Second-generation pterocarpanquinones: synthesis and antileishmanial activity

Journal of Venomous Animals and Toxins including Tropical Diseases

Lívia C. R. M. da Frota¹  Viviane dos Santos Faiões²  Edézio Ferreira Cunha-Junior³  Julio C. F. Barcellos⁴ 

[1] Instituto de Pesquisa de Produtos naturais, Universidade Federal do Rio de Janeiro;Laboratório de Bioquímica de Tripanosomatídeos, Instituto Oswaldo Cruz, FIOCUZ;Laboratório de Imunofarmacologia Parasitária, Universidade do Estado do Rio de Janeiro;Laboratório de Química, Universidade Federal do Rio de Janeiro, campus Professor Aloísio Teixeira

关键词: Leishmania;    Pterocarpanquinone;    LQ-118;    Phenotypic assay;    Leishmaniasis;    Drug discovery;    Neglected diseases;   

DOI  :  10.1186/s40409-018-0174-7

学科分类：过敏症与临床免疫学

来源: SciELO

【 摘 要 】

BackgroundDespite the development of new therapies for leishmaniasis, among the 200 countries or territories reporting to the WHO, 87 were identified as endemic for Tegumentary Leishmaniasis and 75 as endemic for Visceral Leishmaniasis. The identification of antileishmanial drug candidates is essential to fill the drug discovery pipeline for leishmaniasis. In the hit molecule LQB-118 selected, the first generation of pterocarpanquinones was effective and safe against experimental visceral and cutaneous leishmaniasis via oral delivery. In this paper, we report the synthesis and antileishmanial activity of the second generation of pterocarpanoquinones.

【 授权许可】

CC BY