1403478-75-0Relevant academic research and scientific papers
Diversity-oriented synthesis-facilitated medicinal chemistry: Toward the development of novel antimalarial agents
Comer, Eamon,Beaudoin, Jennifer A.,Kato, Nobutaka,Fitzgerald, Mark E.,Heidebrecht, Richard W.,Lee, Maurice Dupont,Masi, Daniela,Mercier, Marion,Mulrooney, Carol,Muncipinto, Giovanni,Rowley, Ann,Crespo-Llado, Keila,Serrano, Adelfa E.,Lukens, Amanda K.,Wiegand, Roger C.,Wirth, Dyann F.,Palmer, Michelle A.,Foley, Michael A.,Munoz, Benito,Scherer, Christina A.,Duvall, Jeremy R.,Schreiber, Stuart L.
, p. 8496 - 8502 (2014/12/11)
Here, we describe medicinal chemistry that was accelerated by a diversity-oriented synthesis (DOS) pathway, and in vivo studies of our previously reported macrocyclic antimalarial agent that derived from the synthetic pathway. Structure-activity relationships that focused on both appendage and skeletal features yielded a nanomolar inhibitor of P. falciparum asexual blood-stage growth with improved solubility and microsomal stability and reduced hERG binding. The build/couple/pair (B/C/P) synthetic strategy, used in the preparation of the original screening library, facilitated medicinal chemistry optimization of the antimalarial lead.
MACROLACTAM COMPOUNDS AND METHODS FOR THE TREATMENT OF MALARIA
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Page/Page column 98, (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.
