1. Synthesis and biological evaluation against Mycobacterium tuberculosis and Leishmania amazonensis of a series of diaminated terpenoids.
- Author
-
Dos Reis DB, Souza TCA, Lourenço MCS, de Almeida MV, Barbosa A, Eger I, and Saraiva MF
- Subjects
- Drug Design, Leishmania mexicana growth & development, Microbial Sensitivity Tests, Molecular Structure, Mycobacterium tuberculosis growth & development, Parasitic Sensitivity Tests, Structure-Activity Relationship, Antiprotozoal Agents chemical synthesis, Antiprotozoal Agents pharmacology, Antitubercular Agents chemical synthesis, Antitubercular Agents pharmacology, Diamines chemical synthesis, Diamines pharmacology, Leishmania mexicana drug effects, Mycobacterium tuberculosis drug effects, Terpenes chemical synthesis, Terpenes pharmacology
- Abstract
We report the synthesis of a series of diaminated terpenoids containing, as side-chain of the diamine core, the "head-to-tail" prenyl derivatives, with amino amino spacers of variable length. In vitro biological activity of these compounds was evaluated against Mycobacterium tuberculosis and Leishmania amazonensis, and the structure-activity relationships are discussed. Different biological results were observed depending on the terpenic side-chain length. The best results were obtained for trans,trans-farnesol derivatives. Moreover, these results demonstrated that the stereochemistry of the double bond could play an important role in determining antitubercular and antileishmanial activities of these compounds., (Copyright © 2016 Elsevier Masson SAS. All rights reserved.)
- Published
- 2016
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