Design, synthesis and studies on novel N-Mannich base derivatives of isatin targeting dihydrofolate reductase receptor

Abstract

Major challenge with the existing treatment for Cerebral Malaria is to target the drug effectively to the brain. The present study involves the designing of N-Mannich base derivatives of Primaquine bearing isatin as heterocyclic scaffolds and identification based on binding interactions with dihydrofolate reductase (DHFR) receptor. Identified potential candidates were synthesized and characterized, followed by their determination of partition coefficient using shake flask method. The synthesized compounds were characterized by analytical techniques such as FT-IR, 1H NMR. Cumulative studies have provided us best candidate DTS-29 with good affinity and better lipophilicty and will be taken for further investigations.