Synthesis and biological evaluation against Mycobacterium tuberculosis and Leishmania amazonensis of a series of diaminated terpenoids
| Autor: | Mauricio Frota Saraiva, Thalita Cristina Alves Souza, Iriane Eger, Maria C.S. Lourenço, Mauro V. de Almeida, Dijovani Batista dos Reis, Adriano Barbosa |
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| Rok vydání: | 2016 |
| Předmět: |
0301 basic medicine
Leishmania mexicana Antiprotozoal Agents Antitubercular Agents Microbial Sensitivity Tests Diamines Mycobacterium tuberculosis Terpene 03 medical and health sciences chemistry.chemical_compound Structure-Activity Relationship 0302 clinical medicine Parasitic Sensitivity Tests Diamine Structure–activity relationship Pharmacology biology Molecular Structure Terpenes Biological activity General Medicine biology.organism_classification Terpenoid In vitro 030104 developmental biology chemistry Biochemistry 030220 oncology & carcinogenesis Drug Design |
| Zdroj: | Biomedicinepharmacotherapy = Biomedecinepharmacotherapie. 84 |
| ISSN: | 1950-6007 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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