Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives
Articolo
Data di Pubblicazione:
2014
Citazione:
Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives / A. Barteselli, S. Parapini, N. Basilico, D. Mommo, A. Sparatore. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - 22:21(2014 Nov 01), pp. 5757-5765. [10.1016/j.bmc.2014.09.040]
Abstract:
With the aim to explore the potentiality of new chemical scaffolds for the design of new antimalarials, a set of new indeno[2,1-c]quinolines bearing different basic heads has been synthesized and tested in vitro against chloroquine sensitive (CQ-S) and chloroquine resistant (CQ-R) strains of Plasmodium falciparum. Most of the synthesized compounds exhibited a moderate antiplasmodial activity, inhibiting the growth of both CQ-S and CQ-R strains of P. falciparum with IC50 ranging from 0.24 to 6.9μM and with a very low resistance index. The most potent compounds (1.2-1.3-fold the CQ on the W-2 strain) can be considered as promising 'lead compounds' to be further optimized to improve efficacy and selectivity against Plasmodia.
Tipologia IRIS:
01 - Articolo su periodico
Keywords:
Indeno[2,1-c]quinoline; Antimalarial activity; Plasmodium falciparum; Antiplasmodial activity
Elenco autori:
A. Barteselli, S. Parapini, N. Basilico, D. Mommo, A. Sparatore
Link alla scheda completa: