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Page 1
Discovery of sulfone containing metallo-β-lactamase inhibitors with reduced bacterial cell efflux and histamine release issues.
Bennett F, Huang Y, Dong S, Jiang J, Hunter D, Zhao Z, Gu X, Scott JD, Tang H, Yang D, Xiao L, Scapin G, Fischmann T, Mirza A, Dayananth P, Painter RE, Villafania A, Garlisi CG, Zhang R, Mayhood TW, Si Q, Li N, Amin RP, Chen F, Bhatt B, Regan CP, Regan H, Lin X, Wu J, Leithead A, Young K, Pasternak A. Bennett F, et al. Among authors: amin rp. Bioorg Med Chem Lett. 2024 Oct 11;114:129989. doi: 10.1016/j.bmcl.2024.129989. Online ahead of print. Bioorg Med Chem Lett. 2024. PMID: 39396683
Comprehensive genotoxicity and carcinogenicity assessment of molnupiravir.
Escobar PA, Sobol Z, Miller RR, Ferry-Martin S, Stermer A, Jacob B, Muniappa N, Sanchez R, Blanchard KT, Galijatovic-Idrizbegovic A, Amin RP, Troth SP. Escobar PA, et al. Among authors: amin rp. Toxicol Sci. 2024 Sep 20:kfae112. doi: 10.1093/toxsci/kfae112. Online ahead of print. Toxicol Sci. 2024. PMID: 39302733
Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration.
Dong S, Zhao Z, Tang H, Li G, Pan J, Gu X, Jiang J, Xiao L, Scapin G, Hunter DN, Yang D, Huang Y, Bennett F, Yang SW, Mandal M, Tang H, Su J, Tudge C, deJesus RK, Ding FX, Lombardo M, Hicks JD, Fischmann T, Mirza A, Dayananth P, Painter RE, Villafania A, Garlisi CG, Zhang R, Mayhood TW, Si Q, Li N, Amin RP, Bhatt B, Chen F, Regan CP, Regan H, Lin X, Wu J, Leithead A, Pollack SR, Scott JD, Nargund RP, Therien AG, Black T, Young K, Pasternak A. Dong S, et al. Among authors: amin rp. J Med Chem. 2024 Mar 14;67(5):3400-3418. doi: 10.1021/acs.jmedchem.3c01614. Epub 2024 Feb 22. J Med Chem. 2024. PMID: 38387069
Lead Optimization to Advance Protease-Activated Receptor-1 Antagonists in Early Discovery.
Mandal M, Madeira M, Amin RP, Buevich AV, Cheng A, Labroli M, Liu X, Acton J, Pio B, Basso A, Chobanian H, Dong G, Dropinski J, Guo Y, Guo Z, Kurowski S, Korfmacher W, Lee S, Meng D, Ondeyka D, Yang Z, Zhang R, Wei H, Wu Z, Zhang F, Wollenberg G, Biftu T, Greenlee WJ, Chintala M, Maletic M, Zhu Z. Mandal M, et al. Among authors: amin rp. J Med Chem. 2022 Apr 14;65(7):5575-5592. doi: 10.1021/acs.jmedchem.1c02048. Epub 2022 Mar 29. J Med Chem. 2022. PMID: 35349275
Development of ProTx-II Analogues as Highly Selective Peptide Blockers of Nav1.7 for the Treatment of Pain.
Adams GL, Pall PS, Grauer SM, Zhou X, Ballard JE, Vavrek M, Kraus RL, Morissette P, Li N, Colarusso S, Bianchi E, Palani A, Klein R, John CT, Wang D, Tudor M, Nolting AF, Biba M, Nowak T, Makarov AA, Reibarkh M, Buevich AV, Zhong W, Regalado EL, Wang X, Gao Q, Shahripour A, Zhu Y, de Simone D, Frattarelli T, Pasquini NM, Magotti P, Iaccarino R, Li Y, Solly K, Lee KJ, Wang W, Chen F, Zeng H, Wang J, Regan H, Amin RP, Regan CP, Burgey CS, Henze DA, Sun C, Tellers DM. Adams GL, et al. Among authors: amin rp. J Med Chem. 2022 Jan 13;65(1):485-496. doi: 10.1021/acs.jmedchem.1c01570. Epub 2021 Dec 21. J Med Chem. 2022. PMID: 34931831
Guiding Chemically Synthesized Peptide Drug Lead Optimization by Derisking Mast Cell Degranulation-Related Toxicities of a NaV1.7 Peptide Inhibitor.
Morissette P, Li N, Ballard JE, Vavrek M, Adams GL, Regan C, Regan H, Lee KJ, Wang W, Burton A, Chen F, Gerenser P, Li Y, Kraus RL, Tellers D, Palani A, Zhu Y, Sun C, Bianchi E, Colarusso S, De Simone D, Frattarelli T, Pasquini NM, Amin RP. Morissette P, et al. Among authors: amin rp. Toxicol Sci. 2022 Jan 24;185(2):170-183. doi: 10.1093/toxsci/kfab138. Toxicol Sci. 2022. PMID: 34897513
A Series of Novel, Highly Potent, and Orally Bioavailable Next-Generation Tricyclic Peptide PCSK9 Inhibitors.
Tucker TJ, Embrey MW, Alleyne C, Amin RP, Bass A, Bhatt B, Bianchi E, Branca D, Bueters T, Buist N, Ha SN, Hafey M, He H, Higgins J, Johns DG, Kerekes AD, Koeplinger KA, Kuethe JT, Li N, Murphy B, Orth P, Salowe S, Shahripour A, Tracy R, Wang W, Wu C, Xiong Y, Zokian HJ, Wood HB, Walji A. Tucker TJ, et al. Among authors: amin rp. J Med Chem. 2021 Nov 25;64(22):16770-16800. doi: 10.1021/acs.jmedchem.1c01599. Epub 2021 Oct 27. J Med Chem. 2021. PMID: 34704436
Invention of MK-8262, a Cholesteryl Ester Transfer Protein (CETP) Inhibitor Backup to Anacetrapib with Best-in-Class Properties.
Vachal P, Duffy JL, Campeau LC, Amin RP, Mitra K, Murphy BA, Shao PP, Sinclair PJ, Ye F, Katipally R, Lu Z, Ondeyka D, Chen YH, Zhao K, Sun W, Tyagarajan S, Bao J, Wang SP, Cote J, Lipardi C, Metzger D, Leung D, Hartmann G, Wollenberg GK, Liu J, Tan L, Xu Y, Chen Q, Liu G, Blaustein RO, Johns DG. Vachal P, et al. Among authors: amin rp. J Med Chem. 2021 Sep 23;64(18):13215-13258. doi: 10.1021/acs.jmedchem.1c00959. Epub 2021 Aug 10. J Med Chem. 2021. PMID: 34375108
26 results