SYNTHESES OF UNUSUAL BIOLOGICALLY ACTIVE TERPENES

不寻常的生物活性萜烯的合成

• 批准号: 3278722
• 负责人: LEO A PAQUETTE
• 金额: $ 16.66万
• 依托单位: OHIO STATE UNIVERSITY
• 依托单位国家: 美国
• 财政年份: 1983
• 资助国家: 美国
• 起止时间: 1983-04-01 至 1991-03-31
• 项目状态: 已结题
• 来源: https://reporter.nih.gov/project-details/3278722
• 关键词: antibiotics; antifungal agents; antileukemic agent; antineoplastics; beta lactam antibiotic; diterpenes; drug design /synthesis /production; drug metabolism; sesquiterpenes; terpenes; tumor promoters

Protocols are offered by which ongoing synthetic efforts should culminate in the acquisition of: (a) pleuromutilin, a diterpene antibiotic produced by several basidiomycetes; (b) sterpuric acid, a sesquiterpenoid metabolite of the fungus Stereum purpureum; and (c) 3Beta-hydroxy-7Beta-kemp-8(9)-en-6-one, a cembrene-derived diterpene produced by nasute termite soldiers. In addition, new efforts are outlined for the purpose of developing new methodologies that will culminate in the laboratory preparation of: (d) acetoxycrenulide, a unique bicyclic cyclopropane-containing diterpenoid exuded by small brown phaeophyta; (e) 7,8-epoxy-4-basmen-6-one, a tricyclic diterpenoid of unusual structure produced by certain types of Oriental tobacco; (f) jatrophatrione, a tricyclic triketo diterpene possessing a 5/9/5-fused ring skeleton that exhibits good inhibitory activity toward the P-388 (3PS) lymphocytic leukemia test system; (g) neolemnanyl acetate, an irregular sesquiterpene produced by the Pacific soft coral Lemnalia africana; (h) cerorubenic acid-III, a kairomone secreted by Ceroplastes rubens recognized for its ability to control the ovipositional behavior of certain insects; and (i) punctatin A, a product of the dung fungus Poronia punctata that is reputed for its antibiotic activity.

提供了正在进行的合成努力应该达到顶峰的协议 在获得：(A)截胸素，一种产生的二萜抗生素 由几种担子菌产生；(B)倍半萜代谢物斯特普酸 )；及(C) 3β-羟基-7-β-Kemp-8(9)-烯-6-酮，一种来自西红花的二萜 由初生白蚁士兵生产。此外，还概述了新的努力。 为了开发新的方法论，最终将 一种独特的双环化合物：(D)乙酰氧基奎尼特的实验室制备 小型棕色褐藻分泌的含环丙烷二萜；(E) 7，8-环氧基-4-碱基-6-酮，一种结构特殊的三环二萜 由某些类型的东方烟草生产；(F)马托菲酮，a 具有5/9/5-稠环骨架的三环三酮二萜， 对P-388(3PS)淋巴细胞具有良好的抑制活性 白血病检测系统；(G)乙酸新龙脑酯，一种不规则倍半萜 由太平洋软珊瑚Lemnalia africana生产；(H)Cerorubenic ACID-III，一种由Ceroplastes Rubens分泌的凯旋酮，因其 控制某些昆虫产卵行为的能力；及(I) 斑点菌素A，一种著名的粪便真菌斑点孔菌的产品 因为它的抗菌活性。