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Synthesis of various fused heterocyclic rings from thiazolopyridine and their pharmacological and antimicrobial evaluations
Author(s) -
Mahmoud Naglaa F. H.,
Balamon Mina G.
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.4011
Subject(s) - chemistry , antimicrobial , pyridine , combinatorial chemistry , potency , lead compound , mtt assay , reagent , stereochemistry , docking (animal) , in vitro , organic chemistry , biochemistry , medicine , nursing
Various fused‐heterocyclic‐derivatives containing thiazolopyridine moieties has been synthesized by allowing 5‐aminothiazolo[3,2‐a]pyridine derivative 1 to undergo annulations reactions with different reagents under different‐reaction conditions. The biological assessment of compounds 2 , 11 , 14 , 15 , and 19 showed remarkable antimicrobial activities. In addition, selected derivatives of the products were screened for their anticancer activities against two tumor cell lines using MTT assay and the results showed that some of these compounds have potent cytotoxic effect, as concluded from their IC 50 values. Meanwhile, compounds 3a , 7 have exhibited very strong potency as anticancer candidates. Thiazolopyridine structures have been confirmed as a useful lead compounds for the development of new anticancer agents. Molecular docking showed that,‐some of the synthesized compounds more suitable inhibitor against‐ALR2 with farther alteration in future.