Name: Picolinoyl chloride hydrochloride. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: Picolinoyl chloride hydrochloride, is researched, Molecular C6H5Cl2NO, CAS is 39901-94-5, about Ring Distortion of Vincamine Leads to the Identification of Re-Engineered Antiplasmodial Agents.
There is a significant need for new agents to combat malaria, which resulted in ~409,000 deaths globally in 2019. We utilized a ring distortion strategy to create complex and diverse compounds from vincamine with the goal of discovering mols. with re-engineered biol. activities. We found compound 8 (V3b) to target chloroquine-resistant Plasmodium falciparum Dd2 parasites (EC50 = 1.81 ± 0.09 μM against Dd2 parasites; EC50 > 40 μM against HepG2 cells) and established structure-activity relationships for 25 related analogs. New analog 30 (V3ss, Dd2, EC50 = 0.25 ± 0.004 μM; HepG2, EC50 > 25 μM) was found to demonstrate the most potent activity, which prevents exit on the parasite from the schizont stage of intraerythrocytic development and requires >24 h to kill P. falciparum Dd2 cells. These findings demonstrate the potential that vincamine ring distortion has toward the discovery of novel antimalarial agents and other therapies significant to human health.
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