Research article

CHARACTERIZATION AND OPTIMIZATION OF THE ANTIMALARIAL AND DRUG METABOLISM AND PHARMACOKINETIC ACTIVITIES OF BETA-HYDROXY ETHYLAMINE BASED PLASMEPSIN INHIBITORS

1Mr. Alok Semwal, 2Mrs. Usha Singh, 3Miss Shalini Kesharwani, 4Dr. Prasoon Saxena, 5Dr. Alok Pratap Singh, 6Mr. Anshul Tyagi, 7Mr. Nitish Kumar, 8Miss. Prerna Gupta,

Online First: January 08, 2023


First, in malaria-endemic areas, antimalarial drugs were often given to high-risk individuals including pregnant women and children at improperly low doses. The drug's shelf life will be reduced if resistance spreads more rapidly. As a result of the current method for determining dose, this is a logical fallout. Another approach to dose discovery is to use phase 2 research to first characterize the PK-PD and calibrate in vitro susceptibility data in vivo. It is feasible to accurately quantify the early therapeutic responses by mPlasmepsins, a kind of aspartic protease found in Plasmodium, are critical to the parasite's ability to survive in the host. Plasmeptins in the digestive vacuole break down hemoglobin, providing food for the parasite. Several parasite proteins are processed for export into the erythrocyte by the protease known as Plasmepsin V. For the time being, we don't know how the human body uses the other plasmepsins that have not been identified. There has been a lot of interest in the digestive vacuole-targeting plasmepsin inhibitors throughout the past decade. Due to the need for new antimalarial drugs that may quickly lower parasitemia, precise parasitemia modulation data from in vivo models is required. A new family of antimalarial drugs has been proposed based on the pharmacological properties of hydroxyethyl amines, a group of alkanolamine molecules.

Keywords

Antimalarial Drug Metabolism, Hydroxy-ethylamine, Plasmepsin, Pharmacokinetic, Plasmodium.