Life Sciences & Biotechnology
Title : | Design and development of anti-malarial agents targeting the invasion machinery and asexual stages of malaria parasite |
Area of research : | Life Sciences & Biotechnology |
Principal Investigator : | Dr. Prashant Revan Murumkar , Maharaja Sayajirao University Of Baroda, Gujarat |
Timeline Start Year : | 2023 |
Timeline End Year : | 2026 |
Contact info : | prashant_murumkar@yahoo.com |
Equipments : | Rotary Evaporator with chiller |
Details
Executive Summary : | The current antimalarial drugs are facing resistance due to the specialized stages of Plasmodium falciparum, which invade mosquito gut walls, erythrocytes, and hepatocytes. The actin-myosin complex supports these invasions. Most drugs target the erythrocytic phase of the parasite, with only a few FDA-approved drugs effective against pre-erythrocytic or multistage stages. Few compounds target the glideosomal complex, and some hetrocycles like benzimidazoles have shown strong asexual blood stage activity, inhibiting microtubule and hemozoin formation. Researchers have also reported heterocyclic moiety-containing compounds like astemizole for malaria disease management. To address this issue, researchers are exploring different heterocyclic compounds like pthalamide, 2-aminopyridine, and L-proline in combination with piperaquin, which has shown efficient potency against malaria and is used in combination therapy with dihydroartemisinin. The piperquine moiety is known for interfering with the detoxification of heme. The project aims to design and synthesize a novel series of piperazinyl quinoline substituted heterocyclic compounds with activity against the asexual phase of the parasite. The compounds will have active pharmacophores like piperaquine and heterocycle scaffolds through a linker to offer final hybrids. The synthesized compounds will be evaluated for in vitro and invivo biological screening targeting the asexual site and invasion machinery of the malaria parasite. |
Total Budget (INR): | 28,93,260 |
Organizations involved