EUROPEAN JOURNAL OF
PHARMACEUTICAL AND MEDICAL RESEARCH

An International Peer Reviewed Journal for Pharmaceutical, Medical & Biological Sciences

An Official Publication of Society for Advance Healthcare Research (Reg. No. : 01/01/01/31674/16)

European Journal of Pharmaceutical and Medical Research (EJPMR) has indexed with various reputed international bodies like : Google Scholar , Indian Science Publications , InfoBase Index (In Process) , SOCOLAR, China , Research Bible, Fuchu, Tokyo. JAPAN , International Society for Research activity (ISRA) , Scientific Indexing Services (SIS) , Polish Scholarly Bibliography , Global Impact Factor (GIF) (Under Process) , Universal Impact Factor , International Scientific Indexing (ISI), UAE  , Index Copernicus , CAS (A Division of American Chemical Society) USA (Under Process) , Directory of Open Access Journal (DOAJ, Sweden, in process) , UDLedge Science Citation Index , CiteFactor , Directory Of Research Journal Indexing (DRJI) , Indian citation Index (ICI) , Journal Index (JI, Under Process) , Directory of abstract indexing for Journals (DAIJ) , Open Access Journals (Under Process) , Impact Factor Services For International Journals (IFSIJ) , Cosmos Impact Factor , Jour Informatics (Under Process) , Eurasian Scientific Journal Index (ESJI) , International Innovative Journal Impact Factor (IIJIF) , Science Library Index, Dubai, United Arab Emirates , Pubmed Database [NLM ID: 101669306] (Under Process) , IP Indexing (Under Process) , 

 ISSN 2394-3211

Impact Factor: 4.897

 ICV - 79.57

Abstract

SYNTHESIS AND ANTIPLASMODIAL EVALUATION OF A NEW TRIOXAQUINE

Hannah N. Wamakima, Peter G. Kirira, Margaret M. Nganga, Winnie R. Gimode, Brendon Naicker, Matshawendile Tukulula and Francis W. Muregi*

ABSTRACT

The ultimate objective of this work was to develop a novel antimalarial hybrid drug based on quinoline and trioxane pharmacophoric scaffold that is effective against drug-resistant malaria, especially in the face of emerging resistance against artemisinin based combination therapy (ACT). The synthetic design involved introduction of a linker to 4,7-dichloroquinoline and subsequent coupling with artesunate to form the dual drug. The structure’s molecular formula C30H38N3ClO7 was confirmed by electron spray ionization mass spectrum that showed a molecular ion peaks at m/z 588.24 and 590.24 amu with a relative abundance of 100% and 38.8% respectively against an exact value of 587.24 amu. Through biological studies, it was established that the drug’s antiplasmodial activity (IC50) against chloroquine (CQ)-sensitive (CQS, D6) and CQ-resistant (CQR, W2) isolates (CQS, 6.89 ng mL-1; CQR, 3.62 ng mL-1) was comparable (p>0.05) to that of artesunate (CQR, 6.67 ng mL-1; CQR, 4.04 ng mL-1), currently the most potent antimalarial in the artemisinin family. The drug had a good safety profile, with low percentage inhibition of human HeLa cell proliferation (29%), and IC50 values >10 000 ng mL-1. The findings validate the concept of ‘‘covalent bitherapy’’ as a feasible strategy in antimalarial drug development.

Keywords: Malaria, Drug resistance, Hybrid drug, Covalent biotherapy.


[Full Text Article]

INDEXING

NEWS & UPDATION

  • New Issue Published

    Its Our pleasure to inform you that, EJPMR 1 October 2018 Issue has been Published, Kindly check it on http://www.ejpmr.com/home/current_issues

  • EJPMR OCTOBER ISSUE PUBLISHED

    OCTOBER 2018 Issue has been successfully launched on 1 October 2018

  • EJPMR New Impact Factor

    Its our Pleasure to Inform you that EJPMR Impact Factor has been increased from 4.161 to 4.897 due to high quality Publication at International Level

  • Index Copernicus Value

    EJPMR Received Index Copernicus Value 79.57, due to High Quality Publication in EJPMR at International Level

  • Journal web site support Internet Explorer, Google Chrome, Mozilla Firefox, Opera, Saffari for easy download of article without any trouble.

    .

  • Article Invited for Publication

    Article are invited for publication in EJPMR Coming Issue

Google Scholar Indian Science Publications InfoBase Index (In Process) SOCOLAR, China Research Bible, Fuchu, Tokyo. JAPAN International Society for Research activity (ISRA) Scientific Indexing Services (SIS) Polish Scholarly Bibliography Global Impact Factor (GIF) (Under Process) Universal Impact Factor International Scientific Indexing (ISI), UAE Index Copernicus CAS (A Division of American Chemical Society) USA (Under Process) Directory of Open Access Journal (DOAJ, Sweden, in process) UDLedge Science Citation Index CiteFactor Directory Of Research Journal Indexing (DRJI) Indian citation Index (ICI) Journal Index (JI, Under Process) Directory of abstract indexing for Journals (DAIJ) Open Access Journals (Under Process) Impact Factor Services For International Journals (IFSIJ) Cosmos Impact Factor Jour Informatics (Under Process) Eurasian Scientific Journal Index (ESJI) International Innovative Journal Impact Factor (IIJIF) Science Library Index, Dubai, United Arab Emirates Pubmed Database [NLM ID: 101669306] (Under Process) IP Indexing (Under Process)