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Guangfu Yang - One of the best experts on this subject based on the ideXlab platform.
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synthesis in vitro protoporphyrinogen oxidase inhibition and herbicidal activity of n benzothiazol 5 yl hexahydro 1h Isoindole 1 3 diones and n benzothiazol 5 yl hexahydro 1h isoindol 1 ones
Chemical Biology & Drug Design, 2014Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Guangfu YangAbstract:Protoporphyrinogen oxidase (EC 1.3.3.4) is one of the most significant targets for a large family of herbicides. As part of our continuous efforts to search for novel protoporphyrinogen oxidase-inhibiting herbicides, N-(benzothiazol-5-yl)tetrahydroIsoindole-1,3-dione was selected as a lead compound for structural optimization, leading to the syntheses of a series of novel N-(benzothiazol-5-yl)hexahydro-1H-Isoindole-1,3-diones (1a-o) and N-(benzothiazol-5-yl)hexahydro-1H-isoindol-1-ones (2a-i). These newly prepared compounds were characterized by elemental analyses, (1) H NMR, and ESI-MS, and the structures of 1h and 2h were further confirmed by X-ray diffraction analyses. The bioassays indicated that some compounds displayed comparable or higher protoporphyrinogen oxidase inhibition activities in comparison with the commercial control. Very promising, compound 2a, ethyl 2-((6-fluoro-5-(4,5,6,7-tetrahydro-1-oxo-1H-isoindol-2(3H)-yl)benzo[d]thiazol-2-yl)-sulfanyl)acetate, was recognized as the most potent candidate with K(i) value of 0.0091 μm. Further greenhouse screening results demonstrated that some compounds exhibited good herbicidal activity against Chenopodium album at the dosage of 150 g/ha.
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design and syntheses of novel n benzothiazol 5 yl 4 5 6 7 tetrahydro 1h Isoindole 1 3 2h dione and n benzothiazol 5 yl isoindoline 1 3 dione as potent protoporphyrinogen oxidase inhibitors
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Yin Tan, Guangfu YangAbstract:Discovery of protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors has been one of the hottest research areas in the field of herbicide development for many years. As a continuation of our research work on the development of new PPO-inhibiting herbicides, a series of novel N-(benzothiazol-5-yl)-4,5,6,7-tetrahydro-1H-Isoindole-1,3(2H)-diones (1a-p) and N-(benzothiazol-5-yl)isoindoline-1,3-diones (2a-h) were designed and synthesized according to the ring-closing strategy of two ortho-substituents. The bioassay results indicated that some newly synthesized compounds exhibited higher PPO inhibition activity than the control of sulfentrazone. Compound 1a, S-(5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl) O-methyl carbonothioate, was identified as the most potent inhibitor with k(i) value of 0.08 μM, about 9 times higher than that of sulfentrazone (k(i) = 0.72 μM). Further green house assay showed that compound 1b, methyl 2-((5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl)thio)acetate, exhibited herbicidal activity comparable to that of sulfentrazone even at a concentration of 37.5 g ai/ha. In addition, among six tested crops, wheat exhibited high tolerance to compound 1b even at a dosage of 300 g ai/ha. These results indicated that compound 1b might have the potential to be developed as a new herbicide for weed control of wheat field.
Lili Jiang - One of the best experts on this subject based on the ideXlab platform.
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synthesis in vitro protoporphyrinogen oxidase inhibition and herbicidal activity of n benzothiazol 5 yl hexahydro 1h Isoindole 1 3 diones and n benzothiazol 5 yl hexahydro 1h isoindol 1 ones
Chemical Biology & Drug Design, 2014Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Guangfu YangAbstract:Protoporphyrinogen oxidase (EC 1.3.3.4) is one of the most significant targets for a large family of herbicides. As part of our continuous efforts to search for novel protoporphyrinogen oxidase-inhibiting herbicides, N-(benzothiazol-5-yl)tetrahydroIsoindole-1,3-dione was selected as a lead compound for structural optimization, leading to the syntheses of a series of novel N-(benzothiazol-5-yl)hexahydro-1H-Isoindole-1,3-diones (1a-o) and N-(benzothiazol-5-yl)hexahydro-1H-isoindol-1-ones (2a-i). These newly prepared compounds were characterized by elemental analyses, (1) H NMR, and ESI-MS, and the structures of 1h and 2h were further confirmed by X-ray diffraction analyses. The bioassays indicated that some compounds displayed comparable or higher protoporphyrinogen oxidase inhibition activities in comparison with the commercial control. Very promising, compound 2a, ethyl 2-((6-fluoro-5-(4,5,6,7-tetrahydro-1-oxo-1H-isoindol-2(3H)-yl)benzo[d]thiazol-2-yl)-sulfanyl)acetate, was recognized as the most potent candidate with K(i) value of 0.0091 μm. Further greenhouse screening results demonstrated that some compounds exhibited good herbicidal activity against Chenopodium album at the dosage of 150 g/ha.
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design and syntheses of novel n benzothiazol 5 yl 4 5 6 7 tetrahydro 1h Isoindole 1 3 2h dione and n benzothiazol 5 yl isoindoline 1 3 dione as potent protoporphyrinogen oxidase inhibitors
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Yin Tan, Guangfu YangAbstract:Discovery of protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors has been one of the hottest research areas in the field of herbicide development for many years. As a continuation of our research work on the development of new PPO-inhibiting herbicides, a series of novel N-(benzothiazol-5-yl)-4,5,6,7-tetrahydro-1H-Isoindole-1,3(2H)-diones (1a-p) and N-(benzothiazol-5-yl)isoindoline-1,3-diones (2a-h) were designed and synthesized according to the ring-closing strategy of two ortho-substituents. The bioassay results indicated that some newly synthesized compounds exhibited higher PPO inhibition activity than the control of sulfentrazone. Compound 1a, S-(5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl) O-methyl carbonothioate, was identified as the most potent inhibitor with k(i) value of 0.08 μM, about 9 times higher than that of sulfentrazone (k(i) = 0.72 μM). Further green house assay showed that compound 1b, methyl 2-((5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl)thio)acetate, exhibited herbicidal activity comparable to that of sulfentrazone even at a concentration of 37.5 g ai/ha. In addition, among six tested crops, wheat exhibited high tolerance to compound 1b even at a dosage of 300 g ai/ha. These results indicated that compound 1b might have the potential to be developed as a new herbicide for weed control of wheat field.
Zhifang Wang - One of the best experts on this subject based on the ideXlab platform.
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synthesis in vitro protoporphyrinogen oxidase inhibition and herbicidal activity of n benzothiazol 5 yl hexahydro 1h Isoindole 1 3 diones and n benzothiazol 5 yl hexahydro 1h isoindol 1 ones
Chemical Biology & Drug Design, 2014Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Guangfu YangAbstract:Protoporphyrinogen oxidase (EC 1.3.3.4) is one of the most significant targets for a large family of herbicides. As part of our continuous efforts to search for novel protoporphyrinogen oxidase-inhibiting herbicides, N-(benzothiazol-5-yl)tetrahydroIsoindole-1,3-dione was selected as a lead compound for structural optimization, leading to the syntheses of a series of novel N-(benzothiazol-5-yl)hexahydro-1H-Isoindole-1,3-diones (1a-o) and N-(benzothiazol-5-yl)hexahydro-1H-isoindol-1-ones (2a-i). These newly prepared compounds were characterized by elemental analyses, (1) H NMR, and ESI-MS, and the structures of 1h and 2h were further confirmed by X-ray diffraction analyses. The bioassays indicated that some compounds displayed comparable or higher protoporphyrinogen oxidase inhibition activities in comparison with the commercial control. Very promising, compound 2a, ethyl 2-((6-fluoro-5-(4,5,6,7-tetrahydro-1-oxo-1H-isoindol-2(3H)-yl)benzo[d]thiazol-2-yl)-sulfanyl)acetate, was recognized as the most potent candidate with K(i) value of 0.0091 μm. Further greenhouse screening results demonstrated that some compounds exhibited good herbicidal activity against Chenopodium album at the dosage of 150 g/ha.
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design and syntheses of novel n benzothiazol 5 yl 4 5 6 7 tetrahydro 1h Isoindole 1 3 2h dione and n benzothiazol 5 yl isoindoline 1 3 dione as potent protoporphyrinogen oxidase inhibitors
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Yin Tan, Guangfu YangAbstract:Discovery of protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors has been one of the hottest research areas in the field of herbicide development for many years. As a continuation of our research work on the development of new PPO-inhibiting herbicides, a series of novel N-(benzothiazol-5-yl)-4,5,6,7-tetrahydro-1H-Isoindole-1,3(2H)-diones (1a-p) and N-(benzothiazol-5-yl)isoindoline-1,3-diones (2a-h) were designed and synthesized according to the ring-closing strategy of two ortho-substituents. The bioassay results indicated that some newly synthesized compounds exhibited higher PPO inhibition activity than the control of sulfentrazone. Compound 1a, S-(5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl) O-methyl carbonothioate, was identified as the most potent inhibitor with k(i) value of 0.08 μM, about 9 times higher than that of sulfentrazone (k(i) = 0.72 μM). Further green house assay showed that compound 1b, methyl 2-((5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl)thio)acetate, exhibited herbicidal activity comparable to that of sulfentrazone even at a concentration of 37.5 g ai/ha. In addition, among six tested crops, wheat exhibited high tolerance to compound 1b even at a dosage of 300 g ai/ha. These results indicated that compound 1b might have the potential to be developed as a new herbicide for weed control of wheat field.
Yang Zuo - One of the best experts on this subject based on the ideXlab platform.
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synthesis in vitro protoporphyrinogen oxidase inhibition and herbicidal activity of n benzothiazol 5 yl hexahydro 1h Isoindole 1 3 diones and n benzothiazol 5 yl hexahydro 1h isoindol 1 ones
Chemical Biology & Drug Design, 2014Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Guangfu YangAbstract:Protoporphyrinogen oxidase (EC 1.3.3.4) is one of the most significant targets for a large family of herbicides. As part of our continuous efforts to search for novel protoporphyrinogen oxidase-inhibiting herbicides, N-(benzothiazol-5-yl)tetrahydroIsoindole-1,3-dione was selected as a lead compound for structural optimization, leading to the syntheses of a series of novel N-(benzothiazol-5-yl)hexahydro-1H-Isoindole-1,3-diones (1a-o) and N-(benzothiazol-5-yl)hexahydro-1H-isoindol-1-ones (2a-i). These newly prepared compounds were characterized by elemental analyses, (1) H NMR, and ESI-MS, and the structures of 1h and 2h were further confirmed by X-ray diffraction analyses. The bioassays indicated that some compounds displayed comparable or higher protoporphyrinogen oxidase inhibition activities in comparison with the commercial control. Very promising, compound 2a, ethyl 2-((6-fluoro-5-(4,5,6,7-tetrahydro-1-oxo-1H-isoindol-2(3H)-yl)benzo[d]thiazol-2-yl)-sulfanyl)acetate, was recognized as the most potent candidate with K(i) value of 0.0091 μm. Further greenhouse screening results demonstrated that some compounds exhibited good herbicidal activity against Chenopodium album at the dosage of 150 g/ha.
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design and syntheses of novel n benzothiazol 5 yl 4 5 6 7 tetrahydro 1h Isoindole 1 3 2h dione and n benzothiazol 5 yl isoindoline 1 3 dione as potent protoporphyrinogen oxidase inhibitors
Journal of Agricultural and Food Chemistry, 2011Co-Authors: Lili Jiang, Yang Zuo, Zhifang Wang, Yin Tan, Guangfu YangAbstract:Discovery of protoporphyrinogen oxidase (PPO, EC 1.3.3.4) inhibitors has been one of the hottest research areas in the field of herbicide development for many years. As a continuation of our research work on the development of new PPO-inhibiting herbicides, a series of novel N-(benzothiazol-5-yl)-4,5,6,7-tetrahydro-1H-Isoindole-1,3(2H)-diones (1a-p) and N-(benzothiazol-5-yl)isoindoline-1,3-diones (2a-h) were designed and synthesized according to the ring-closing strategy of two ortho-substituents. The bioassay results indicated that some newly synthesized compounds exhibited higher PPO inhibition activity than the control of sulfentrazone. Compound 1a, S-(5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl) O-methyl carbonothioate, was identified as the most potent inhibitor with k(i) value of 0.08 μM, about 9 times higher than that of sulfentrazone (k(i) = 0.72 μM). Further green house assay showed that compound 1b, methyl 2-((5-(1,3-dioxo-4,5,6,7-tetrahydro-1H-isoindol-2(3H)-yl)-6-fluorobenzothiazol-2-yl)thio)acetate, exhibited herbicidal activity comparable to that of sulfentrazone even at a concentration of 37.5 g ai/ha. In addition, among six tested crops, wheat exhibited high tolerance to compound 1b even at a dosage of 300 g ai/ha. These results indicated that compound 1b might have the potential to be developed as a new herbicide for weed control of wheat field.
Yu Zhou - One of the best experts on this subject based on the ideXlab platform.
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Rhodium(III)-Catalyzed C–H Activation of α-Iminonitriles or α-Imino Esters and Cyclization with Acrylates to 2H-Isoindoles
Journal of Organic Chemistry, 2018Co-Authors: Yazhou Li, Jianhui Zhou, Feifei Fang, Bin Xu, Yu ZhouAbstract:Rh(III) catalysts have played increasingly important roles in the activation of C–H bonds to build heterocyclic scaffolds. However, there are few reports on the more challenging synthesis of pharmaceutically important 2H-Isoindoles and fused 2H-Isoindoles. The process reported herein is an effective strategy to produce 2H-Isoindole or fused 2H-Isoindole derivatives via a Rh(III)-catalyzed transformation of α-iminonitriles or α-imino esters with acrylates.
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Rhodium(III)-Catalyzed C–H Activation of α‑Iminonitriles or α‑Imino Esters and Cyclization with Acrylates to 2H‑Isoindoles
2018Co-Authors: Jianhui Zhou, Feifei Fang, Hong Liu, Yu ZhouAbstract:Rh(III) catalysts have played increasingly important roles in the activation of C–H bonds to build heterocyclic scaffolds. However, there are few reports on the more challenging synthesis of pharmaceutically important 2H-Isoindoles and fused 2H-Isoindoles. The process reported herein is an effective strategy to produce 2H-Isoindole or fused 2H-Isoindole derivatives via a Rh(III)-catalyzed transformation of α-iminonitriles or α-imino esters with acrylates
