2. Academic Validation
  3. Isolation, structure elucidation, and synthesis of antiplasmodial quinolones from Crinum firmifolium

Isolation, structure elucidation, and synthesis of antiplasmodial quinolones from Crinum firmifolium

  • Bioorg Med Chem. 2017 Aug 1;25(15):4203-4211. doi: 10.1016/j.bmc.2017.06.017.
Christopher C Presley 1,  Yongle Du 1,  Seema Dalal 2,  Emilio F Merino 3,  Joshua H Butler 3,  Stéphan Rakotonandrasana 4,  Vincent E Rasamison 4,  Maria B Cassera 3,  David G I Kingston 5
Affiliations

Affiliations

  • 1 Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, VA 24061, United States.
  • 2 Department of Biochemistry and Virginia Tech Center for Drug Discovery, M/C 0308, Virginia Tech, Blacksburg, VA 24061, United States.
  • 3 Department of Biochemistry and Molecular Biology, and Center for Tropical and Emerging Global Diseases (CTEGD), University of Georgia, Athens, GA 30602, United States.
  • 4 Centre National d'Application des Recherches Pharmaceutiques, B.P 702, Antananarivo 101, Madagascar.
  • 5 Department of Chemistry and Virginia Tech Center for Drug Discovery, M/C 0212, Virginia Tech, Blacksburg, VA 24061, United States. Electronic address: dkingston@vt.edu.
PMID: 28648491 DOI: 10.1016/j.bmc.2017.06.017
Abstract

Antiplasmodial bioassay guided fractionation of a Madagascar collection of Crinum firmifolium led to the isolation of seven compounds. Five of the seven compounds were determined to be 2-alkylquinolin-4(1H)-ones with varying side chains. Compounds 1 and 4 were determined to be known compounds with reported antiplasmodial activities, while 5 was believed to be a new branched 2-alkylquinolin-4(1H)-one, however, it was isolated in limited quantities and in admixture and therefore was synthesized to confirm its structure as a new antiplasmodial compound. Along with 5, two Other new and branched compounds 6 and 7 were synthesized as well. Accompanying the five quinolones were two known compounds 2 and 3 which are inactive against Plasmodium falciparum. The isolation, structure elucidation, total synthesis, and biological evaluation of these compounds are discussed in this article.

Keywords

Amaryllidaceae; Antiplasmodial; Crinum; Quinolone.

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