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Toshiaki Kudo - One of the best experts on this subject based on the ideXlab platform.
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X-ray crystallographic analysis of IMP-1 metallo-β-lactamase complexed with a 3-aminoPhthalic Acid Derivative, structure-based drug design, and synthesis of 3,6-disubstituted Phthalic Acid Derivative inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Jun Saito, Takashi Watanabe, Mototsugu Yamada, Toshiaki KudoAbstract:3-(4-Hydroxypiperidine-1-yl) Phthalic Acid 1 shows potent inhibitory activity against metallo-β-lactamase, which is known to inactivate β-lactam antibiotics such as carbapenems. Here, the structure of co-crystals of the metallo-β-lactamase IMP-1 and 1 was first analyzed by X-ray crystallography, and then used for structure-based drug design. Four novel compounds bearing substituents at the 6-position were synthesized to produce 3,6-disubstituted Phthalic Acid Derivatives, and their IMP-1 inhibitory activity and synergistic effect with the carbapenem biapenem (BIPM) were evaluated. 3,6-Disubstituted Phthalic Acid Derivatives showed potent IMP-1 inhibitory activity. In particular, compound 13 showed 10-fold higher IMP-1 inhibitory activity as compared with the parent Derivative 1.
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Metallo-β-lactamase inhibitory activity of Phthalic Acid Derivatives
Bioorganic & Medicinal Chemistry Letters, 2009Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Toshiaki KudoAbstract:4-Butyl-3-methylPhthalic Acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted Phthalic Acids afforded 3-phenylPhthalic Acid Derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl Phthalic Acid Derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1.
Yukiko Hiraiwa - One of the best experts on this subject based on the ideXlab platform.
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X-ray crystallographic analysis of IMP-1 metallo-β-lactamase complexed with a 3-aminoPhthalic Acid Derivative, structure-based drug design, and synthesis of 3,6-disubstituted Phthalic Acid Derivative inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Jun Saito, Takashi Watanabe, Mototsugu Yamada, Toshiaki KudoAbstract:3-(4-Hydroxypiperidine-1-yl) Phthalic Acid 1 shows potent inhibitory activity against metallo-β-lactamase, which is known to inactivate β-lactam antibiotics such as carbapenems. Here, the structure of co-crystals of the metallo-β-lactamase IMP-1 and 1 was first analyzed by X-ray crystallography, and then used for structure-based drug design. Four novel compounds bearing substituents at the 6-position were synthesized to produce 3,6-disubstituted Phthalic Acid Derivatives, and their IMP-1 inhibitory activity and synergistic effect with the carbapenem biapenem (BIPM) were evaluated. 3,6-Disubstituted Phthalic Acid Derivatives showed potent IMP-1 inhibitory activity. In particular, compound 13 showed 10-fold higher IMP-1 inhibitory activity as compared with the parent Derivative 1.
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Metallo-β-lactamase inhibitory activity of Phthalic Acid Derivatives
Bioorganic & Medicinal Chemistry Letters, 2009Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Toshiaki KudoAbstract:4-Butyl-3-methylPhthalic Acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted Phthalic Acids afforded 3-phenylPhthalic Acid Derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl Phthalic Acid Derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1.
Akihiro Morinaka - One of the best experts on this subject based on the ideXlab platform.
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X-ray crystallographic analysis of IMP-1 metallo-β-lactamase complexed with a 3-aminoPhthalic Acid Derivative, structure-based drug design, and synthesis of 3,6-disubstituted Phthalic Acid Derivative inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Jun Saito, Takashi Watanabe, Mototsugu Yamada, Toshiaki KudoAbstract:3-(4-Hydroxypiperidine-1-yl) Phthalic Acid 1 shows potent inhibitory activity against metallo-β-lactamase, which is known to inactivate β-lactam antibiotics such as carbapenems. Here, the structure of co-crystals of the metallo-β-lactamase IMP-1 and 1 was first analyzed by X-ray crystallography, and then used for structure-based drug design. Four novel compounds bearing substituents at the 6-position were synthesized to produce 3,6-disubstituted Phthalic Acid Derivatives, and their IMP-1 inhibitory activity and synergistic effect with the carbapenem biapenem (BIPM) were evaluated. 3,6-Disubstituted Phthalic Acid Derivatives showed potent IMP-1 inhibitory activity. In particular, compound 13 showed 10-fold higher IMP-1 inhibitory activity as compared with the parent Derivative 1.
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Metallo-β-lactamase inhibitory activity of Phthalic Acid Derivatives
Bioorganic & Medicinal Chemistry Letters, 2009Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Toshiaki KudoAbstract:4-Butyl-3-methylPhthalic Acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted Phthalic Acids afforded 3-phenylPhthalic Acid Derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl Phthalic Acid Derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1.
Takayoshi Fukushima - One of the best experts on this subject based on the ideXlab platform.
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X-ray crystallographic analysis of IMP-1 metallo-β-lactamase complexed with a 3-aminoPhthalic Acid Derivative, structure-based drug design, and synthesis of 3,6-disubstituted Phthalic Acid Derivative inhibitors.
Bioorganic & Medicinal Chemistry Letters, 2014Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Jun Saito, Takashi Watanabe, Mototsugu Yamada, Toshiaki KudoAbstract:3-(4-Hydroxypiperidine-1-yl) Phthalic Acid 1 shows potent inhibitory activity against metallo-β-lactamase, which is known to inactivate β-lactam antibiotics such as carbapenems. Here, the structure of co-crystals of the metallo-β-lactamase IMP-1 and 1 was first analyzed by X-ray crystallography, and then used for structure-based drug design. Four novel compounds bearing substituents at the 6-position were synthesized to produce 3,6-disubstituted Phthalic Acid Derivatives, and their IMP-1 inhibitory activity and synergistic effect with the carbapenem biapenem (BIPM) were evaluated. 3,6-Disubstituted Phthalic Acid Derivatives showed potent IMP-1 inhibitory activity. In particular, compound 13 showed 10-fold higher IMP-1 inhibitory activity as compared with the parent Derivative 1.
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Metallo-β-lactamase inhibitory activity of Phthalic Acid Derivatives
Bioorganic & Medicinal Chemistry Letters, 2009Co-Authors: Yukiko Hiraiwa, Akihiro Morinaka, Takayoshi Fukushima, Toshiaki KudoAbstract:4-Butyl-3-methylPhthalic Acid was recognized as a metallo-beta-lactamase inhibitor. The structure-activity relationship study of substituted Phthalic Acids afforded 3-phenylPhthalic Acid Derivatives as potent IMP-1 inhibitors. On the other hand, 3-substituted with 4-hydroxyphenyl Phthalic Acid Derivative displayed a potent combination effect with biapenem (BIPM) against Pseudomonas aeruginosa that produce IMP-1.
Woosum Cho - One of the best experts on this subject based on the ideXlab platform.
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Antitumor and antiangiogenic activities of Phthalic Acid Derivative polymers with medium-molecular-weight
Molecular Crystals and Liquid Crystals Science and Technology. Section A. Molecular Crystals and Liquid Crystals, 2000Co-Authors: Sang-rock Lee, Woosum ChoAbstract:Abstract α-Methoxy-3,6-endo-methylene-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil (MMTFU), was synthesized from 5-fluorouracil (5-FU) and α-methoxy-3,6-endo-methylene-1,2,3,6-tetrahydrophthaloylchloride (MMTC). Poly(3,6-endo-methylene-1,2,3,6-tetrahydroPhthalicanhydride) [poly(MTA)] and poly(α-methoxy-3,6-endo-methylene-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil) [poly(MMTFU)] were prepared from corresponding monomers by photo-polymerizations using 2,2-dimethoxy-2-phenylacetophenone as the photoinitiator. The synthesized MMTFU and polymers were identified by FT-IR, 1H-NMR, and 13C-NMR spectroscopies. The number average molecular weights and polydispersity indices determined by GPC were 6,200 and 1.3 for poly(MTA) and 7,700 and 2.9 for poly(MMTFU). The cytotoxicities of the prepared polymers were lower than that of 5-FU. The in vivo antitumor activities of the polymers against mice bearing sarcoma 180 tumor cell line were greater as compared with that of 5-FU. The antiangiogenic activity of poly(MTA) examin...