The effect of fluorine substitution on the haemotoxicity of Primaquine

Paul M. O'Neill; Malcolm D. Tingle; Roziahanim Mahmud; Richard C. Storr; Steve Ward; B. Kevin Park

doi:10.1016/0960-894x(95)00400-n

The effect of fluorine substitution on the haemotoxicity of Primaquine

Paul M. O'Neill, Malcolm D. Tingle, Roziahanim Mahmud, Richard C. Storr, Steve Ward, B. Kevin Park

University of Liverpool

Research output: Contribution to journal › Article › peer-review

11 Citations (Scopus)

Abstract

5-Fluoro-6-methoxy-8-nitroquinoline was synthesised by a modified Skraup Reaction and was subsequently converted into 5-fluoroprimaquine in three steps. 5-Fluoroprimaquine 9 is less susceptible to in vitro bioactivation than primaquine 1 in a range of different species. However, significant bioactivation of 9 was observed with hepatic microsomes from two species including man.

Original language	English
Pages (from-to)	2309-2314
Number of pages	6
Journal	Bioorganic & Medicinal Chemistry Letters
Volume	5
Issue number	20
DOIs	https://doi.org/10.1016/0960-894x(95)00400-n
Publication status	Published - 19 Oct 1995
Externally published	Yes

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Cite this

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title = "The effect of fluorine substitution on the haemotoxicity of Primaquine",

abstract = "5-Fluoro-6-methoxy-8-nitroquinoline was synthesised by a modified Skraup Reaction and was subsequently converted into 5-fluoroprimaquine in three steps. 5-Fluoroprimaquine 9 is less susceptible to in vitro bioactivation than primaquine 1 in a range of different species. However, significant bioactivation of 9 was observed with hepatic microsomes from two species including man.",

author = "O'Neill, \{Paul M.\} and Tingle, \{Malcolm D.\} and Roziahanim Mahmud and Storr, \{Richard C.\} and Steve Ward and \{Kevin Park\}, B.",

year = "1995",

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doi = "10.1016/0960-894x(95)00400-n",

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journal = "Bioorganic \& Medicinal Chemistry Letters",

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T1 - The effect of fluorine substitution on the haemotoxicity of Primaquine

AU - O'Neill, Paul M.

AU - Tingle, Malcolm D.

AU - Mahmud, Roziahanim

AU - Storr, Richard C.

AU - Ward, Steve

AU - Kevin Park, B.

PY - 1995/10/19

Y1 - 1995/10/19

N2 - 5-Fluoro-6-methoxy-8-nitroquinoline was synthesised by a modified Skraup Reaction and was subsequently converted into 5-fluoroprimaquine in three steps. 5-Fluoroprimaquine 9 is less susceptible to in vitro bioactivation than primaquine 1 in a range of different species. However, significant bioactivation of 9 was observed with hepatic microsomes from two species including man.

AB - 5-Fluoro-6-methoxy-8-nitroquinoline was synthesised by a modified Skraup Reaction and was subsequently converted into 5-fluoroprimaquine in three steps. 5-Fluoroprimaquine 9 is less susceptible to in vitro bioactivation than primaquine 1 in a range of different species. However, significant bioactivation of 9 was observed with hepatic microsomes from two species including man.

U2 - 10.1016/0960-894x(95)00400-n

DO - 10.1016/0960-894x(95)00400-n

M3 - Article

VL - 5

SP - 2309

EP - 2314

JO - Bioorganic & Medicinal Chemistry Letters

JF - Bioorganic & Medicinal Chemistry Letters

IS - 20

ER -

The effect of fluorine substitution on the haemotoxicity of Primaquine

Abstract

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