Design, Synthesis, and Biological Activity of Silicon-Containing Carboxamide Fungicides.

Bioisosteric silicon replacement has proven to be a valuable strategy in the design of bioactive molecules for crop protection and drug development. Twenty-one novel carboxamides possessing a silicon-containing biphenyl moiety were synthesized and tested for their antifungal activity and succinate dehydrogenase (SDH) enzymatic inhibitory activity. Among these novel succinate dehydrogenase inhibitors (SDHIs), compounds , , and possessing appropriate log and topological polar surface area values showed excellent inhibitory effects against , , , and at 10 mg/L in vitro, and the EC values of and were 0.

Synthesis and Biological Activity of Silicon-Containing Ethylsulfonylpyridine Insecticides.

Ethylsulfonylpyridines are a novel chemical class of insecticides with excellent broad-spectrum activity and an unprecedented mode of action. With the objective of discovering novel ethylsulfonylpyridines with a broader spectrum, wider range of uses, and/or improved properties, we have started a research program aimed at introducing silicon motifs and studying their biological effects. We designed a series of Oxazosulfyl analogues where the hydrogen atom at the 5-position of the pyridyl moiety is replaced by a trialkylsilyl group and prepared these compounds applying denovo synthetic methodology.

Design, Synthesis, and Properties of Silicon-Containing -Diamide Insecticides.

Silicon-containing compounds are sporadically used in crop protection and drug discovery and have demonstrated to increase the biological efficacy as well as to reduce toxicity, improve physicochemical properties, and favorably impact the environmental profile. As part of our research, we have investigated the application of bioisosteric silicon replacements in -diamide insecticides and studied the biological activity and molecular properties of the corresponding novel compounds. At all meaningful structural elements of the -diamides, silicon-containing substituents were introduced and synthetic methodology was developed for their syntheses.

Silicon-Containing Complex II Acaricides─Design, Synthesis, and Pharmacological Optimization.

Bioisosteric replacement has been proven to be a powerful strategy in life science research. In this review, general aspects of carbon-silicon bioisosteric substitution and its applications in pharmaceutical and crop protection research are described. Carbon and their silicon analogues possess similar intrinsic properties.