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The original strain of potato late blight (P. infestans) as test subjects to the table 5.3 results of antibacterial activity test EC50 known SAR discussed: (1) the 16 2 - methyl sulfonyl -5-- substituted - oxadiazole derivatives of the original strain EC50 potato late blight in the 10.05 ~ 59.52 ug / mL between the control hymexazol to 26.49 ug / mL. Where EC50 less than 15 ug / mL of the compounds were Ⅷ 2, Ⅷ 3, Ⅷ 4, Ⅷ 14, Ⅷ 19, Ⅷ 21, Ⅷ 28, EC50 values were 11.53 ug / mL, 1.64 ug / mL, 14.93ug/mL, 11.32 ug / mL, 14.73 ug / mL, 10.05 ug / mL and 10.44 ug / mL, activity of the worst on the potato late blight Ⅷ 22 compounds in the original strain EC50 was 59.52 ug / mL. (2) the same substituent on the benzene ring, one more to replace than a good replacement activity. If compounds Ⅷ 18 (R = 2,3-2 Cl) on the potato late blight bacteria EC50 is the original 21.51 ug / mL, and Ⅷ 28 (R = 3-Cl) on the potato late blight bacteria EC50 is the original 10.44 ug / mL; compounds Ⅷ 19 (R = 2-F) on the potato late blight bacteria EC50 is the original 14.73 ug / mL, and Ⅷ 22 (R = 2,6-2F) inhibition of the potato late blight was 59.52 ug / mL. (3) in the benzene ring of 2,6-bit with a electron withdrawing group, the activity is poor. If compounds Ⅷ 22 (R = 2,6-2F) inhibition of potato late blight was 59.52 ug / mL, such as compounds Ⅷ 26 (R = 2,6-Cl) on the inhibition of potato late blight was 42.93 ug / mL. (4) the same type of substituents on the benzene ring, benzene ring-substituted compounds on the activity of replacing good activity than other positions, such as compounds Ⅷ 16 (R = 4-Br) on the potato late blight EC50 was 28.52 ug / mL, higher than the 2-substituted compounds Ⅷ 29 (R = 2-Br, EC50 = 49.64 ug / mL).
Sclerotia to rape bacteria (S. sclerotiorum) as test subjects to the table 5.3 results of antibacterial activity test EC50 known SAR discussed: (1) the 16 2 - methyl sulfonyl -5-- substituted - oxadiazole Derivatives on Rape sclerotia EC50 bacteria between the 1.87 ~ 17.02ug/mL has good antibacterial activity, the control hymexazol to 7.76 ug / mL. Where EC50 less than 7 ug / mL of the compounds were: Ⅷ 3, Ⅷ 14, Ⅷ 21, Ⅷ 28, EC50 values were 1.87 ug / mL, 6.11 ug / mL, 6.97 ug / mL, 4.50 ug / mL; activity is the lowest of the compounds Ⅷ 18 of the EC50 was 15.08 ug / mL. (2) replace the same position on the benzene ring, electron withdrawing groups and strong electron withdrawing ability than the weak group activity is good, such as compounds Ⅷ 19 (R = 2-F) strain EC50 sclerotia of rape was 8.49 ug / mL higher than the weak electron compounds Ⅷ 29 (R = 2-Br), the EC50 was 14.78 ug / mL. (3) the same type of substituents on the benzene ring, one more to replace than a good replacement activity, such as compounds Ⅷ 4 (R = 2-Cl) EC50 bacteria sclerotia of rape was 8.57 ug / mL, Ⅷ 18 (R = 2,3 - 2Cl) EC50 bacteria sclerotia of rape was 15.08 ug / mL; Ⅷ 23 (R = 2,6-2Cl) EC50 bacteria sclerotia of rape was 17.20 ug / mL, and its activity is much lower than the monosubstituted compounds. (4) the same type of substituents on the benzene ring, benzene ring-substituted compounds on the activity of replacing good activity than other positions, such as compounds Ⅷ 16 (R = 4-Br) on the bacterial pathogen sclerotia rape EC50 was 9.82 ug / mL, higher than the 2-substituted compounds Ⅷ 29 (R = 2-Br), the EC50 was 14.78 ug / mL.
Pepper wilt pathogen (F. oxysporum) to test object, table 5.3 results of antibacterial activity test EC50 known SAR discussed: (1) the 16 2 - methyl sulfonyl -5-- substituted - oxadiazole derivatives extract on Fusarium pathogens EC50 in 6.67 ~ 85.41 ug / mL between the positive control hymexazol to 27.93 ug / mL. Where EC50 less than 10 ug / mL of the compound is Ⅷ 3, Ⅷ 14 and Ⅷ 28, the EC50 were 6.67 ug / mL, 8.52 ug / mL and 9.4 ug / mL, activity is the lowest of the compounds Ⅷ 23 on pepper wilt pathogen EC50 was 85.41 ug / mL. (2) replace the same position on the benzene ring, electron withdrawing groups to electron-donating group activity than the activity of good; such compounds Ⅷ 5 (R = 3,4-2F) of Fusarium pathogens EC50 is 19.15 ug / mL, and under the same conditions compound Ⅷ 23 (R = 2,6-2OCH3) EC50 of Fusarium pathogens is 61.66 ug / mL. (3) the same type of substituents on the benzene ring, one to replace more than replace the good activity, such as compounds Ⅷ 23 (R = 2,6-2Cl) EC50 of Fusarium pathogens is 85.41 ug / mL, and under the same conditions Ⅷ 4 (R = 2-Cl) on the Fusarium pathogens EC50 is 30.48 ug / mL. (4) the same type of substituents on the benzene ring, benzene ring-substituted compounds on the activity of replacing good activity than other positions, such as compounds Ⅷ 16 (R = 4-Br) of Fusarium pathogens EC50 is 21.48 ug / mL, higher than the 2-substituted compounds Ⅷ 29 (R = 2-Br), EC50 was 29.89 ug / mL.
The original strain of cucumber gray mold (B. cinerea) as test subjects to the table 5.3 results of antibacterial activity test EC50 known SAR discussed: (1) the 16 2 - methyl sulfonyl -5-- substituted - oxadiazole derivatives of the original strain of cucumber gray mold, EC50 at 0.18 ~ 21.00 ug / mL between. Where EC50 less than 5 ug / mL of the compounds were: Ⅷ 3, Ⅷ 14, Ⅷ 21, Ⅷ 24, the EC50 were 0.18 ug / mL, 2.26 ug / mL, 1.99 ug / mL and 2.5 ug / mL, EC50 values of the highest compound Ⅷ 29 original strains of cucumber gray mold, EC50 was 21.00 ug / mL. (2) replace the same position on the benzene ring, electron withdrawing groups to electron-donating group activity than a good activity, such as compounds Ⅷ 5 (R = 3,4-2F) of cucumber gray mold of the original strain EC50 was 2.51 ug / mL, and under the same conditions compound Ⅷ 2 (R = 3,4-2OCH3) of cucumber gray mold of the original strain EC50 was 6.89 ug / mL. (3) the same position on the benzene ring, the different types of substituents, electron withdrawing groups and strong electron withdrawing ability than the weak group activity well. If compounds Ⅷ 19 (R = 2-F) on the original strain of cucumber gray mold EC50 is 5.21 ug / mL, and compounds under the same conditions Ⅷ 29 (R = 2-Br) of cucumber gray mold of the original strain EC50 was 21.00 ug / mL. (4) the benzene ring on the same types of substituents, one to replace than polysubstituted good activity, Ⅷ 19 (R = 2-F) of cucumber gray mold of the original strain EC50 was 5.21 ug / mL, and under the same conditions compound Ⅷ 22 (R = 2, 6-2F) of cucumber gray mold of the original strain EC50 was 8.25 ug / mL, Ⅷ 4 (R = 2-Cl) of cucumber gray mold of the original strain EC50 was 7.23 ug / mL, and under the same conditions compound Ⅷ 23 (R = 2,6-2 Cl) of cucumber gray mold of the original strain EC50 was 8.03 ug / mL. (5) the same type of substituents on the benzene ring, benzene ring-substituted compounds on the activity of replacing good activity than other positions, such as compounds Ⅷ 16 (R = 4-Br) of cucumber gray mold of the original strain EC50 was 4.85 ug / mL, higher than the 2-substituted compounds Ⅷ 29 (R = 2-Br), EC50 was 29.89 ug / mL. |
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