkov DA, Vo J, Vora B, Wagner T, Wedel L, Williams SL, Yendluri S, Yue Q, Yifru A, Zhang Y, Rivkin A. Lapointe G, et al. J Med Chem. 2021 May 13;64(9):6329-6357. doi: 10.1021/acs.jmedchem.1c00375. Epub 2021 Apr 30. J Med Chem. 2021. PMID: 33929852
Application of Virtual Screening to the Identification of New LpxC Inhibitor Chemotypes, Oxazolidinone and Isoxazoline.
Lee PS, Lapointe G, Madera AM, Simmons RL, Xu W, Yifru A, Tjandra M, Karur S, Rico A, Thompson K, Bojkovic J, Xie L, Uehara K, Liu A, Shu W, Bellamacina C, McKenney D, Morris L, Tonn GR, Osborne C, Benton BM, McDowell L, Fu J, Sweeney ZK. Lee PS, et al. Among authors: lapointe g. J Med Chem. 2018 Oct 25;61(20):9360-9370. doi: 10.1021/acs.jmedchem.8b01287. Epub 2018 Oct 3. J Med Chem. 2018. PMID: 30226381
Topoisomerase Inhibitors Addressing Fluoroquinolone Resistance in Gram-Negative Bacteria.
Skepper CK, Armstrong D, Balibar CJ, Bauer D, Bellamacina C, Benton BM, Bussiere D, De Pascale G, De Vicente J, Dean CR, Dhumale B, Fisher LM, Fuller J, Fulsunder M, Holder LM, Hu C, Kantariya B, Lapointe G, Leeds JA, Li X, Lu P, Lvov A, Ma S, Madhavan S, Malekar S, McKenney D, Mergo W, Metzger L, Moser HE, Mutnick D, Noeske J, Osborne C, Patel A, Patel D, Patel T, Prajapati K, Prosen KR, Reck F, Richie DL, Rico A, Sanderson MR, Satasia S, Sawyer WS, Selvarajah J, Shah N, Shanghavi K, Shu W, Thompson KV, Traebert M, Vala A, Vala L, Veselkov DA, Vo J, Wang M, Widya M, Williams SL, Xu Y, Yue Q, Zang R, Zhou B, Rivkin A. Skepper CK, et al. Among authors: lapointe g. J Med Chem. 2020 Jul 23;63(14):7773-7816. doi: 10.1021/acs.jmedchem.0c00347. Epub 2020 Jul 7. J Med Chem. 2020. PMID: 32634310
MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery.
Brocklehurst CE, Altmann E, Bon C, Davis H, Dunstan D, Ertl P, Ginsburg-Moraff C, Grob J, Gosling DJ, Lapointe G, Marziale AN, Mues H, Palmieri M, Racine S, Robinson RI, Springer C, Tan K, Ulmer W, Wyler R. Brocklehurst CE, et al. Among authors: lapointe g. J Med Chem. 2024 Feb 8;67(3):2118-2128. doi: 10.1021/acs.jmedchem.3c02029. Epub 2024 Jan 25. J Med Chem. 2024. PMID: 38270627
Correction to "MicroCycle: An Integrated and Automated Platform to Accelerate Drug Discovery".
Brocklehurst CE, Altmann E, André J, Bon C, Caya T, Davis H, Decoret O, Dunstan D, Ertl P, Ginsburg-Moraff C, Grob J, Gosling DJ, Lapointe G, Majumdar D, Marziale AN, Mues H, Palmieri M, Racine S, Robinson RI, Springer C, Tan K, Ulmer W, West L, Wyler R. Brocklehurst CE, et al. Among authors: lapointe g. J Med Chem. 2024 Mar 28;67(6):5111-5112. doi: 10.1021/acs.jmedchem.4c00452. Epub 2024 Mar 12. J Med Chem. 2024. PMID: 38471144 No abstract available.
Ligandability Assessment of IL-1β by Integrated Hit Identification Approaches.
Vulpetti A, Rondeau JM, Bellance MH, Blank J, Boesch R, Boettcher A, Bornancin F, Buhr S, Connor LE, Dumelin CE, Esser O, Hediger M, Hintermann S, Hommel U, Koch E, Lapointe G, Leder L, Lehmann S, Lehr P, Meier P, Muller L, Ostermeier D, Ramage P, Schiebel-Haddad S, Smith AB, Stojanovic A, Velcicky J, Yamamoto R, Hurth K. Vulpetti A, et al. Among authors: lapointe g. J Med Chem. 2024 May 23;67(10):8141-8160. doi: 10.1021/acs.jmedchem.4c00240. Epub 2024 May 10. J Med Chem. 2024. PMID: 38728572
Discovery and In Vivo Exploration of 1,3,4-Oxadiazole and α-Fluoroacrylate Containing IL-17 Inhibitors.
Velcicky J, Bauer MR, Schlapbach A, Lapointe G, Meyer A, Vögtle M, Blum E, Ngo E, Rolando C, Nimsgern P, Teixeira-Fouchard S, Lehmann H, Furet P, Berst F, Schümann J, Stringer R, Larger P, Schmid C, Prendergast CT, Riek S, Schmutz P, Lehmann S, Berghausen J, Scheufler C, Rondeau JM, Burkhart C, Knoepfel T, Gommermann N. Velcicky J, et al. Among authors: lapointe g. J Med Chem. 2024 Sep 26;67(18):16692-16711. doi: 10.1021/acs.jmedchem.4c01520. Epub 2024 Sep 14. J Med Chem. 2024. PMID: 39276085
187 results