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Page 1
Inhibition of MMP-1 and MMP-13 with phosphinic acids that exploit binding in the S2 pocket.
Reiter LA, Rizzi JP, Pandit J, Lasut MJ, McGahee SM, Parikh VD, Blake JF, Danley DE, Laird ER, Lopez-Anaya A, Lopresti-Morrow LL, Mansour MN, Martinelli GJ, Mitchell PG, Owens BS, Pauly TA, Reeves LM, Schulte GK, Yocum SA. Reiter LA, et al. Among authors: parikh vd. Bioorg Med Chem Lett. 1999 Jan 18;9(2):127-32. doi: 10.1016/s0960-894x(98)00729-x. Bioorg Med Chem Lett. 1999. PMID: 10021913
Discovery of Brain-Penetrant, Irreversible Kynurenine Aminotransferase II Inhibitors for Schizophrenia.
Dounay AB, Anderson M, Bechle BM, Campbell BM, Claffey MM, Evdokimov A, Evrard E, Fonseca KR, Gan X, Ghosh S, Hayward MM, Horner W, Kim JY, McAllister LA, Pandit J, Paradis V, Parikh VD, Reese MR, Rong S, Salafia MA, Schuyten K, Strick CA, Tuttle JB, Valentine J, Wang H, Zawadzke LE, Verhoest PR. Dounay AB, et al. Among authors: parikh vd. ACS Med Chem Lett. 2012 Jan 25;3(3):187-92. doi: 10.1021/ml200204m. eCollection 2012 Mar 8. ACS Med Chem Lett. 2012. PMID: 24900455 Free PMC article.
Structure-Based Design of Irreversible Human KAT II Inhibitors: Discovery of New Potency-Enhancing Interactions.
Tuttle JB, Anderson M, Bechle BM, Campbell BM, Chang C, Dounay AB, Evrard E, Fonseca KR, Gan X, Ghosh S, Horner W, James LC, Kim JY, McAllister LA, Pandit J, Parikh VD, Rago BJ, Salafia MA, Strick CA, Zawadzke LE, Verhoest PR. Tuttle JB, et al. Among authors: parikh vd. ACS Med Chem Lett. 2012 Oct 24;4(1):37-40. doi: 10.1021/ml300237v. eCollection 2013 Jan 10. ACS Med Chem Lett. 2012. PMID: 24900560 Free PMC article.
Design and discovery of a selective small molecule κ opioid antagonist (2-methyl-N-((2'-(pyrrolidin-1-ylsulfonyl)biphenyl-4-yl)methyl)propan-1-amine, PF-4455242).
Verhoest PR, Basak AS, Parikh V, Hayward M, Kauffman GW, Paradis V, McHardy SF, McLean S, Grimwood S, Schmidt AW, Vanase-Frawley M, Freeman J, Van Deusen J, Cox L, Wong D, Liras S. Verhoest PR, et al. J Med Chem. 2011 Aug 25;54(16):5868-77. doi: 10.1021/jm2006035. Epub 2011 Jul 22. J Med Chem. 2011. PMID: 21744827
Discovery and Characterization of (R)-6-Neopentyl-2-(pyridin-2-ylmethoxy)-6,7-dihydropyrimido[2,1-c][1,4]oxazin-4(9H)-one (PF-06462894), an Alkyne-Lacking Metabotropic Glutamate Receptor 5 Negative Allosteric Modulator Profiled in both Rat and Nonhuman Primates.
Stepan AF, Claffey MM, Reese MR, Balan G, Barreiro G, Barricklow J, Bohanon MJ, Boscoe BP, Cappon GD, Chenard LK, Cianfrogna J, Chen L, Coffman KJ, Drozda SE, Dunetz JR, Ghosh S, Hou X, Houle C, Karki K, Lazzaro JT, Mancuso JY, Marcek JM, Miller EL, Moen MA, O'Neil S, Sakurada I, Skaddan M, Parikh V, Smith DL, Trapa P, Tuttle JB, Verhoest PR, Walker DP, Won A, Wright AS, Whritenour J, Zasadny K, Zaleska MM, Zhang L, Shaffer CL. Stepan AF, et al. J Med Chem. 2017 Sep 28;60(18):7764-7780. doi: 10.1021/acs.jmedchem.7b00604. Epub 2017 Sep 13. J Med Chem. 2017. PMID: 28817277
Metabolism and clinical pharmacokinetics of 2-methyl-n-(2'-(pyrrolidinyl-1-ylsulfonyl)-n-[1,1'-biphenyl]-4-yl)propran-1-amine: insights into monoamine oxidase- and CYP-mediated disposition by integration of in vitro ADME tools.
Sawant Basak A, Byon W, Tseng-Lovering E, Funk C, Wood L, Lin C, Delnomdedieu M, Verhoest P, Parikh V, Cox LM, Miller E, Gao H, Obach RS. Sawant Basak A, et al. Xenobiotica. 2014 May;44(5):438-54. doi: 10.3109/00498254.2013.850552. Epub 2013 Dec 4. Xenobiotica. 2014. PMID: 24304147
11 results