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 59
- Downloads 0
VALIDATED HIGH PERFORMANCE LIQUID CHROMATOGRAPHY (HPLC) METHOD FOR ANALYSIS OF METHAMPHETAMINE IN HUMAN URINE USING LIQUID-LIQUID EXTRACTION
 Objective: Methamphetamine (also known as pil kuda or syabu) is one of the illicit drugs, which are common among students and teenagers. InMalaysia, methamphetamine was found to be the most commonly abused amphetamine-...
Challenges and Opportunities of Nuclear Medicine in Health Care
AERB Sponsored National Seminar Challenges and Opportunities of Nuclear Medicine in Health Care (Saturday 02 February 201 Organized by-Chameli Devi Institute of Pharmacy, Indore
ALTERED AUTONOMIC BALANCE IN NORMAL TENSION GLAUCOMA
Objective: To study autonomic imbalance if any in normal tension glaucoma (NTG)patients by heart rate variability (HRV)and head-up tilt (HUT)test.Methods: The study subjects of age between 45 and 65 years of either sex c...
DEVELOPMENT AND VALIDATION OF NEW STABILITY INDICATING REVERSED-PHASE HIGH-PERFORMANCE LIQUID CHROMATOGRAPHY METHOD FOR SIMULTANEOUS DETERMINATION OF METFORMIN HYDROCHLORIDE AND ERTUGLIFLOZIN IN BULK AND PHARMACEUTICAL DOSAGE FORM
Objective: The present study deals with the development, validation, and application of simple, precise, and accurate high-performance liquid chromatography (HPLC) method for the simultaneous estimation of metformin hydr...
Synthesis and anti–microbial activity of 1,2,3–triazole tethered nitroguiacol ethers
Nitro aromatic/nitrophenols have been widely distributed in nature and are mostly isolated from marine microorganisms and had shown a broad spectrum of anti–microbial activities against a wide range of microbial pathog...