• The Korean Journal of Pesticide Science
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• v.10 no.2
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• pp.69-75
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• 2006

For the development of new agrochemical fungicide 3-amino-2-phenylimino-1,3-thiazolines 2 were designed through the molecular modification based on isostere concept of 3-methyl-2-phenylimino-1,3-thiazolines 1 which showed antifungal activity against rice blast. All the compounds 2 were fit Lipinski rule and they had higher solubility in water than that of 1 by virtual calculation. We constructed 195 kinds of focused library of 3-amino-2-phenylimino-1,3-thiazolines through 6H-[1,3,4]thiadiazines (195 compounds) which synthesized from the reaction of thiourea 4 with $\gamma$-chloroacetoacetanilides 5.

• The Korean Journal of Pesticide Science
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• v.10 no.3
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• pp.165-171
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• 2006

A new 3-amino-1,3-thiazoline chemical library was synthesized through parallel synthetic technology and in vivo antifungal activity of the compounds were investigated against the typical 6 plant diseases (100 ppm). The characteristic feature of these derivatives was that both a benzyl moiety in C-2 imino and an amino group in C-3 of 2-imino-1,3-thiazoline scaffold were substituted in the molecule respectively. Some compounds showed antifungal activity with selectivity against tomato late blight and rice blast. The fungitoxicity would be attributed to 3,4-dichlorophenyl moiety of the benzyl group.