Synthesis and Antimalarial Activity of 4-Methylaminoquinoline Compounds against Drug-Resistant Parasite

Autor:	Anamika Sharma, Ashan Manhas, Renu Tripathi, Prince Joshi, Vinay Shankar Tiwari, Wahajul Haq, Sushobhan Chowdhury, Niti Kumar, Kanchan Yadav
Rok vydání:	2020
Předmět:	biology Chemistry General Chemical Engineering Plasmodium falciparum General Chemistry Drug resistance Pharmacology biology.organism_classification In vitro Article In vivo Antimalarial Agent Cytotoxicity QD1-999 IC50 Plasmodium yoelii
Zdroj:	ACS Omega ACS Omega, Vol 6, Iss 20, Pp 12984-12994 (2021)
ISSN:	2470-1343
Popis:	A series of novel 4-aminoquinoline analogues bearing a methyl group at 4-aminoquinoline moiety were synthesized via a new and robust synthetic route comprising in situ tert-butoxycarbonyl (Boc) deprotection-methylation cascade resulting in the corresponding N-methylated secondary amine using Red-Al and an efficient microwave-assisted strategy for the fusion of N-methylated secondary amine with 4-chloroquinoline nucleus to access the series of novel 4-N-methylaminoquinoline analogues. The new series of compounds were evaluated for their antimalarial activity in in vitro and in vivo models. Among 21 tested compounds, 9a-i have shown a half-maximal inhibitory concentration (IC50) value less than 0.5 μM (i.e.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2cc54012a2da140ef04909ff1f86701f https://pubmed.ncbi.nlm.nih.gov/34056449 Zobrazit plný text záznamu