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INTERNATIONAL JOURNAL OF PHARMACEUTICAL RESEARCH

A Step Towards Excellence
Published by : Advanced Scientific Research
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0975-2366
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IJPR 9[3] July - September 2017 Special Issue

July - September 9[3] 2017

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Synthesis and Biological Activity of Some Quinolino Pyrazole Derivatives

Author: SHILPI SONKER, DR.DEVENDERPATHAK
Abstract: A new series of pyrazole based quinoline were synthesized and evaluated for antimalarial and antibacterial activity. The rationale behind the synthesis of new series of quinolino pyrazoles (4a-4e) and (4a’-4e’) is in order to discover a new molecule which leads to dual anti-malarial–antimicrobial agents. The synthesized novel compounds were screened for their anti-malarial activity using Vero cell line (C1008; Monkey kidney fibroblast) against Plasmodium falciparum (3D7 strain) with the Chloroquine diphosphate and SI was measured by using IC50 and CC50 of compound. The results revealed that compounds 4c, 4e, 4a’ and 4e’ showed higher efficacies and potencies for anti-malarial activity comparable to the reference standard Chloroquine diphosphate. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity against two gram positive, gram negative and antifungal strain. Four compounds 4c, 4e, 4a’ and 4d’showed considerable broad spectrum activity against all the tested Gram-positive and Gram-negative bacterial strains as well as displayed significant antifungal activity.
Keyword: Chalcones, Pyrazoles, Sulfonamides, Plasmodium falciparum, Antimalarial activity, Antimicrobial activity, SYBR Green-I (Invitrogen)
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