Second-generation pterocarpanquinones: synthesis and antileishmanial activity

[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.

[学科分类] 过敏症与临床免疫学

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