37019-16-2Relevant articles and documents
Microwave assisted synthesis, docking and antimalarial evaluation of hybrid PABA-substituted 1,3,5-triazine derivatives
Adhikari, Nayana,Kashyap, Ankita,Shakya, Anshul,Ghosh, Surajit Kumar,Bhattacharyya, Dibya Ranjan,Bhat, Hans Raj,Singh, Udaya Pratap
, p. 2389 - 2399 (2020)
A series of novel PABA-substituted 1,3,5-triazine derivatives were developed via microwave assisted synthesis and subsequently tested for antimalarial activity against chloroquine sensitive 3D7 strain of Plasmodium falciparum using chloroquine as standard. Antimalarial screening result showed that synthesized compounds exhibited IC50 in the range of 4.46 to 79.72 μg mL?1. Among the tested compounds, 4c and 4f showed significant antimalarial activity with low binding energies (BE) -172.32 and 160.41 kcal mol?1 via interacting with Arg122 through the involvement of COOH of the phenyl linked to 1,3,5-triazine. In conclusion, these core scaffolds can be used for future antimalarial drug development.
Novel functionalized melamine-based nitroheterocycles: Synthesis and activity against trypanosomatid parasites
Baliani, Alessandro,Peal, Valerie,Gros, Ludovic,Brun, Reto,Kaiser, Marcel,Barrett, Michael P.,Gilbert, Ian H.
supporting information; experimental part, p. 1154 - 1166 (2009/05/30)
Human African trypanosomiasis (HAT), caused by the protozoan parasite Trypanosoma brucei spp., is a major health problem in sub-Saharan Africa. New drugs are urgently required for the disease. Selective uptake of toxic compounds into trypanosomes has been achieved by exploiting plasma membrane transporters. For example, the P2 aminopurine transporter, along with other transporters, selectively concentrates melamine and benzamidine moieties into trypanosomes. We have previously reported the use of the melamine motif to selectively target nitrofuran to the trypanosome. In this paper we report the further investigation of the structure activity relationships and the effect of the introduction of different functionalized substituents onto the melamine unit. Most of the compounds tested in vitro for their trypanocidal activity showed activities in the submicromolar range against T. b. rhodesiense. The Royal Society of Chemistry 2009.