137434-47-0Relevant articles and documents
Discovery and structure-activity relationships of pyrrolone antimalarials
Murugesan, Dinakaran,Mital, Alka,Kaiser, Marcel,Shackleford, David M.,Morizzi, Julia,Katneni, Kasiram,Campbell, Michael,Hudson, Alan,Charman, Susan A.,Yeates, Clive,Gilbert, Ian H.
supporting information, p. 2975 - 2990 (2013/05/23)
In the pursuit of new antimalarial leads, a phenotypic screening of various commercially sourced compound libraries was undertaken by the World Health Organisation Programme for Research and Training in Tropical Diseases (WHO-TDR). We report here the detailed characterization of one of the hits from this process, TDR32750 (8a), which showed potent activity against Plasmodium falciparum K1 (EC50 ～ 9 nM), good selectivity (>2000-fold) compared to a mammalian cell line (L6), and significant activity against a rodent model of malaria when administered intraperitoneally. Structure-activity relationship studies have indicated ways in which the molecule could be optimized. This compound represents an exciting start point for a drug discovery program for the development of a novel antimalarial.
A New Synthesis of N-Substituted-2-alkyl(or aryl)quinazolin-4-amines by Amide Base-Mediated Cyclization of Carboximidamides Derived from 2-(Trifluoromethyl)benzenamine
Patterson, Steven E.,Janda, Lubomir,Strekowski, Lucjan
, p. 703 - 706 (2007/10/02)
A one-pot preparation carboximidamides (amidines) 11-14 involves treatment of amides 2-5 with phosphorus pentachloride followed by the treatment of the resultant crude imidoyl chlorides 7-10 with ammonia.Amidines 11-14 are cyclized to quinazolines 20-26 i
