Exploring boron applications in modern agriculture: A structure-activity relationship study of a novel series of multi-substitution benzoxaboroles for identification of potential fungicides.

Bioorganic & Medicinal Chemistry Letters
Chunliang LiuYong-Kang Zhang

Abstract

Several boron-containing small molecules have been approved by the US FDA to treat human diseases. We explored potential applications of boron-containing compounds in modern agriculture by pursuing multiple research and development programs. Here, we report a novel series of multi-substitution benzoxaboroles (1-36), a compound class that we recently reported as targeting geranylgeranyl transferase I (GGTase I) and thereby inhibiting protein prenylation (Kim et al., 2020). These compounds were designed, synthesized, and tested against the agriculturally important fungal pathogens Mycosphaerella fijiensis and Colletotrichum sublineolum in a structure-activity relationship (SAR) study. Compounds 13, 28, 30, 34 and 36 were identified as active leads with excellent antifungal MIC95 values in the range of 1.56-3.13 ppm against M. fijiensis and 0.78-3.13 ppm against C. sublineolum.

References

Mar 1, 2011·Bioorganic & Medicinal Chemistry Letters·Xianfeng LiJon Wright
Oct 1, 2009·Future Medicinal Chemistry·Stephen J BakerYi Xia
Aug 2, 2017·Nature Chemical Biology·Jeff S PiotrowskiCharles Boone
Jun 24, 2020·ACS Chemical Biology·Sang Hu KimLeah E Cowen

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