Skip to content
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Menu
Home
About Us
Resources
Profiles Metrics
Authors Directory
Institutions Directory
Top Authors
Top Institutions
Top Sponsors
AI Digest
Contact Us
Publication Details
AFRICAN RESEARCH NEXUS
SHINING A SPOTLIGHT ON AFRICAN RESEARCH
agricultural and biological sciences
Synthesis of lupeol derivatives and their antileishmanial and antitrypanosomal activities
Natural Product Research, Volume 32, No. 3, Year 2018
Notification
URL copied to clipboard!
Description
The natural product lupeol 1 was isolated from aerial parts of Vernonia scorpioides with satisfactory yield, which made it viable to be used as starting material in semisynthetic approach. Ten lupeol derivatives 2–11 were prepared by classical procedures. Including, five new esters derivatives 7–11, which were obtained by structural modifications in the isopropylidene fragment. All semisynthetic compounds and lupeol 1–11 were confirmed by 1H NMR, 13C NMR and HRMS. Their antiprotozoal activity was evaluated in vitro against L. amazonensis and T. cruzi. Derivative 6 showed the best antitrypanosomal activity (IC50 = 12.48 μg/mL) and the lowest cytotoxic derivative (CC50 = 161.50 μg/mL). The mechanism of action of the most active derivatives (4, 6 and 11) is not dependent from the enzyme trypanothione reductase. © 2017 Informa UK Limited, trading as Taylor & Francis Group.
Authors & Co-Authors
Sandjo, Louis P.
Brazil, Florianopolis
Universidade Federal de Santa Catarina
Steindel, Mário
Brazil, Florianopolis
Universidade Federal de Santa Catarina
Biavatti, Maique Weber
Brazil, Florianopolis
Universidade Federal de Santa Catarina
Statistics
Citations: 19
Authors: 3
Affiliations: 1
Identifiers
Doi:
10.1080/14786419.2017.1353982
ISSN:
14786419