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Synthesis and Bioactivity of Novel N , N′ ‐Diacylhydrazine Derivatives Containing Furan (II)
Author(s) -
Li Xichen,
Yang Xinling,
Cui Zining,
Li Ying,
He Hongwu,
Ling Yun
Publication year - 2010
Publication title -
chinese journal of chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.28
H-Index - 41
eISSN - 1614-7065
pISSN - 1001-604X
DOI - 10.1002/cjoc.201090214
Subject(s) - chemistry , furan , bioassay , stereochemistry , ecdysone , proton nmr , organic chemistry , hormone , biochemistry , genetics , biology
Diacylhydrazines have been found as molting hormone analogs since RH‐5849 was reported as the first nonsteroidal ecdysone agonist in 1988. Optimizations on diacylhydrizines with benzoheterocycle containing oxygen were widely explored in recent years. In order to find novel compounds with high bioactivity, a series of mono‐ ( I ) and di‐acylhydrazine ( II ) derivatives containing furan were designed and synthesized. Their structures were confirmed by 1 H NMR, IR, elemental analyses and single crystal X‐ray diffraction analyses ( II 7 ). The bioassay results showed that some of the mono‐acylhydrazine ( I ) derivatives exhibited good larvicidal activity against Culex pipiens pallens at 10 mg/L and better than those of di‐acylhydrazines ( II ). Generally, the anti‐tumor activity of di‐acylhydrazines ( II ) was better than that of mono‐acylhydrazines ( I ).