71429-13-5Relevant academic research and scientific papers
Design, synthesis, antimalarial activity and docking study of 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines
Chetia, Dipak,Kalita, Jahnabi,Rudrapal, Mithun
, p. 928 - 937 (2020/08/19)
Background: Malaria is a growing infectious disease burden due to the increasing emergence of resistant strains of Plasmodium falciparum. Because of the limited therapeutic effi-cacy of available antimalarial drugs, the development of potent antimalarial drug agents is there-fore an urgent requirement to fight against resistant malaria. Objective: The objective of this work was to develop novel quinoline-baed antimalarial agents that would be active against resistant P. falciparum malaria. Methods: Some 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines were synthesized for the evaluation of their potential as possible antimalarial agents, particularly against resistant malaria. The antimalarial activity of synthesized compounds was evaluated in vitro against blood-stage parasites of P. falciparum. Further, molecular docking and drug-likeness including ADMET (Absorption, Distribution, Metabolism, Elimination and Toxicity) studies were also carried out using in silico tools. Results: Results reveal the in vitro antimalarial activity of synthesized 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines against P. falciparum. The docking study investigates the an-timalarial effectiveness of synthesized quinolines as novel plasmepsin 2 inhibitors. Drug-likeness prediction exhibits acceptable drug-likeness and ADMET properties. Conclusion: Based upon our findings, it is concluded that the molecular scaffold of 7-chloro-4-(2-(substituted benzylidene)hydrazineyl)quinolines may be used as a lead structure for further modi-fications in the search of more potent antimalarial drug molecules.
Quinoline-azetidinone hybrids: Synthesis and in vitro antiproliferation activity against Hep G2 and Hep 3B human cell lines
Alegaon,Parchure,Araujo,Salve,Alagawadi,Jalalpure,Kumbar
, p. 1566 - 1571 (2017/03/17)
In search of new heterocyclic anticancer agents, a new quinoline-azetidinone hybrid template have been designed, synthesized and screened for their cytotoxic activity against human cancer cell lines such as Hep G2, and Hep 3B by the MTT assay and results were compared with paclitaxel, 5-fluorouracil and doxorubicin. Interestingly, some of the compounds were found significantly active against both cell lines. The compound 6f (IC50?=?0.04?±?0.01?μM) exhibited potent antiproliferation activity against Hep G2 cell line, and 6j compound (IC50?=?0.66?±?0.01?μM) demonstrated potent antiproliferation activity against Hep 3B cell line and provide to be more potent as cytotoxic agents than standard drugs. Morphological changes suggest the induction of apoptosis and describe the mechanism of action of these hybrid antitumor agents.
Synthesis and antitubercular activity of 7-chloro-4-quinolinylhydrazones derivatives
Candea, Andre L.P.,Ferreira, Marcelle de L.,Pais, Karla C.,Cardoso, Laura N.de F.,Kaiser, Carlos R.,Henriques, Maria das Gracas M.de O.,Lourenco, Maria C.S.,Bezerra, Flavio A.F.M.,de Souza, Marcus V.N.
scheme or table, p. 6272 - 6274 (2010/06/20)
A series of twenty-one 7-chloro-4-quinolinylhydrazones (3a-u) have been synthesized and evaluated for their in vitro antibacterial activity against Mycobacterium tuberculosis H37Rv. The compounds 3f, 3i and 3o were non-cytotoxic and exhibited a
