2-HYDROXY-4-METHOXYBENZALDEHYDE: LARVICIDAL STRUCTURE-ACTIVITY STUDIES

Abstract

2-Hydroxy-4-methoxybenzaldehyde (1), a compound isolated from Mondia whytei (Hook) Skeels (Asclepiaceae) roots exhibited larvicidal activity (LD₅₀22 mg/mL). A total of 18 other derivatives and closely related congeners revealed varying levels of larvicidal activity. Several closely related congeners, like 2-benzyloxy-4-methoxybenzaldehyde (2), 2-hydroxybenzaldehyde (12), 2-benzyloxybenzaldehyde (3) and benzylphenyl ether (4), showed marked improvement in activity (LD₅₀10, 9, 4.8, 1.2 mg/mL, respectively) against Anopheles gambiae larvae. 2-Benzoyloxy-4-methoxybenzaldehyde (5) exhibited similar activity level (LD₅₀ 28 mg/mL) as 1.



KEY WORDS: 2-Hydroxy-4-methoxybenzaldehyde, Larvicides, Structure-activity relationships, 2-Hdroxybenzaldehyde, 2-Benzyloxybenzaldehyde, Benzylphenyl ether Anopheles gambiae,


Bull. Chem. Soc. Ethiop. 2005, 19(1), 61-68.