Drug intelligence / Profile preview

acetyl sulfisoxazole

Development stage
Unknown
Lead developer
Roche
Modality
Orthosteric Ligands → Classical Binding Small Molecules → Small Molecules
Administration
Oral
01

Overview

Acetyl sulfisoxazole is an ester prodrug of the sulfonamide antibiotic sulfisoxazole. It is a synthetic analog of para-aminobenzoic acid (PABA) and acts as a broad-spectrum antibacterial agent. The drug works by competing with PABA for the bacterial enzyme dihydropteroate synthase, thereby inhibiting the incorporation of PABA into dihydrofolic acid—the precursor to folic acid. This inhibition blocks bacterial folic acid synthesis and de novo synthesis of purines and pyrimidines, resulting in cell growth arrest and death. Acetylation makes the compound less water-soluble; it is hydrolyzed in vivo to active sulfisoxazole after oral administration. Acetyl sulfisoxazole is often used in combination with erythromycin for treating acute otitis media caused by *Haemophilus influenzae*[1][2][3][5][6].

Brand names
GantrisinLipo Gantrisin
Other names
sulfisoxazole acetylacetylsulfafurazole80-74-0
02

Targets

DHPS (Dihydropteroate synthase)

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