Anderson, Marc O.; Sherrill, John; Madrid, Peter B.; Liou, Ally P.; Weisman, Jennifer L.; DeRisi, Joseph L.; Guy, R. Kiplin published the artcile< Parallel synthesis of 9-aminoacridines and their evaluation against chloroquine-resistant Plasmodium falciparum>, SDS of cas: 22717-55-1, the main research area is synthesis antimalarial aminoacridine derivative.
A parallel synthetic strategy to the 9-aminoacridine scaffold of the classical antimalarial drug quinacrine is presented. The method features a new route to 9-chloroacridines that utilizes triflates of salicylic acid derivatives, which are com. available in a variety of substitution patterns. The route allows ready variation of the 2 diversity elements present in this class of mols.: the tricyclic aromatic heterocyclic core, and the disubstituted diamine side-chain. In this study, a library of 175 compounds was designed, although only 93 of the final products had purities acceptable for screening. Impurity was generally due to incomplete removal of 9-acridones, a degradation product of the 9-chloroacridine synthetic intermediates. The library was screened against two strains of P. falciparum, including a model of the drug-resistant parasite, and 6 novel compounds were found to have IC50 values in the low nanomolar range.
Bioorganic & Medicinal Chemistry published new progress about Antimalarials. 22717-55-1 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H7ClO3, SDS of cas: 22717-55-1.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics