PMID: 3773935Oct 1, 1986Paper

Esters of 3,4-dihydroxybenzoic acid, highly effective inhibitors of the sn-glycerol-3-phosphate oxidase of Trypanosoma brucei brucei

Molecular and Biochemical Parasitology
R W GradyA B Clarkson

Abstract

Alkyl esters of 3,4-dihydroxybenzoic acid are inhibitors of the sn-glycerol-3-phosphate oxidase system of Trypanosoma brucei brucei in vitro and have significant trypanocidal activity in vivo when combined with glycerol. While the parent acid has little inhibitory activity in vitro, the esters are highly active with activity increasing as the chain length of the esterifying alcohol increases. The n-dodecyl ester was more than 400 times as active as salicylhydroxamic acid and 15 times more active than the corresponding p-n-alkyloxybenzhydroxamic acid, one of the most active sn-glycerol-3-phosphate oxidase inhibitors previously reported. When combined with glycerol (to block an alternative pathway of glycolysis) and tested in vitro against intact parasites, this ester was 100 times more effective than salicylhydroxamic acid and 10 times more effective than p-n-dodecyloxybenzhydroxamic acid. It was also active against T. b. brucei in mice when combined with glycerol whereas the latter compound was not. Esters of 3,4,5-trihydroxybenzoic acid (gallic acid) were also highly active while those of 2,3-dihydroxybenzoic acid were much less inhibitory and those of 2,5-dihydroxybenzoic acid were inactive. A related compound, 2',4',5'-trihy...Continue Reading

References

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Citations

Jan 1, 1989·Comparative Biochemistry and Physiology. B, Comparative Biochemistry·A B ClarksonR W Grady
Jan 6, 2000·Comparative Biochemistry and Physiology. Part C, Pharmacology, Toxicology & Endocrinology·Y FukaiK Kita
Jul 13, 2002·Parasitology International·Yoshihisa FukaiKiyoshi Kita
Jun 12, 2003·Parasitology International·Yoshisada YabuNobuo Ohta
Jan 1, 1989·Parasitology·A H Fairlamb
Dec 27, 2011·Acta Crystallographica. Section E, Structure Reports Online·Xu-Ji ShenXiao-Hui Zheng
Oct 15, 1995·European Journal of Biochemistry·M H HoefnagelP R Rich
Nov 18, 2005·Parasitology International·Yoshisada YabuNobuo Ohta
Feb 26, 2015·The FEBS Journal·Somchart MaenpuenPimchai Chaiyen
Jun 27, 2002·Biochimica Et Biophysica Acta·Coichi NiheiKiyoshi Kita

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