2. Academic Validation
  3. Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials

Lead optimization of 3-carboxyl-4(1H)-quinolones to deliver orally bioavailable antimalarials

  • J Med Chem. 2012 May 10;55(9):4205-19. doi: 10.1021/jm201642z.
Yiqun Zhang 1,  Julie A Clark,  Michele C Connelly,  Fangyi Zhu,  Jaeki Min,  W Armand Guiguemde,  Anupam Pradhan,  Lalitha Iyer,  Anna Furimsky,  Jason Gow,  Toufan Parman,  Farah El Mazouni,  Margaret A Phillips,  Dennis E Kyle,  Jon Mirsalis,  R Kiplin Guy
Affiliations

Affiliation

  • 1 Department of Chemical Biology and Therapeutics, St. Jude Children's Research Hospital, 262 Danny Thomas Place, Memphis, Tennessee 38105, USA.
PMID: 22435599 DOI: 10.1021/jm201642z
Abstract

Malaria is a protozoal parasitic disease that is widespread in tropical and subtropical regions of Africa, Asia, and the Americas and causes more than 800,000 deaths per year. The continuing emergence of multidrug-resistant Plasmodium falciparum drives the ongoing need for the development of new and effective antimalarial drugs. Our previous work has explored the preliminary structural optimization of 4(1H)-quinolone ester derivatives, a new series of antimalarials related to the endochins. Herein, we report the lead optimization of 4(1H)-quinolones with a focus on improving both antimalarial potency and bioavailability. These studies led to the development of orally efficacious antimalarials including Quinolone analogue 20g, a promising candidate for further optimization.

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