Bennett G A, Mullen G B, DeCory T R, Maryniak D M, Jones W E, Mitchell J T, Allen S D, St Georgiev V
Arch Pharm (Weinheim). 1989 Sep;322(9):531-4. doi: 10.1002/ardp.19893220904.
The synthesis and antifungal activity of a series of novel 5-carbonyl derivatives of 3-phenyl-3-(1H-imidazol-1-ylmethyl)-2-methylisoxazolidines (4) are discussed. The preparation of the title compounds involved a 1,3-dipolar cycloaddition reaction of alpha-substituted ketonitrones with either acrylic esters, acrylamide or methyl vinyl ketone to furnish cis/trans-diastereomeric mixtures of the desired 5-carbonyl isoxazolidines 4. The anifungal activity was evaluated in vitro in solid agar cultures. Some of the compounds tested exerted moderate to potent activity against a wide variety of dermatophytes and yeast and systemic fungi.
讨论了一系列新型3-苯基-3-(1H-咪唑-1-基甲基)-2-甲基异恶唑烷-5-羰基衍生物(4)的合成及其抗真菌活性。标题化合物的制备涉及α-取代酮亚胺与丙烯酸酯、丙烯酰胺或甲基乙烯基酮的1,3-偶极环加成反应，以提供所需的5-羰基异恶唑烷4的顺式/反式非对映异构体混合物。在固体琼脂培养物中体外评估了抗真菌活性。所测试的一些化合物对多种皮肤癣菌、酵母菌和全身性真菌表现出中度至强效活性。
