Novel Quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione Derivatives Against Chloroquine-resistant Plasmodium falciparum was written by Rogerio, Kamilla Rodrigues;Graebin, Cedric Stephan;Pinto Domingues, Luiza Helena;Oliveira, Luana Santos;Fernandes da Silva, Vitoria de Souza;Daniel-Ribeiro, Claudio Tadeu;Carvalho, Leonardo J. M.;Boechat, Nubia. And the article was included in Current Topics in Medicinal Chemistry in 2020.Reference of 638-07-3 The following contents are mentioned in the article:
In this work DHPMs were combined with the quinoline nucleus to obtain new quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione compounds I (R = H, 4-OMe, 4-Cl, etc.; n = 1, 2) with improved antiplasmodial activity as well as decreased cytotoxicity. Nineteen quinolinyl-pyrrolo[3,4-d]pyrimidine-2,5-dione derivatives connected by a linker group to quinoline ring moieties with different substituents were synthesized and assayed against chloroquine-resistant Plasmodium falciparum, along with the reference drug chloroquine. The derivative without substituents on the aromatic ring I (R = H; n = 1) and the compound I (R = 4-Cl; n = 1) provided the best results, with IC50 = 1.15μM and 1.5μM, resp. Compared to the parent drugs, these compounds presented marked decreases in cytotoxicity, with MDL50 values over 1,000μM and selectivity indexes of >869.5 and >666.6, resp. This study involved multiple reactions and reactants, such as Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3Reference of 638-07-3).
Ethyl 4-chloro-3-oxobutanoate (cas: 638-07-3) belongs to organic chlorides. Organic chlorides are compounds containing a carbon-chlorine bond, which are widely used in the oil field as a wax dissolver. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Reference of 638-07-3
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics