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Page 1
Structure-Activity Relationship of Heterocyclic P2Y14 Receptor Antagonists: Removal of the Zwitterionic Character with Piperidine Bioisosteres.
Jung YH, Salmaso V, Wen Z, Bennett JM, Phung NB, Lieberman DI, Gopinatth V, Randle JCR, Chen Z, Salvemini D, Karcz TP, Cook DN, Jacobson KA. Jung YH, et al. Among authors: randle jcr. J Med Chem. 2021 Apr 22;64(8):5099-5122. doi: 10.1021/acs.jmedchem.1c00164. Epub 2021 Mar 31. J Med Chem. 2021. PMID: 33787273 Free PMC article.
Bridged Piperidine Analogues of a High Affinity Naphthalene-Based P2Y14R Antagonist.
Wen Z, Salmaso V, Jung YH, Phung NB, Gopinatth V, Shah Q, Patterson AT, Randle JCR, Chen Z, Salvemini D, Lieberman DI, Whitehead GS, Karcz TP, Cook DN, Jacobson KA. Wen Z, et al. Among authors: randle jcr. J Med Chem. 2022 Feb 24;65(4):3434-3459. doi: 10.1021/acs.jmedchem.1c01964. Epub 2022 Feb 3. J Med Chem. 2022. PMID: 35113556 Free PMC article.
(S)-1-((S)-2-{[1-(4-amino-3-chloro-phenyl)-methanoyl]-amino}-3,3-dimethyl-butanoyl)-pyrrolidine-2-carboxylic acid ((2R,3S)-2-ethoxy-5-oxo-tetrahydro-furan-3-yl)-amide (VX-765), an orally available selective interleukin (IL)-converting enzyme/caspase-1 inhibitor, exhibits potent anti-inflammatory activities by inhibiting the release of IL-1beta and IL-18.
Wannamaker W, Davies R, Namchuk M, Pollard J, Ford P, Ku G, Decker C, Charifson P, Weber P, Germann UA, Kuida K, Randle JC. Wannamaker W, et al. J Pharmacol Exp Ther. 2007 May;321(2):509-16. doi: 10.1124/jpet.106.111344. Epub 2007 Feb 8. J Pharmacol Exp Ther. 2007. PMID: 17289835