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xu_0501

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[ Last edited by xu_0501 on 2010-11-18 at 22:07 ]

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1楼 2010-11-11 23:20:26

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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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3楼2010-11-12 21:04:08

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nirvana979

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200人民币还有点可能

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2楼2010-11-12 11:05:23

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yunyanwuhen

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xu_0501(金币+200, 翻译EPI+1):您翻译得很好啊，表述很简洁，感谢，感谢! 2010-11-13 15:03:27

楼上的有机器翻译的嫌疑，很多句子都读不通，请楼主仔细看看哦
下面是我自己的翻译

第一段：
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 Ⅷ2, Ⅷ3, Ⅷ4, Ⅷ14, Ⅷ19, Ⅷ21 and Ⅷ28  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 Ⅷ22 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 Ⅷ18 (R=2,3-2 Cl) on P. infestans was 21.51 ug/mL, and that of compound Ⅷ28(R=3-Cl) on P. infestans was 10.44 ug/mL; EC50 of compound Ⅷ19(R=2-F) on P. infestans was 14.73 ug/mL, and that of compound Ⅷ22 (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 Ⅷ22 (R=2,6-2F) on P. infestans was 59.52 ug/mL and that of compound Ⅷ26 (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 Ⅷ16 (R=4-Br) on P. infestans (28.52 ug/mL) was higher than that of compound Ⅷ29 (R=2-Br) (49.64 ug/mL).

第二段：
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 Ⅷ3, Ⅷ14, Ⅷ21 and Ⅷ28  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 Ⅷ18 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 Ⅷ19 (R=2-F) on  S. sclerotiorum (EC50=8.49 ug/mL) was higher than that of compound Ⅷ29(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 Ⅷ4 (R=2-Cl) on S. sclerotiorum  was 8.57 ug/mL, while EC50 values of compound Ⅷ18 (R=2,3-2Cl) and Ⅷ23 (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 Ⅷ16 (R=4-Br) on S. sclerotiorum (EC50=9.82 ug/mL) was higher than that of compound Ⅷ29 (R=2-Br) (EC50=14.78 ug/mL).

第三段：
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 Ⅷ3, Ⅷ14 and Ⅷ28 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 Ⅷ23 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 Ⅷ5(R=3,4-2F) on F. oxysporum was 19.15 ug/mL while that of compound Ⅷ23 (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 Ⅷ23 (R=2,6-2Cl) on F. oxysporum was 85.41 ug/mL while that of compound Ⅷ4 (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 Ⅷ16 (R=4-Br) on F. oxysporum (EC50=21.48 ug/mL) was higher than that of compound Ⅷ29 (R=2-Br) (EC50=29.89 ug/mL).

第四段：
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 Ⅷ3, Ⅷ14, Ⅷ21 and Ⅷ24 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 Ⅷ29 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 Ⅷ5(R=3,4-2F) on B. cinerea was 2.51 ug/mL while that of compound Ⅷ2 (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 Ⅷ19(R=2-F) on B. cinerea was 5.21 ug/mL while that of compound Ⅷ29(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 Ⅷ19 (R=2-F) on B. cinerea was 5.21 ug/mL while that of compound Ⅷ22 (R=2,6-2F) was 8.25 ug/mL; EC50 of compound Ⅷ4 (R=2-Cl) on B. cinerea was 7.23 ug/mL while that of compound Ⅷ23 (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 Ⅷ16 (R=4-Br) on B. cinerea (EC50=4.85 ug/mL) was higher than that of compound Ⅷ29 (R=2-Br) (EC50=29.89 ug/mL).

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4楼2010-11-13 00:41:54

已阅关注TA 给TA发消息送TA红花 TA的回帖