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Page 1
Target-Based Identification and Optimization of 5-Indazol-5-yl Pyridones as Toll-like Receptor 7 and 8 Antagonists Using a Biochemical TLR8 Antagonist Competition Assay.
Knoepfel T, Nimsgern P, Jacquier S, Bourrel M, Vangrevelinghe E, Glatthar R, Behnke D, Alper PB, Michellys PY, Deane J, Junt T, Zipfel G, Limonta S, Hawtin S, Andre C, Boulay T, Loetscher P, Faller M, Blank J, Feifel R, Betschart C. Knoepfel T, et al. Among authors: alper pb. J Med Chem. 2020 Aug 13;63(15):8276-8295. doi: 10.1021/acs.jmedchem.0c00130. Epub 2020 Jul 30. J Med Chem. 2020. PMID: 32786235
Synthesis and evaluation of arylaminoethyl amides as noncovalent inhibitors of cathepsin S. Part 3: heterocyclic P3.
Tully DC, Liu H, Alper PB, Chatterjee AK, Epple R, Roberts MJ, Williams JA, Nguyen KT, Woodmansee DH, Tumanut C, Li J, Spraggon G, Chang J, Tuntland T, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: alper pb. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1975-80. doi: 10.1016/j.bmcl.2005.12.095. Epub 2006 Jan 30. Bioorg Med Chem Lett. 2006. PMID: 16446091
Synthesis and SAR of arylaminoethyl amides as noncovalent inhibitors of cathepsin S: P3 cyclic ethers.
Tully DC, Liu H, Chatterjee AK, Alper PB, Epple R, Williams JA, Roberts MJ, Woodmansee DH, Masick BT, Tumanut C, Li J, Spraggon G, Hornsby M, Chang J, Tuntland T, Hollenbeck T, Gordon P, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: alper pb. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5112-7. doi: 10.1016/j.bmcl.2006.07.033. Epub 2006 Jul 28. Bioorg Med Chem Lett. 2006. PMID: 16876402
Arylaminoethyl carbamates as a novel series of potent and selective cathepsin S inhibitors.
Tully DC, Liu H, Chatterjee AK, Alper PB, Williams JA, Roberts MJ, Mutnick D, Woodmansee DH, Hollenbeck T, Gordon P, Chang J, Tuntland T, Tumanut C, Li J, Harris JL, Karanewsky DS. Tully DC, et al. Among authors: alper pb. Bioorg Med Chem Lett. 2006 Oct 1;16(19):5107-11. doi: 10.1016/j.bmcl.2006.07.032. Epub 2006 Jul 28. Bioorg Med Chem Lett. 2006. PMID: 16876407
Imidazolopiperazines: lead optimization of the second-generation antimalarial agents.
Nagle A, Wu T, Kuhen K, Gagaring K, Borboa R, Francek C, Chen Z, Plouffe D, Lin X, Caldwell C, Ek J, Skolnik S, Liu F, Wang J, Chang J, Li C, Liu B, Hollenbeck T, Tuntland T, Isbell J, Chuan T, Alper PB, Fischli C, Brun R, Lakshminarayana SB, Rottmann M, Diagana TT, Winzeler EA, Glynne R, Tully DC, Chatterjee AK. Nagle A, et al. Among authors: alper pb. J Med Chem. 2012 May 10;55(9):4244-73. doi: 10.1021/jm300041e. Epub 2012 Apr 23. J Med Chem. 2012. PMID: 22524250 Free PMC article.
Discovery of structurally novel, potent and orally efficacious GPR119 agonists.
Alper P, Azimioara M, Cow C, Mutnick D, Nikulin V, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessel T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Alper P, et al. Bioorg Med Chem Lett. 2014 May 15;24(10):2383-7. doi: 10.1016/j.bmcl.2014.03.023. Epub 2014 Mar 27. Bioorg Med Chem Lett. 2014. PMID: 24751443
Novel tricyclic pyrazolopyrimidines as potent and selective GPR119 agonists.
Azimioara M, Alper P, Cow C, Mutnick D, Nikulin V, Lelais G, Mecom J, McNeill M, Michellys PY, Wang Z, Reding E, Paliotti M, Li J, Bao D, Zoll J, Kim Y, Zimmerman M, Groessl T, Tuntland T, Joseph SB, McNamara P, Seidel HM, Epple R. Azimioara M, et al. Bioorg Med Chem Lett. 2014 Dec 1;24(23):5478-83. doi: 10.1016/j.bmcl.2014.10.010. Epub 2014 Oct 13. Bioorg Med Chem Lett. 2014. PMID: 25455488
Discovery of Tropifexor (LJN452), a Highly Potent Non-bile Acid FXR Agonist for the Treatment of Cholestatic Liver Diseases and Nonalcoholic Steatohepatitis (NASH).
Tully DC, Rucker PV, Chianelli D, Williams J, Vidal A, Alper PB, Mutnick D, Bursulaya B, Schmeits J, Wu X, Bao D, Zoll J, Kim Y, Groessl T, McNamara P, Seidel HM, Molteni V, Liu B, Phimister A, Joseph SB, Laffitte B. Tully DC, et al. Among authors: alper pb. J Med Chem. 2017 Dec 28;60(24):9960-9973. doi: 10.1021/acs.jmedchem.7b00907. Epub 2017 Dec 8. J Med Chem. 2017. PMID: 29148806
19 results