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Novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 2. Mechanism of inhibition and structure-based improvement of pharmaceutical properties.
Liu G, Huth JR, Olejniczak ET, Mendoza R, DeVries P, Leitza S, Reilly EB, Okasinski GF, Fesik SW, von Geldern TW. Liu G, et al. Among authors: leitza s. J Med Chem. 2001 Apr 12;44(8):1202-10. doi: 10.1021/jm000503f. J Med Chem. 2001. PMID: 11312920
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intracellular adhesion molecule-1 interaction. 1. Identification of an additional binding pocket based on an anilino diaryl sulfide lead.
Liu G, Link JT, Pei Z, Reilly EB, Leitza S, Nguyen B, Marsh KC, Okasinski GF, von Geldern TW, Ormes M, Fowler K, Gallatin M. Liu G, et al. Among authors: leitza s. J Med Chem. 2000 Oct 19;43(21):4025-40. doi: 10.1021/jm0002782. J Med Chem. 2000. PMID: 11052808
Discovery of potent antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 3. Amide (C-ring) structure-activity relationship and improvement of overall properties of arylthio cinnamides.
Pei Z, Xin Z, Liu G, Li Y, Reilly EB, Lubbers NL, Huth JR, Link JT, von Geldern TW, Cox BF, Leitza S, Gao Y, Marsh KC, DeVries P, Okasinski GF. Pei Z, et al. Among authors: leitza s. J Med Chem. 2001 Aug 30;44(18):2913-20. doi: 10.1021/jm010059w. J Med Chem. 2001. PMID: 11520199
Discovery of novel p-arylthio cinnamides as antagonists of leukocyte function-associated antigen-1/intercellular adhesion molecule-1 interaction. 4. Structure-activity relationship of substituents on the benzene ring of the cinnamide.
Winn M, Reilly EB, Liu G, Huth JR, Jae HS, Freeman J, Pei Z, Xin Z, Lynch J, Kester J, von Geldern TW, Leitza S, DeVries P, Dickinson R, Mussatto D, Okasinski GF. Winn M, et al. Among authors: leitza s. J Med Chem. 2001 Dec 6;44(25):4393-403. doi: 10.1021/jm0103108. J Med Chem. 2001. PMID: 11728185
An evaluation of 3,4-methylenedioxy phenyl replacements in the aminopiperidine chromone class of MCHr1 antagonists.
Iyengar RR, Lynch JK, Mulhern MM, Judd AS, Freeman JC, Gao J, Souers AJ, Zhao G, Wodka D, Doug Falls H, Brodjian S, Dayton BD, Reilly RM, Swanson S, Su Z, Martin RL, Leitza ST, Houseman KA, Diaz G, Collins CA, Sham HL, Kym PR. Iyengar RR, et al. Among authors: leitza st. Bioorg Med Chem Lett. 2007 Feb 15;17(4):874-8. doi: 10.1016/j.bmcl.2006.11.065. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17234405
Identification of diamino chromone-2-carboxamides as MCHr1 antagonists with minimal hERG channel activity.
Judd AS, Souers AJ, Wodka D, Zhao G, Mulhern MM, Iyengar RR, Gao J, Lynch JK, Freeman JC, Falls HD, Brodjian S, Dayton BD, Reilly RM, Gintant G, Limberis JT, Mikhail A, Leitza ST, Houseman KA, Diaz G, Bush EN, Shapiro R, Knourek-Segel V, Hernandez LE, Marsh KC, Sham HL, Collins CA, Kym PR. Judd AS, et al. Among authors: leitza st. Bioorg Med Chem Lett. 2007 Apr 15;17(8):2365-71. doi: 10.1016/j.bmcl.2006.11.068. Epub 2006 Dec 1. Bioorg Med Chem Lett. 2007. PMID: 17350253