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Microwave assisted synthesis, docking and antimalarial evaluation of hybrid PABA‐substituted 1,3,5‐triazine derivatives
Author(s) -
Adhikari Nayana,
Kashyap Ankita,
Shakya Anshul,
Ghosh Surajit Kumar,
Bhattacharyya Dibya Ranjan,
Bhat Hans Raj,
Singh Udaya Pratap
Publication year - 2020
Publication title -
journal of heterocyclic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.321
H-Index - 59
eISSN - 1943-5193
pISSN - 0022-152X
DOI - 10.1002/jhet.3955
Subject(s) - chemistry , plasmodium falciparum , triazine , chloroquine , combinatorial chemistry , docking (animal) , 1,3,5 triazine , stereochemistry , in vitro , organic chemistry , malaria , biochemistry , medicine , nursing , immunology , biology
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 IC 50 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.