2. Academic Validation
  3. Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives

Synthesis and evaluation of the antiplasmodial activity of novel indeno[2,1-c]quinoline derivatives

  • Bioorg Med Chem. 2014 Nov 1;22(21):5757-65. doi: 10.1016/j.bmc.2014.09.040.
Anna Barteselli 1,  Silvia Parapini 2,  Nicoletta Basilico 3,  Danilo Mommo 1,  Anna Sparatore 4
Affiliations

Affiliations

  • 1 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy.
  • 2 Dipartimento di Scienze Farmacologiche e Biomolecolari, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy.
  • 3 Dipartimento di Scienze Biomediche Chirurgiche e Odontoiatriche, Università degli Studi di Milano, Via C. Pascal 36, 20133 Milano, Italy.
  • 4 Dipartimento di Scienze Farmaceutiche, Università degli Studi di Milano, Via Mangiagalli 25, 20133 Milano, Italy. Electronic address: anna.sparatore@unimi.it.
PMID: 25311562 DOI: 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 6.9 μM 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.

Keywords

Antimalarial activity; Antiplasmodial activity; Indeno[2,1-c]quinoline; Plasmodium falciparum.

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