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High-Throughput Crystallography Reveals Boron-Containing Inhibitors of a Penicillin-Binding Protein with Di- and Tricovalent Binding Modes.
Newman H, Krajnc A, Bellini D, Eyermann CJ, Boyle GA, Paterson NG, McAuley KE, Lesniak R, Gangar M, von Delft F, Brem J, Chibale K, Schofield CJ, Dowson CG. Newman H, et al. Among authors: eyermann cj. J Med Chem. 2021 Aug 12;64(15):11379-11394. doi: 10.1021/acs.jmedchem.1c00717. Epub 2021 Jul 31. J Med Chem. 2021. PMID: 34337941 Free PMC article.
Optimization of physicochemical properties and safety profile of novel bacterial topoisomerase type II inhibitors (NBTIs) with activity against Pseudomonas aeruginosa.
Reck F, Ehmann DE, Dougherty TJ, Newman JV, Hopkins S, Stone G, Agrawal N, Ciaccio P, McNulty J, Barthlow H, O'Donnell J, Goteti K, Breen J, Comita-Prevoir J, Cornebise M, Cronin M, Eyermann CJ, Geng B, Carr GR, Pandarinathan L, Tang X, Cottone A, Zhao L, Bezdenejnih-Snyder N. Reck F, et al. Among authors: eyermann cj. Bioorg Med Chem. 2014 Oct 1;22(19):5392-409. doi: 10.1016/j.bmc.2014.07.040. Epub 2014 Aug 4. Bioorg Med Chem. 2014. PMID: 25155913
X-ray crystal structures of Escherichia coli RNA polymerase with switch region binding inhibitors enable rational design of squaramides with an improved fraction unbound to human plasma protein.
Molodtsov V, Fleming PR, Eyermann CJ, Ferguson AD, Foulk MA, McKinney DC, Masse CE, Buurman ET, Murakami KS. Molodtsov V, et al. Among authors: eyermann cj. J Med Chem. 2015 Apr 9;58(7):3156-71. doi: 10.1021/acs.jmedchem.5b00050. Epub 2015 Mar 23. J Med Chem. 2015. PMID: 25798859 Free PMC article.
Negishi cross-coupling enabled synthesis of novel NAD(+)-dependent DNA ligase inhibitors and SAR development.
Murphy-Benenato KE, Gingipalli L, Boriack-Sjodin PA, Martinez-Botella G, Carcanague D, Eyermann CJ, Gowravaram M, Harang J, Hale MR, Ioannidis G, Jahic H, Johnstone M, Kutschke A, Laganas VA, Loch JT 3rd, Miller MD, Oguto H, Patel SJ. Murphy-Benenato KE, et al. Among authors: eyermann cj. Bioorg Med Chem Lett. 2015 Nov 15;25(22):5172-7. doi: 10.1016/j.bmcl.2015.09.075. Epub 2015 Oct 14. Bioorg Med Chem Lett. 2015. PMID: 26463129
Plasmodial Kinase Inhibitors: License to Cure?
Cabrera DG, Horatscheck A, Wilson CR, Basarab G, Eyermann CJ, Chibale K. Cabrera DG, et al. Among authors: eyermann cj. J Med Chem. 2018 Sep 27;61(18):8061-8077. doi: 10.1021/acs.jmedchem.8b00329. Epub 2018 Jun 4. J Med Chem. 2018. PMID: 29771541 Free PMC article.
Identification, Characterization, and Optimization of 2,8-Disubstituted-1,5-naphthyridines as Novel Plasmodium falciparum Phosphatidylinositol-4-kinase Inhibitors with in Vivo Efficacy in a Humanized Mouse Model of Malaria.
Kandepedu N, Gonzàlez Cabrera D, Eedubilli S, Taylor D, Brunschwig C, Gibhard L, Njoroge M, Lawrence N, Paquet T, Eyermann CJ, Spangenberg T, Basarab GS, Street LJ, Chibale K. Kandepedu N, et al. Among authors: eyermann cj. J Med Chem. 2018 Jul 12;61(13):5692-5703. doi: 10.1021/acs.jmedchem.8b00648. Epub 2018 Jun 27. J Med Chem. 2018. PMID: 29889526
Antimalarial Lead-Optimization Studies on a 2,6-Imidazopyridine Series within a Constrained Chemical Space To Circumvent Atypical Dose-Response Curves against Multidrug Resistant Parasite Strains.
Le Manach C, Paquet T, Wicht K, Nchinda AT, Brunschwig C, Njoroge M, Gibhard L, Taylor D, Lawrence N, Wittlin S, Eyermann CJ, Basarab GS, Duffy J, Fish PV, Street LJ, Chibale K. Le Manach C, et al. Among authors: eyermann cj. J Med Chem. 2018 Oct 25;61(20):9371-9385. doi: 10.1021/acs.jmedchem.8b01333. Epub 2018 Oct 16. J Med Chem. 2018. PMID: 30256636
Lerisetron Analogues with Antimalarial Properties: Synthesis, Structure-Activity Relationship Studies, and Biological Assessment.
Mueller R, Reddy V, Nchinda AT, Mebrahtu F, Taylor D, Lawrence N, Tanner L, Barnabe M, Eyermann CJ, Zou B, Kondreddi RR, Lakshminarayana SB, Rottmann M, Street LJ, Chibale K. Mueller R, et al. Among authors: eyermann cj. ACS Omega. 2020 Mar 17;5(12):6967-6982. doi: 10.1021/acsomega.0c00327. eCollection 2020 Mar 31. ACS Omega. 2020. PMID: 32258933 Free PMC article.
42 results