Call For Paper Volume:6 Issue:11 Nov'2019 |

SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AGENTS

Publication Date : 13/09/2017


DOI : 10.21884/IJMTER.2017.4274.UKPDH

Author(s) :

Jagadeesh Kumar Ega , Kavitha Siddoju .


Volume/Issue :
Volume 4
,
Issue 9
(09 - 2017)



Abstract :

Malaria is very common parasitic diseases of the developing world and drug resistance has hindered their efficient control. Pyrazole derivatives were synthesized using aldol condensation and subsequent cyclization reactions. The intermediate α, β unsaturated ketones, (2 and 3) were synthesized by aldol condensation of 1-phenyl-3-p-tolyl-1H-pyrazole-4-carbaldehyde I with 2-acetylthiophene and acetophenone respectively in alcoholic KOH. The target thienyl and phenyl pyrazolines were synthesized by cyclization of the intermediate α, β unsaturated ketones (2 and 3) with hydrazine hydrate in ethanol or the appropriate aliphatic acid. The compounds were synthesized in a good yield (71.39%-95.23%). The compounds were purified by recrystallization and their chemical structure was characterized by elemental microanalysis, IR, and 1HNMR spectroscopy. In vivo antimalarial was conducted using four day suppression test and Alamar blue reduction method, respectively. The results for antimalarial activity conducted using P. berghei infected mice at a dose level of 48.46µmol/kg/day showed that all the synthesized compounds have lower activity than the standard drug chloroquine phosphate. Compound 2c, 1-phenyl-4-(3-(thiophen-2-yl)-4,5-dihydro-1H-pyrazol-5-yl)-3-p-tolyl-1H-pyrazole, showed relatively the highest % suppression, 63.40%.


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SYNTHESIS AND BIOLOGICAL SCREENING OF SOME PYRAZOLE DERIVATIVES AS ANTIMALARIAL AGENTS

September 7, 2017