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Title: 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, Saraiva MF. Journal: Biomed Pharmacother; 2016 Dec; 84():1739-1747. PubMed ID: 27876209. 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.[Abstract] [Full Text] [Related] [New Search]