Tempone, Andre G.
Anderson, Edward A.
Total Authors: 5
 Univ Oxford, Chem Res Lab, 12 Mansfield Rd, Oxford OX1 3TA - England
 Univ Sao Paulo, Inst Med Trop, Programa Posgrad Med Trop, Av Dr Eneas de Carvalho Aguiar 470, BR-05403000 Sao Paulo - Brazil
 Adolfo Lutz Inst, Ctr Parasitol & Mycol, Av Dr Arnaldo 351, BR-01246000 Sao Paulo - Brazil
Total Affiliations: 3
n. 2, SI
JAN 10 2020.
Web of Science Citations:
Chagas disease and visceral leishmaniasis are neglected protozoan diseases with significant impact in developing countries. Due to the limited number and toxicity of current therapies, new drug leads are urgently needed. In this work, four aporphine natural products were synthesized using an enantioselective, modular and convergent strategy, comprising eight steps in the longest linear sequence; key steps included Bischler-Napieralski cyclization/Noyori asymmetric reduction to construct the tetrahydroisoquinolines, and palladium-catalyzed arylation to close the C ring. Norglaucine, nordicentrine and dicentrine showed promising bioactivity against T. cruzi and L. infantum, suggesting potential for further development of these scaffolds as antiparasitic agents. (C) 2019 Elsevier Ltd. All rights reserved. (AU)