Structure-activity relationship fungicides

Data in Table VI support the following structure-activity relationships fungicidal activity roughly... 

Synthesis-Directing Structure-Activity Relationships of Some Fungicides Inhibiting Ergosterol Biosynthesis... 

The recent reviews by Jager (11) and Kramer et al (12) describe the synthetic routes and biological activity of selected tritylimidazoles, trityltriazoles and other variously substituted N-azole fungicides. The information that follows will describe certain structural activity relationships of selected EBI fungicides containing pyridine and pyrimidine heterocyclic moieties. 

This model was then used to suggest new structure activity relationships and contribute towards novel fungicide design. 

Akagi, T., Mitani, S., Komyoji, T. and Nagatani, K. (1995). Quantitative Structure-Activity Relationships of Fluazinam and Related Fungicidal N-Rhenylpyridinamines Preventive Activity Against Botrytis Cinerea. J.Pestic.Sci.,20,279-290. 

Miyashita, Y, Ohsako, H., Takayama, C. and Sasaki, S. (1992). Multivariate Structure-Activity Relationships Analysis of Fungicidal and Herbicidal Thiocarbamates Using Partial Least Squares Method. Quant.Struct.-Act.Relat, 11,17-22. 

Singh, N., Gupta, R.L. and Roy, N.K. (1996). Synthesis and Quantitative Structure-Activity Relationships of Aryl-2-Chloroethyl-Methyl Phosphate Fungicides. Indian l.Chem.,35B, 697-702. 

Silylmethyltriazoles represent a new, highly active class of triazole fungicides, whose success in a wide variety of crops and climatic conditions confirms the utility of organosilicon compounds as agrichemicals. This paper describes their discovery, synthesis, and structure-activity relationships. Based on the results of worldwide field evaluations, some of which are presented, a member of this class, DPX-H6573, is being developed as a broad spectrum foliar fungicide. 

Exploration of the area of imidazole-l-carboxamides has led to the discovery of prochloraz, a broad-spectrum fungicide for use on a variety of crops. Prochloraz and its analogues are inhibitors of ergosterol biosynthesis and structure-activity relationships in the area are discussed. In particular, the usefulness of an in vitro assay for sterol biosynthesis as a guide to the chemical effort is considered. Finally, the biological activity of prochloraz is briefly described. 

S. (1992) Multivariate structure-activity relationships analysis of fungicidal and herbiddal thiocarbamates using partial least squares method. Quant. Struct. -Act. Relat., 11, 17—22. 

Other pharmacological activities have also been correlated with quantum-chemically derived descriptors. For instance, the quantitative structure-activity relationship developed for the antibacterial activity of a series of monocyclic (i-lactam antibiotics included the atomic charges, the bond orders, the dipole moment, and the first excitation energy of the compound [103]. The fungicidal activity of A3-l,2,4-thiadiazolines has been correlated with an index of frontier orbital electron density derived from semi-empirical PM3 molecular orbital calculations [104],... 

In this chapter, a rationale of the structure-activity relationships of various series of bioactive secondary metabolites from Indo-Pacific marine invertebrates is reviewed. These include alkaloids, terpenes and polybrominated diphenyl ethers which were subjected to a series of bioassays in search for insecticidal, antibacterial, fungicidal, and cytotoxic lead compounds. From these various biotests, it was observed that the bioactivity of an analogue is not due to general toxicity but rather possesses a degree of specificity on a particular target biomolecule. The relationship between chemical structures and biological activity is related to the specific action of a compound. 

Structure-activity Relationships of Antidotes to Benzimidazole Fungicides... 

There, the fungicidal activity was detected and an optimization program carried out [88] that finally led after three years of work and the preparation of over 700 analogs [88b] to an optimized structure, famoxadone for patents see [89]. In-vivo structure-activity relationships have been reported with the oomycetes Phy-tophthora infestans and Plasmopara viticola [88]. Famoxadone was announced in 1996 as a broad spectrum fungicide for the control of diseases caused by Ascomy-cetes and Basidiomycetes in various crops and particularly against downy mildew diseases caused by oomycetes in potato, vines and vegetables [90]. 

Structure-activity relationship (SAR) studies, correlating preventive fungicidal potency against wheat brown rust and barley powdery mildew, have been described only for special subclasses of N-benzyl-4-pyrimidine-amines [19, 20]. 

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