1333331-66-0Relevant academic research and scientific papers
Diversity-oriented synthesis yields a novel lead for the treatment of malaria
Heidebrecht Jr., Richard W.,Mulrooney, Carol,Austin, Christopher P.,Barker Jr., Robert H.,Beaudoin, Jennifer A.,Cheng, Ken Chih-Chien,Comer, Eamon,Dandapani, Sivaraman,Dick, Justin,Duvall, Jeremy R.,Ekland, Eric H.,Fidock, David A.,Fitzgerald, Mark E.,Foley, Michael,Guha, Rajarshi,Hinkson, Paul,Kramer, Martin,Lukens, Amanda K.,Masi, Daniela,Marcaurelle, Lisa A.,Su, Xin-Zhuan,Thomas, Craig J.,Weiwer, Michel,Wiegand, Roger C.,Wirth, Dyann,Xia, Menghang,Yuan, Jing,Zhao, Jinghua,Palmer, Michelle,Munoz, Benito,Schreiber, Stuart
supporting information; scheme or table, p. 112 - 117 (2012/04/04)
Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synthesis (DOS) led to the initial hit. Structure-activity relationships guided the synthesis of compounds having improved potency and water solubility, yielding a subnanomolar inhibitor of parasite asexual blood-stage growth. Optimized compound 27 has an excellent off-target activity profile in erythrocyte lysis and HepG2 assays and is stable in human plasma. This compound is available via the molecular libraries probe production centers network (MLPCN) and is designated ML238.
MACROLACTAM COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA
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Page/Page column 88, (2012/11/06)
The present invention relates to a macrolactam compound, and methods for treating a subject with malaria using the macrolactam compound, represented by the following structural formula (l), wherein the values and preferred values of the variables are defined herein.
Diversity-oriented synthesis of 13- to 18-membered macrolactams via ring-closing metathesis
Dandapani, Sivaraman,Lowe, Jason T.,Comer, Eamon,Marcaurelle, Lisa A.
, p. 8042 - 8048 (2011/12/03)
An efficient build/couple/pair approach to diversity-oriented synthesis was employed to access several structurally complex macrolactams. In this paper, we describe the successful evaluation of ring-closing metathesis toward the systematic generation of skeletal diversity. By appropriately varying the nature and chain length of the alkenol fragment, a diverse collection of 13- to 18-membered macro-lactams were obtained.
