Translaminar redistribution is valuable for fungicide activity but difficult to measure and predict. The translaminar activity of 38 fungicides active against cucumber powdery mildew was measured experimentally and used to develop a QSAR (Quantitative structure-activity relationship) model of translaminar movement from calculated parameters. Over 300 physiochemical parameters generated from energy-minimized 3D structures were considered and one-parameter, two-parameter, and five-parameter models were developed.
View Article and Find Full Text PDFThe relentless need for the discovery and development of new agrochemicals continues as a result of driving forces such as loss of existing products through the development of resistance, the necessity for products with more favorable environmental and toxicological profiles, shifting pest spectra, and the changing agricultural needs and practices of the farming community. These new challenges underscore the demand for novel, high-quality starting points to accelerate the discovery of new agrochemicals that address market challenges. This article discusses the efforts to identify the optimum ranges of physicochemical properties of agrochemicals through analysis of modern commercial products.
View Article and Find Full Text PDFDrug Discov Today
January 2015
Twelve drugs from four chemical classes are currently available for treatment of systemic fungal infections in humans. By contrast, more than 100 structurally distinct compounds from over 30 chemical classes have been developed as agricultural fungicides, and these fungicides target many modes of action not represented among human antifungal drugs. In this article we introduce the diverse aspects of agricultural fungicides and compare them with human antifungal drugs.
View Article and Find Full Text PDFPestic Biochem Physiol
November 2013
Translaminar redistribution is a key component of activity for many fungicides. The influence of physical properties (including water solubility, lipophilicity, melting point, and molar volume) on translaminar activity, however, is not well understood. Cucumber powdery mildew was used as a biological indicator to examine the influence of physical properties on translaminar activity of 61 fungicides in simple, uniform formulations, including three modes-of-action and a range of physical properties.
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