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Discovery and Optimization of Novel SUCNR1 Inhibitors: Design of Zwitterionic Derivatives with a Salt Bridge for the Improvement of Oral Exposure.
Velcicky J, Wilcken R, Cotesta S, Janser P, Schlapbach A, Wagner T, Piechon P, Villard F, Bouhelal R, Piller F, Harlfinger S, Stringer R, Fehlmann D, Kaupmann K, Littlewood-Evans A, Haffke M, Gommermann N. Velcicky J, et al. Among authors: piechon p. J Med Chem. 2020 Sep 10;63(17):9856-9875. doi: 10.1021/acs.jmedchem.0c01020. Epub 2020 Aug 28. J Med Chem. 2020. PMID: 32856916
Discovery and Optimization of DNA Gyrase and Topoisomerase IV Inhibitors with Potent Activity against Fluoroquinolone-Resistant Gram-Positive Bacteria.
Lapointe G, Skepper CK, Holder LM, Armstrong D, Bellamacina C, Blais J, Bussiere D, Bian J, Cepura C, Chan H, Dean CR, De Pascale G, Dhumale B, Fisher LM, Fulsunder M, Kantariya B, Kim J, King S, Kossy L, Kulkarni U, Lakshman J, Leeds JA, Ling X, Lvov A, Ma S, Malekar S, McKenney D, Mergo W, Metzger L, Mhaske K, Moser HE, Mostafavi M, Namballa S, Noeske J, Osborne C, Patel A, Patel D, Patel T, Piechon P, Polyakov V, Prajapati K, Prosen KR, Reck F, Richie DL, Sanderson MR, Satasia S, Savani B, Selvarajah J, Sethuraman V, Shu W, Tashiro K, Thompson KV, Vaarla K, Vala L, Veselkov DA, Vo J, Vora B, Wagner T, Wedel L, Williams SL, Yendluri S, Yue Q, Yifru A, Zhang Y, Rivkin A. Lapointe G, et al. Among authors: piechon p. J Med Chem. 2021 May 13;64(9):6329-6357. doi: 10.1021/acs.jmedchem.1c00375. Epub 2021 Apr 30. J Med Chem. 2021. PMID: 33929852
Application of Transition-Metal Catalysis, Biocatalysis, and Flow Chemistry as State-of-the-Art Technologies in the Synthesis of LCZ696.
Gu X, Zhao J, Chen L, Li Y, Yu B, Tian X, Min Z, Xu S, Gu H, Sun J, Lu X, Chang M, Wang X, Zhao L, Ye S, Yang H, Tian Y, Gao F, Gai Y, Jia G, Wu J, Wang Y, Zhang J, Zhang X, Liu W, Gu X, Luo X, Dong H, Wang H, Schenkel B, Venturoni F, Filipponi P, Guelat B, Allmendinger T, Wietfeld B, Hoehn P, Kovacic N, Hermann L, Schlama T, Ruch T, Derrien N, Piechon P, Kleinbeck F. Gu X, et al. Among authors: piechon p. J Org Chem. 2020 Jun 5;85(11):6844-6853. doi: 10.1021/acs.joc.0c00473. Epub 2020 May 15. J Org Chem. 2020. PMID: 32412751
Bioinspired co-crystals of Imatinib providing enhanced kinetic solubility.
Reggane M, Wiest J, Saedtler M, Harlacher C, Gutmann M, Zottnick SH, Piechon P, Dix I, Müller-Buschbaum K, Holzgrabe U, Meinel L, Galli B. Reggane M, et al. Among authors: piechon p. Eur J Pharm Biopharm. 2018 Jul;128:290-299. doi: 10.1016/j.ejpb.2018.05.012. Epub 2018 May 4. Eur J Pharm Biopharm. 2018. PMID: 29733951
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