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Page 1
Identification and Profiling of a Novel Diazaspiro[3.4]octane Chemical Series Active against Multiple Stages of the Human Malaria Parasite Plasmodium falciparum and Optimization Efforts.
Le Manach C, Dam J, Woodland JG, Kaur G, Khonde LP, Brunschwig C, Njoroge M, Wicht KJ, Horatscheck A, Paquet T, Boyle GA, Gibhard L, Taylor D, Lawrence N, Yeo T, Mok S, Eastman RT, Dorjsuren D, Talley DC, Guo H, Simeonov A, Reader J, van der Watt M, Erlank E, Venter N, Zawada JW, Aswat A, Nardini L, Coetzer TL, Lauterbach SB, Bezuidenhout BC, Theron A, Mancama D, Koekemoer LL, Birkholtz LM, Wittlin S, Delves M, Ottilie S, Winzeler EA, von Geldern TW, Smith D, Fidock DA, Street LJ, Basarab GS, Duffy J, Chibale K. Le Manach C, et al. Among authors: von geldern tw. J Med Chem. 2021 Feb 25;64(4):2291-2309. doi: 10.1021/acs.jmedchem.1c00034. Epub 2021 Feb 12. J Med Chem. 2021. PMID: 33573376
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: von geldern tw. J Med Chem. 2000 Oct 19;43(21):4025-40. doi: 10.1021/jm0002782. J Med Chem. 2000. PMID: 11052808
Liver-selective glucocorticoid antagonists: a novel treatment for type 2 diabetes.
von Geldern TW, Tu N, Kym PR, Link JT, Jae HS, Lai C, Apelqvist T, Rhonnstad P, Hagberg L, Koehler K, Grynfarb M, Goos-Nilsson A, Sandberg J, Osterlund M, Barkhem T, Höglund M, Wang J, Fung S, Wilcox D, Nguyen P, Jakob C, Hutchins C, Färnegårdh M, Kauppi B, Ohman L, Jacobson PB. von Geldern TW, et al. J Med Chem. 2004 Aug 12;47(17):4213-30. doi: 10.1021/jm0400045. J Med Chem. 2004. PMID: 15293993
Discovery of 2-[4-{{2-(2S,5R)-2-cyano-5-ethynyl-1-pyrrolidinyl]-2-oxoethyl]amino]- 4-methyl-1-piperidinyl]-4-pyridinecarboxylic acid (ABT-279): a very potent, selective, effective, and well-tolerated inhibitor of dipeptidyl peptidase-IV, useful for the treatment of diabetes.
Madar DJ, Kopecka H, Pireh D, Yong H, Pei Z, Li X, Wiedeman PE, Djuric SW, Von Geldern TW, Fickes MG, Bhagavatula L, McDermott T, Wittenberger S, Richards SJ, Longenecker KL, Stewart KD, Lubben TH, Ballaron SJ, Stashko MA, Long MA, Wells H, Zinker BA, Mika AK, Beno DW, Kempf-Grote AJ, Polakowski J, Segreti J, Reinhart GA, Fryer RM, Sham HL, Trevillyan JM. Madar DJ, et al. Among authors: von geldern tw. J Med Chem. 2006 Oct 19;49(21):6416-20. doi: 10.1021/jm060777o. J Med Chem. 2006. PMID: 17034148
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