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Molecular
Modelling & Structure-Activity Relationships of
4-Amino-mono and bis-Quinolines: Novel Antimalarials with
Activity in vitro
and in
vivo
Research team: Dr F M D Ismail, M
J Dascombe, S. Alizadeh-Shekalgourabi,Prof. M. G. B. Drew, W. A. Moule, and V. Male
Programme of studies: This project
involves the synthesis of novel bisquinoline antimalarials,
including those related to metaquine, many of which
demonstrate activity against the K1 mult-drug resistant strain
of P. falciparum (collaborative project with Prof.
Wilairat, Dept. of Biochemistry, Mahidol) and activity in
vivo against P. berghei. Currently, projects are available
to synthesise rationally designed antimalarials molecules
which conform to our unpublished bisquinoline receptor
map. Ref: a) F. M. D. Ismail, M. J. Dascombe, P. Carr and
S. E. North An exploration of the structure-activity
relationships of 4-aminoquinolines: Novel antimalarials with
activity in-vivo:Journal of Pharmacy and Pharmacology, August
1996, Vol 48 (8), pp 841-850; b) Ismail FMD, Dascombe MJ, Carr
P, Merette SAM, Rouault P Novel aryl-bis-quinolines with
antimalarial activity in-vivo: Journal of Pharmacy and
Pharmacology 50 (5): 483-492 MAY 1998
Medicines
for Malaria Venture
Ref: Synthesis and Biological Activity of novel
antimalarials. S. Alizadeh-Shekalgourabi. (2001) Ph.d Thesis,
in progress. |
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