2. Academic Validation
  3. Bistacrine derivatives as new potent antimalarials

Bistacrine derivatives as new potent antimalarials

  • Bioorg Med Chem. 2016 Aug 15;24(16):3636-42. doi: 10.1016/j.bmc.2016.06.003.
Ines Schmidt 1,  Gabriele Pradel 2,  Ludmilla Sologub 2,  Alexandra Golzmann 2,  Che J Ngwa 2,  Anna Kucharski 1,  Tanja Schirmeister 3,  Ulrike Holzgrabe 4
Affiliations

Affiliations

  • 1 Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany.
  • 2 Institute of Molecular Biotechnology, RWTH Aachen University, Worringerweg 1, 52074 Aachen, Germany.
  • 3 Institute of Pharmacy and Biochemistry, University of Mainz, Staudinger Weg 5, 55099 Mainz, Germany.
  • 4 Institute of Pharmacy and Food Chemistry, University of Würzburg, Am Hubland, 97074 Würzburg, Germany. Electronic address: ulrike.holzgrabe@uni-wuerzburg.de.
PMID: 27316542 DOI: 10.1016/j.bmc.2016.06.003
Abstract

Linking two tacrine molecules results in a tremendous increase of activity against Plasmodia in comparison to the monomer. This finding prompted the synthesis of a library of monomeric and dimeric tacrine derivatives in order to derive structure-activity relationships. The most active compounds towards chloroquine sensitive Plasmodium strain 3D7 and chloroquine resistant strain Dd2 show IC50 values in the nanomolar range of concentration, low cytotoxicity and target the cysteine protease falcipain-2, which is essential for Parasite growth.

Keywords

Antimalarials; Bistacrines; Falcipain-2 inhibitors.

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