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Synthesis and antimalarial activity of ethyl 3‐amino‐4‐oxo‐9‐(phenylsubstituted)thieno[2,3‐ b ]quinoline‐2‐carboxylate derivatives
Author(s) -
Charris Jaime,
Barazarte Arthur,
Domínguez JosÉ,
Lobo Gricela,
Camacho JosÉ,
Ferrer Rosa,
Gamboa Neira,
Rodrigues Juan,
Capparelli Mario V.
Publication year - 2007
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.5570440320
Subject(s) - chemistry , quinoline , hemoglobin , hydrolysis , plasmodium berghei , in vivo , stereochemistry , in vitro , carboxylate , antimalarial agent , plasmodium falciparum , biochemistry , organic chemistry , microbiology and biotechnology , malaria , immunology , biology
A series of thieno[ 2 ,3‐ b ]quinolone derivatives were synthesized and investigated for their abilities to inhibit β‐hematin formation, hemoglobin hydrolysis and in vivo for their efficacy in rodent Plasmodium berghei. Compound 3b was the most promising as inhibitor of hemoglobin hydrolysis, and its effects as inhibitor of β‐hematin formation was promising. When the aromatic ring was substituted in 2 (Me), in 3 (CF 3 ) or in 2,4 (Cl) the inhibition of hemoglobin proteolysis was maximal (88%), the rest of compounds maintained a low inhibition. The most active compound to emerge in vitro and in murine studies, was 3b suggesting an antimalarial activity via multiple mechanisms.