| Autor: |
Conroy T; School of Chemistry, The University of Sydney , Building F11, Sydney, New South Wales 2006, Australia., Guo JT, Elias N, Cergol KM, Gut J, Legac J, Khatoon L, Liu Y, McGowan S, Rosenthal PJ, Hunt NH, Payne RJ |
| Jazyk: |
angličtina |
| Zdroj: |
Journal of medicinal chemistry [J Med Chem] 2014 Dec 26; Vol. 57 (24), pp. 10557-63. Date of Electronic Publication: 2014 Dec 08. |
| DOI: |
10.1021/jm501439w |
| Abstrakt: |
Analogues of the natural product gallinamide A were prepared to elucidate novel inhibitors of the falcipain cysteine proteases. Analogues exhibited potent inhibition of falcipain-2 (FP-2) and falcipain-3 (FP-3) and of the development of Plasmodium falciparum in vitro. Several compounds were equipotent to chloroquine as inhibitors of the 3D7 strain of P. falciparum and maintained potent activity against the chloroquine-resistant Dd2 parasite. These compounds serve as promising leads for the development of novel antimalarial agents. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
|
