Antifungal diterpenoids of Pseudolarix kaempferi, and their structure-activity relationship study.
The in vitro antifungal activities of 19 structurally diversified analogues of pseudolaric acids tested against the major pathogenic fungus Candida albicans has led to the establishment of a very clear structure-activity relationship of pseudolaric acids derivatives. Pseudolaric acid A was first found to be a potent antifungal component comparable with pseudolaric acid B. Among the tested 19 diterpenoids, pseudolaric acids A2 (1), B2 (3), B3 (4) and methyl pseudolarate A2 (2) are new isolates of the root bark of Pseudolarix kaempferi, and their structures were elucidated mainly by 2D-NMR techniques and chemical methods. Compounds 12-19 were first semi-synthesized by efficient routines from pseudolaric acid B.
Yang
Sheng-Ping
SP
State Key Laboratory of Drug Research, Institute of Materia Medica, Shanghai Institute for Biological Sciences, Chinese Academy of Sciences, 555 Zu Chong Zhi Road, Zhangjiang Hi-Tech Park, Shanghai 201203, People's Republic of China.
Dong
Lei
L
Wang
Ying
Y
Wu
Yan
Y
Yue
Jian-Min
JM
D000818:Animals; D000935:Antifungal Agents / Q000737:chemistry* / Q000494:pharmacology*; D002176:Candida albicans / Q000187:drug effects; D004224:Diterpenes / Q000737:chemistry* / Q000302:isolation & purification / Q000494:pharmacology*; D008517:Phytotherapy; D028201:Pinaceae / Q000737:chemistry*; D013329:Structure-Activity Relationship
D000935:Antifungal Agents; D004224:Diterpenes; C058391:pseudolaric acid B; C058390:pseudolaric acid A