2. Academic Validation
  3. Novel squaramides with in vitro liver stage antiplasmodial activity

Novel squaramides with in vitro liver stage antiplasmodial activity

  • Bioorg Med Chem. 2016 Apr 15;24(8):1786-92. doi: 10.1016/j.bmc.2016.03.005.
Carlos J A Ribeiro 1,  Margarida Espadinha 1,  Marta Machado 2,  Jiri Gut 3,  Lídia M Gonçalves 1,  Philip J Rosenthal 3,  Miguel Prudêncio 2,  Rui Moreira 1,  Maria M M Santos 4
Affiliations

Affiliations

  • 1 Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Professor Gama Pinto, 1649-003 Lisboa, Portugal.
  • 2 Instituto de Medicina Molecular, Faculdade de Medicina, Universidade de Lisboa, Av. Professor Egas Moniz, 1649-028 Lisboa, Portugal.
  • 3 Department of Medicine, San Francisco General Hospital, University of California, San Francisco, CA 94143, USA.
  • 4 Research Institute for Medicines (iMed.ULisboa), Faculty of Pharmacy, Universidade de Lisboa, Av. Professor Gama Pinto, 1649-003 Lisboa, Portugal. Electronic address: mariasantos@ff.ulisboa.pt.
PMID: 26968650 DOI: 10.1016/j.bmc.2016.03.005
Abstract

A structure-activity relationship study was performed with ten 8-aminoquinoline-squaramides compounds active against liver stage malaria parasites, using human hepatoma cells (Huh7) infected by Plasmodium berghei parasites. In addition, their blood-schizontocidal activity was assessed against chloroquine-resistant W2 strain Plasmodium falciparum. Compound 3 was 7.3-fold more potent than the positive control primaquine against liver-stage parasites, illustrating the importance of the squarate moiety to activity.

Keywords

8-Aminoquinoline; Antiplasmodial activity; Liver stage; Malaria; Squaramide.

Figures
嗨！很高兴为您提供帮助！

尊敬的 MCE 客户您好，
请您选择所在区域，我们将转接对应客服为您服务！

热门区域

A

B

C

F

G

H

J

L

N

Q

S

T

X

Y

Z

热 A B C F G H J L N Q S T X Y Z