Structure-Activity Relationships of Fungicidal N-Substituted Phenyl 1,3,5- Trimethylpyrazole-4-carboxamides in the Inhibition of Succinate Dehydrogenase (SDH) Isolated from Rhizoctonia solani $K{\ddot{u}}hn$

벼 잎집무늬 마름병균 (Rhizoctonia solani $K{\ddot{u}}hn$)에서 분리한 Succinate Dehydrogenase (SDH) 에 대한 N-치환 phenyl 1,3,5-trimethylpyrazole-4-carboxamide 유도체의 효소활성저해

Eighteen N-substituted phenyl 1, 3, 5-trimethylpyrazole-4-carboxamides were synthesized to screen for their mycelial growth inhibition activity against Rhizoctonia solani $K{\ddot{u}}hn$ $(pEC_{50})$ and to measure enzymatic inhibition activity of these compounds $(pI_{50})$ against succinate dehydrogenase (SDH) isolated from Rhizoctonia solani $K{\ddot{u}}hn$ A structure-activity relationship formulated by regression analysis showed that 79% of the variance in mycelial growth inhibition activity can be explained with SDH inhibition activity and chromatographic capacity factor $(\acute{k})$ as a hydrophobic parameter related to the penetration and transport processes in the biological system.

18 종의 N-치환 phenyl 1,3,5-trimethylpyrazole-4-carboxamide 를 합성하여 벼 잎집무늬 마름병균 Rhizoctonia solani $K{\ddot{u}}hn$ 에 대한 균사생육억제력 $(pEC_{50})$ 과 이 균에서 분리한 succinate dehydrogenase (SDH)의 효소활성 저해력 $(pI_{50})$ 을 측정하였다. 구조-활성 상관연구를 통해 균사생육억제력이 SDH 효소저해력과 소수성인자인 chromatographic capacity factor $(\acute{k})$ 에 의해 79%까지 유의성 있게 해석되었으며 이는 합성한 화합물의 주작용점이 SDH 이고 생체내에서 작용점까지 도달하는데 필요한 소수성성질이 살균력의 발현에 중요한 인자임을 보여준다.