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With P. infestans as the experimental objects, the SAR analysis was carried on the EC50 results of antifungal activity test showed in table 5.3. The results showed: (1) the EC50 values of 16 2-methylsulfonyl-5-substituent-thiadiazole derivatives on P. infestans were between 10.05 ug/mL and 59.52 ug/mL while that of hymexazol was 26.49 ug/mL. The EC50 values of compound ¢ø2, ¢ø3, ¢ø4, ¢ø14, ¢ø19, ¢ø21 and ¢ø28  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, respectively, which were below 15 ug/mL. EC50 of the lowest activity of comound ¢ø22 on P. infestans was 59.52 ug/mL. (2) Compired the same substituents on the aryl, monosubstituents had better activity than polysubstituents. For example, EC50 of compound ¢ø18 (R=2,3-2 Cl) on P. infestans was 21.51 ug/mL, and that of compound ¢ø28(R=3-Cl) on P. infestans was 10.44 ug/mL; EC50 of compound ¢ø19(R=2-F) on P. infestans was 14.73 ug/mL, and that of compound ¢ø22 (R=2,6-2F) on P. infestans was 59.52 ug/mL.  (3) when there were 2,6 disubstituents by electron withdrawing group, the compound had bad activity. For example,  EC50 of compound ¢ø22 (R=2,6-2F) on P. infestans was 59.52 ug/mL and that of compound ¢ø26 (R=2,6-Cl) on P. infestans was 42.93 ug/mL. (4) Compired with the same substituents on the aryl, the p-substituted compund had higher activity than the compounds substituted at other sites. For example, EC50 of compound ¢ø16 (R=4-Br) on P. infestans (28.52 ug/mL) was higher than that of compound ¢ø29 (R=2-Br) (49.64 ug/mL).

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With S. sclerotiorum as the experimental objects, the SAR analysis was carried on the EC50 results of antifungal activity test showed in table 5.3. The results showed: (1) 16 2-methylsulfonyl-5-substituent-thiadiazole derivatives on S. sclerotiorum had good antifungal activity and their EC50 values were between 1.87 ug/mL and 17.02 ug/mL while that of hymexazol was 7.76 ug/mL. The EC50 values of compound ¢ø3, ¢ø14, ¢ø21 and ¢ø28  were 1.87 ug/mL, 6.11 ug/mL, 6.97 ug/mL and 4.50 ug/mL, respectively, which were below 7 ug/mL. EC50 of the lowest activity of comound ¢ø18 was 15.08 ug/mL. (2) At the same substituted position of the aryl, the stronger the electron withdrawing ability of substituted group , the higher the activity of the compound. For example, the activity of compound ¢ø19 (R=2-F) on  S. sclerotiorum (EC50=8.49 ug/mL) was higher than that of compound ¢ø29(R=2-Br) (EC50=14.78 ug/mL) (3) Compired with the same substituents on the aryl, monosubstituents had higher activity than polysubstituents. For example, EC50 of compound ¢ø4 (R=2-Cl) on S. sclerotiorum  was 8.57 ug/mL, while EC50 values of compound ¢ø18 (R=2,3-2Cl) and ¢ø23 (R=2,6-2Cl) were 15.08 ug/mL and 17.20 ug/mL, respectively, and both of them had much lower activity than monosubstituents. (4) Compired with the same substituents at different positions of the aryl, the p-substituted compund had higher activity than the compounds substituted at other sites. For example, the activity of compound ¢ø16 (R=4-Br) on S. sclerotiorum (EC50=9.82 ug/mL) was higher than that of compound ¢ø29 (R=2-Br) (EC50=14.78 ug/mL).

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With F. oxysporum as the experimental objects, the SAR analysis was carried on the EC50 results of antifungal activity test showed in table 5.3. The results showed: (1) the EC50 values of 16 2-methylsulfonyl-5-substituent-thiadiazole derivatives on F. oxysporum were between 6.67 ug/mL and 85.41 ug/mL while that of hymexazol was 27.93 ug/mL. The EC50 values of compound ¢ø3, ¢ø14 and ¢ø28 were 6.67 ug/mL, 8.52 ug/mL and 9.4 ug/mL, respectively, which were below 10 ug/mL. The EC50 of the lowest activity of compound ¢ø23 on F. oxysporum was 85.41 ug/mL. (2) At the same substituted position of the aryl, the activity of the compounds with electron withdrawing group was higher than that of the compounds with electron donating group. For example, EC50 of compound ¢ø5(R=3,4-2F) on F. oxysporum was 19.15 ug/mL while that of compound ¢ø23 (R=2,6-2OCH3) was 61.66 ug/mL. (3) Compired with the same substituents on the aryl, monosubstituents had higher activity than polysubstituents. For example, EC50 of compound ¢ø23 (R=2,6-2Cl) on F. oxysporum was 85.41 ug/mL while that of compound ¢ø4 (R=2-Cl) on F. oxysporum was 30.48 ug/mL. (4) Compired with the same substituents at different positions of the aryl, the p-substituted compund had higher activity than the compounds substituted at other sites. For example, the activity of compound ¢ø16 (R=4-Br) on F. oxysporum (EC50=21.48 ug/mL) was higher than that of compound ¢ø29 (R=2-Br) (EC50=29.89 ug/mL).

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With B. cinerea as the experimental objects, the SAR analysis was carried on the EC50 results of antifungal activity test showed in table 5.3. The results showed: (1) the EC50 values of 16 2-methylsulfonyl-5-substituent-thiadiazole derivatives on B. cinerea were between 0.18 ug/mL and 21.00 ug/mL. The EC50 values of compound ¢ø3, ¢ø14, ¢ø21 and ¢ø24 were 0.18 ug/mL, 2.26 ug/mL, 1.99 ug/mL and 2.5 ug/mL, respectively, which were below 5 ug/mL. The EC50 of the compound ¢ø29 on B. cinerea was 21 ug/mL, which was the highest one. (2) At the same substituted position of the aryl, the activity of the compounds with electron withdrawing group was higher than that of the compounds with electron donating group. For example, EC50 of compound ¢ø5(R=3,4-2F) on B. cinerea was 2.51 ug/mL while that of compound ¢ø2 (R=3,4-2OCH3) was 6.89 ug/mL. (3) With different type of substituted group at the same substituted position on the aryl, the activity of the compound with electron withdrawing group was higher than that of the compound with electron donating group. For example, EC50 of compound ¢ø19(R=2-F) on B. cinerea was 5.21 ug/mL while that of compound ¢ø29(R=2-Br)  was 21 ug/mL at the same condition. (4) Compired with the same substituents on the aryl, monosubstituents had higher activity than polysubstituents. For example, EC50 of compound ¢ø19 (R=2-F) on B. cinerea was 5.21 ug/mL while that of compound ¢ø22 (R=2,6-2F) was 8.25 ug/mL; EC50 of compound ¢ø4 (R=2-Cl) on B. cinerea was 7.23 ug/mL while that of compound ¢ø23 (R=2,6-2Cl) was 8.03 ug/mL. (5) Compired with the same substituents on the aryl, the p-substituted compund had higher activity than the compounds substituted at other sites. For example, the activity of compound ¢ø16 (R=4-Br) on B. cinerea (EC50=4.85 ug/mL) was higher than that of compound ¢ø29 (R=2-Br) (EC50=29.89 ug/mL).
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