ACS Medicinal Chemistry Letters p. 373 - 377 (2014)
Update date:2022-07-30
Topics:
Jaudzems, Kristaps
Tars, Kaspars
Maurops, Gundars
Ivdra, Natalija
Otikovs, Martins
Leitans, Janis
Kanepe-Lapsa, Iveta
Domraceva, Ilona
Mutule, Ilze
Trapencieris, Peteris
Blackman, Michael J.
Jirgensons, Aigars
Antimalarial hit 1SR (TCMDC-134674) identified in a GlaxoSmithKline cell based screening campaign was evaluated for inhibitory activity against the digestive vacuole plasmepsins (Plm I, II, and IV). It was found to be a potent Plm IV inhibitor with no selectivity over Cathepsin D. A cocrystal structure of 1SR bound to Plm II was solved, providing structural insight for the design of more potent and selective analogues. Structure-guided optimization led to the identification of structurally simplified analogues 17 and 18 as low nanomolar inhibitors of both, plasmepsin Plm IV activity and P. falciparum growth in erythrocytes.
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Doi:10.1002/jhet.3864
(2020)Doi:10.1016/S0040-4039(00)61429-6
(1993)Doi:10.1248/cpb.c15-00309
(2015)Doi:10.1016/j.tetlet.2006.11.083
(2007)Doi:10.1021/ja001180f
(2000)Doi:10.1016/S0040-4020(01)80237-4
(1993)