Antileishmanial agent-13

Antileishmanial agent-13 is a quinoline-isatin hybrid, acts as an antileishmanial agent against L. Major Leishmania strain. Antileishmanial agent-13 acquires the antileishmanial activity via the anti-folate mechanism. Antileishmanial agent-13 has potent inhibition against both promastigote and amastigote forms with IC50s of 0.604 μM and 0.508 μM, respectively[1].

Research Areas >> Infection

Antileishmanial agent-13 (化合物 4e) 对前鞭毛体的体外活性优于 Miltefosine (HY-13685) (IC50=7.8976 μ M)[1]。 Antileishmanial agent-13 (2 μM; 48 h) 显示抗利什曼病活性，主要归因于抗叶酸机制，通过抑制 DHFR-TS 和 PTR1[1]。 Antileishmanial agent-13 (0-100 μM; 72 h) 对非洲绿猴肾细胞 (VERO 细胞) 具有较低的细胞毒性，CC50 值为 155.8 μM[1]。

[1]. Sabt A, et al. New antileishmanial quinoline linked isatin derivatives targeting DHFR-TS and PTR1: Design, synthesis, and molecular modeling studies[J]. European Journal of Medicinal Chemistry, 2022: 114959.