Antifungal Activity of Artemisinin Derivatives

• Published in: Journal of natural products (Washington, D.C.) Vol. 68; no. 8; pp. 1274 - 1276
• Main Authors: Galal, Ahmed M, Ross, Samir A, Jacob, Melissa, ElSohly, Mahmoud A
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 01.08.2005; Amer Chemical Soc; American Society of Pharmacognosy
• Subjects: animal pathogenic fungi; Antibiotics. Antiinfectious agents. Antiparasitic agents; Antifungal agents; Antifungal Agents - chemical synthesis; Antifungal Agents - chemistry; Antifungal Agents - pharmacology; antifungal properties; artemisinin; Artemisinins - chemical synthesis; Artemisinins - chemistry; Artemisinins - pharmacology; Biological and medical sciences; Candida albicans; Candida albicans - drug effects; chemical structure; Chemistry, Medicinal; Combinatorial Chemistry Techniques; Cryptococcus neoformans; Cryptococcus neoformans - drug effects; Life Sciences & Biomedicine; Medical sciences; Microbial Sensitivity Tests; Molecular Structure; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Plant Sciences; Science & Technology; spectral analysis; stereochemistry; ANTIMALARIAL ACTIVITY; Candida albicans; Endoperoxide; Terpenoid; Cryptococcus neoformans; Artemisinin; Tricyclic compound; Oxygen heterocycle; In vitro; Fungi; Peracetal; Antifungal agent; Structure activity relation; Sesquiterpenes; Fungi Imperfecti; Organic peroxide; Thallophyta
• ISSN: 0163-3864; 1520-6025
• DOI: 10.1021/np050074u

A series of 29 artemisinin derivatives (2−30), including four new compounds (16−18, 20), together with artemisinin (1), artemisinic acid (31), and arteannuin B (32), were tested for antifungal activity against two opportunistic pathogens, Candida albicans and Cryptoccocus neoformans. Of all the compounds tested, anhydrodihydro-artemisinin (3) demonstrated more potent antifungal activity against C. neoformans than amphotericin B. Also, β-arteether (7) and α-arteether (8) showed marked activity against C. neoformans. Against C. albicans, the overall antifungal effect of these compounds was weak or negligible. Derivatives 2−30 were prepared according to literature procedures.