Trehalose-6-phosphate-potent anti-onchocerciatic agent

Area of Science:

• * Parasitology
• * Medicinal Chemistry
• * Drug Discovery

Background:

• * Onchocerciasis remains a significant global health concern with a need for improved therapeutic agents.
• * Current treatments for onchocerciasis (river blindness) have limitations, necessitating the development of new drugs.

Purpose of the Study:

• * To synthesize and evaluate alpha, alpha-trehalose-6-phosphate as a potential agent against Onchocerca volvulus.
• * To compare the efficacy of alpha, alpha-trehalose-6-phosphate with diethylcarbamizine citrate, a standard control drug.

Main Methods:

• * Synthesis of alpha, alpha-trehalose-6-phosphate.
• * In vitro assessment of micro and macro-filaricidal activity against Onchocerca volvulus.
• * Comparative analysis with diethylcarbamizine citrate.

Main Results:

• * Alpha, alpha-trehalose-6-phosphate demonstrated significant micro and macro-filaricidal activity.
• * The compound exhibited superior efficacy compared to the control drug, diethylcarbamizine citrate.
• * Inhibition of the enzyme trehalase is proposed as the mechanism of action.

Conclusions:

• * Alpha, alpha-trehalose-6-phosphate is an effective glucose analogue and a potent filaricidal agent.
• * This compound holds potential for the eradication of onchocerciasis in both human and animal populations.
• * Further research into structure-activity relationships supports its therapeutic promise.