Bioactivity-guided mixed synthesis accelerate the serendipity in lead optimization: Discovery of fungicidal homodrimanyl amides

The bioactivity-guided mixed synthesis was conceived, in which the designed mix-reactions were run in parallel for simultaneous construction of different kinds of analogs. The valuable ones were protruded by biological screening. This tactic will facilitate more rapid incorporation of bioactive cand...

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Veröffentlicht in:European journal of medicinal chemistry 2017-08, Vol.136, p.114-121
Hauptverfasser: Li, Dangdang, Zhang, Shasha, Song, Zehua, Wang, Guotong, Li, Shengkun
Format: Artikel
Sprache:eng
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Zusammenfassung:The bioactivity-guided mixed synthesis was conceived, in which the designed mix-reactions were run in parallel for simultaneous construction of different kinds of analogs. The valuable ones were protruded by biological screening. This tactic will facilitate more rapid incorporation of bioactive candidates into pesticide chemists' repertoire, exemplified by the optimization of less explored homodrimanes as antifungal ingredients. The discovery of D9 as a potent fungicidal agent can be completed in
ISSN:0223-5234
1768-3254
DOI:10.1016/j.ejmech.2017.04.073