Agrochemicals azoles

A considerable amount of data concerning actual or suggested applications of various types of oxa/thia-2-azoles has appeared mainly in the patent literature. This covers many areas, such as agrochemicals, pharmaceuticals, polymer, and photographic materials, etc. Some derivatives are commercially important with a variety of industrial uses. A brief account is given below. 

A number of l,4-(oxa/thia)-2-azoles like 5-alkylamino-3-aryl-l,4,2-dithiazolium salts (270) <86JAP(K)6168480) and dithiazolylene derivatives (271) <87JAP(K)52209069> have been patented as useful agrochemicals. For others their suggested applications or activity are specified as detailed below. 

Many of the enzymes in the sterol biosynthesis pathway have selective-inhibitors (Fig. 3). These include some extremely important classes of drugs such as Statins , used to treat high cholesterol, bisphosphonates, used to treat osteoporosis, allylamines (e.g., terbinafine) and azoles used to treat fungal infections, and morpholines which are used as fungicidal agrochemicals. 

It is obvious that a lot of new compounds especially in the fungicidal and insecticidal area are spin-offs from agrochemical research. Important examples are azole fungicides, pyrethroids, benzoylureas and chloronicotinyl insecticides. 

In each data sheet, the core of information is the identification of substructural modification patterns which could be utilized as possible "rules" for the bioisosteric transformation in the lead evolution phase of the dnig design research not only within a single series, but also extended into other categories of bioactive compounds. There are numerous examples in which the structural evolution has occurred from agrochemicals to medicines (an example is the azole-type antimycotics shown in Fig. 1), from herbicides to fungicides as well as to insecticides and vice versa (Fujita, T. In Trends in QSAR and... 

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