THE EFFECT OF FLUORINE SUBSTITUTION ON THE HAEMOTOXICITY OF PRIMAQUINE

Authors
ONEILL PM TINGLE MD MAHMUD R STORR RC WARD SA PARK BK
Citation
Pm. Oneill et al., THE EFFECT OF FLUORINE SUBSTITUTION ON THE HAEMOTOXICITY OF PRIMAQUINE, Bioorganic & medicinal chemistry letters, 5(20), 1995, pp. 2309-2314
Citations number
26
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
20
Year of publication
1995
Pages
2309 - 2314
Database
ISI
SICI code
0960-894X(1995)5:20<2309:TEOFSO>2.0.ZU;2-Z
Abstract
5-Fluoro-6-methoxy-8-nitroquinoline was synthesised by a modified Skra up Reaction and was subsequently converted into 5-fluoroprimaquine in three steps. 5-Fluoroprimaquine 9 is less susceptible to in vitro bioa ctivation than primaquine 1 in a range of different species. However, significant bioactivation of 9 was observed with hepatic microsomes fr om two species including man.