SYNTHESIS AND ANTIPLASMODIAL ACTIVITY OF SOME NOVEL CHALCONE DERIVATIVES
Journal Title: Asian Journal of Pharamceutical and Clinical Research - Year 2015, Vol 8, Issue 2
Abstract
Increased drug resistance in malaria toward many of the existing antimalarials make the condition worse. Hence, indicates the necessity of thenovel molecules to overcome the problem. A series of chalcone derivatives (3a-4e) were primed via Claisen-Schmidt condensation of substitutedaldehydes with substituted methyl ketones. These derivatives were tested against Plasmodium falciparum clinical isolate for their antiplasmodialactivity. Furthermore, in-vitro β-hematin formation assay has been conducted in order to gain insight into the possible mechanism of action. Outof the 10 synthesized compounds, two compounds 4a and 4d exhibited promising antiplasmodial activities (50% inhibitory concentration [IC50]values 7.45±0.65 and 6.01±0.29 μg/ml, respectively). Other compounds (3a, 4b, 4e and 3d) showed moderate inhibition against P. falciparum. Amongall the compounds, 4a showed good hemozoin inhibitory activity (IC50 - 19.75 μg/ml) while 3a and 4d showed moderate type inhibition. Thesemolecules may act as templates for medicinal chemistry to discover novel and hybrid molecules with improved characteristics, which may becomefuture candidates for the treatment of malaria.Keywords: Chalcone, Malaria, Plasmodium falciparum, β-hematin.Â
Authors and Affiliations
Neetu Tomar, Shiv Vardan Singh, Chottes Lal Jain, Gaurav Verma, Anirban Pal, Vineeta Singh
Keywords
Related Articles
- EP ID EP605620
- DOI -
- Views 91
- Downloads 0
EVALUATION AND COMPARISON OF CYTOTOXIC EFFECT OF VILAZODONE HYDROCHLORIDE WITH 5-FLUOROURACIL IN HT-29 BOWEL CANCER CELL LINE
Objectives: Vilazodone hydrochloride is a novel selective serotonin reuptake inhibitor (SSRI) used to treat major depressive disorders. There are only sparse data available to know about the SSRI’s and its association wi...
SLEEP DISTURBANCE AND QUALITY OF SLEEP AMONG PATIENTS WITH CARDIOVASCULAR DISEASES
Objective: This was a descriptive study with the objective to determine the sleep disturbances and the quality of sleep among patients with cardiovascular diseases (CVDs).Methods: Quantitative approach with non-experimen...
EFFICACY OF BOERHAAVIA DIFFUSA L. ON DISRUPTION OF GONADOTROPINS AND TESTOSTERONE IN FLUORIDE INTOXICATED MALE RATS
  Objective: The present study explored the influence of fluoride exposure on gonadotropins and reproductive hormones.Methods: Male Wistar albino rats weighing 100-150 g were administered with 100, 200, and 300 ppm/kg...
DRUG UTILIZATION ANALYSIS OF ANTI-SNAKE VENOM AT A TERTIARY CARE CENTER IN CENTRAL MAHARASHTRA: A 3-YEAR RETROSPECTIVE STUDY
Objectives: In India, snakebite is a major public health problem. Anti-snake venom serum (ASVS) is the definitive treatment for poisonous snakebites. However, the non-availability of effective ASVS to treat the specific...
SOLUBILITY ENHANCEMENT OF GLIBENCLAMIDE USING MESOPOROUS SILICA
Glibenclamide is a BCS Class II drug and poses a major problem during formulation development. In the present study, adsorption onto various carriers was used to enhance the solubility of glibenclamide. It was observed t...