Trehalose-6-phosphate-potent anti-onchocerciatic agent.
Onchocerciasis is a disease that engages the attention of most researchers. Presently, there is not an ideal onchocerciatic agent, hence the search must continues. Consequently alpha, alpha-trehalose-6-phosphate was synthesised and assessed for onchocerciatic activity against O. volvulus; using diethylcarbamizine citrate as the control drug. Results from this study showed that alpha, alpha-trehalose-6-phosphate is a glucose analogue with effective micro and macro-filaricidal agent, better than that of the control drug. The inhibitory action of this compound on enzyme trehalase is a postulate for the mechanism of action of trehalose-6-phosphate. The structure-activity relationship of this new compound is fully discussed. This study postulates that this compound could be used to eradicate onchocerciasis both in man and animals.
Oke
J M
JM
London School of Pharmacy, University of London.
Watt
R A
RA
D000818:Animals; D004049:Diethylcarbamazine / Q000494:pharmacology / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004353:Drug Evaluation, Preclinical; D005369:Filaricides / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D006593:Hexokinase / Q000037:antagonists & inhibitors*; D008297:Male; D017181:Onchocerca volvulus / Q000201:enzymology; D009855:Onchocerciasis / Q000188:drug therapy* / Q000201:enzymology / Q000469:parasitology; D013403:Sugar Phosphates / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D014198:Trehalase / Q000037:antagonists & inhibitors*; D014199:Trehalose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use
D005369:Filaricides; D013403:Sugar Phosphates; C082722:trehalose-6-phosphate; D014199:Trehalose; D006593:Hexokinase; D014198:Trehalase; D004049:Diethylcarbamazine