Synthesis of 5-Keto-5-oxime Derivatives of Milbemycins and Their Activities against Microfilariae
Year: 1991
Type: article
Abstract: Starting from milbemycin D (1), milbemycin A4 (2) and milbemycin A3 (3), a series of 5-keto-5-oxime derivatives were synthesized by selective oximation at the alpha,beta-conjugated carbonyl function of the 5-ketomilbemycins (4-6). The activities of the synthesized compounds were studied in dogs naturally infested with microfilariae of Dirofilaria immitis. The 5-keto-5-oximes of milbemycin D (7), A4 (8) and A3 (9) had quite high efficacy to control the microfilariae and more potency than their parents, while the 5-O-acyl oximes (11-15) also exhibited high activity.
Authors: Yoshihisa Tsukamoto, Kazuo Sato, Shigeru Mio, Soji Sugai, Toshiaki Yanai, Noritoshi Kitano, Shigeki Muramatsu, Yasuo Nakada, Junya Ide
Language: English
Subfield: Infectious Diseases
Field: Medicine
Domain: Health Sciences
Open Access status: bronze
Funder: Daiichi Sankyo Company
OpenAlex ID: W2056864085