Design and Synthesis of a New Class of 4-Aminoquinolinyl- and 9-Anilinoacridinyl Schiff Base Hydrazones as Potent Antimalarial Agents

Autor:	Kumkum Srivastava, Shiv Vardan Singh, Prem M. S. Chauhan, Rajeev K. Srivastava, Jitendra Kumar Saxena, Kuldeep Chauhan, Moni Sharma, Sunil K. Puri
Rok vydání:	2014
Předmět:	Male Stereochemistry Plasmodium falciparum Biochemistry Antimalarials Mice chemistry.chemical_compound Chlorocebus aethiops Drug Discovery Animals Antimalarial Agent Malaria Falciparum Cytotoxicity Vero Cells Heme Schiff Bases Pharmacology Schiff base Strain (chemistry) biology Organic Chemistry Hydrazones biology.organism_classification In vitro chemistry 4-Aminoquinoline Aminoquinolines Acridines Molecular Medicine
Zdroj:	Chemical Biology & Drug Design. 84:175-181
ISSN:	1747-0277
DOI:	10.1111/cbdd.12289
Popis:	A series of novel 4-aminoquinolinyl and 9-anilinoacridinyl Schiff base hydrazones have been synthesized and evaluated for their antimalarial activity. All compounds were evaluated in vitro for their antimalarial activity against chloroquine-sensitive strain 3D7 and the chloroquine-resistant K1 strain of Plasmodium falciparum and for cytotoxicity toward Vero cells. Compounds 17, 20, and 21 displayed good activity against the 3D7 strain with IC50 values ranging from 19.69 to 25.38 nm. Moreover, compounds 16, 17, 21, 24, 32, and 33 exhibited excellent activities (21.64-54.26 nm) against K1 strain and several compounds displayed β-hematin inhibitory activity, suggesting that they act on the heme crystallization process such as CQ. Compounds were also found to be non-toxic with good selectivity index.
Databáze:	OpenAIRE
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