The Experts below are selected from a list of 9 Experts worldwide ranked by ideXlab platform
Shigeru Izawa - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists.
Bioorganic & Medicinal Chemistry, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract A series of novel bicyclic pyrimidine Derivatives was prepared as part of a search for NK 1 antagonist aimed at the treatment of urinary incontinence. Among them, 3g , a pyrimido[4,5- b ][1,5]Oxazocine Derivative, bearing a 4-acetylpiperazinyl group and a 2-methylphenyl group, was shown to have potent NK 1 antagonist activity with a K B value of 0.105 nM and markedly increased the effective bladder capacity of guinea pigs (59.4% at 0.3 mg/kg iv and 62.8% at 3 mg/kg id). Furthermore, the effect of 3g on bladder function appeared to differ from that of tolterodine, another classical anti-pollakiuria agent, as determined by the distention-induced rhythmic bladder contraction assay using a urethane-anesthetized guinea pig model. Compound 3g is expected to be a promising agent for the treatment of urinary incontinence.
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2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist.
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract The structurally novel pyrimido[4,5- b ][1,5]Oxazocine Derivative 3 , a hybrid compound of pyrido[4,3- b ]- and [2,3- b ]-1,5-Oxazocine ( 1 and 2 , respectively), was designed and synthesized. We examined the atropisomeric property and the NK 1 antagonist activity of 3 . Compound 3 was found to possess both a feature of 1 , free rotation about the biaryl bond, and a feature of 2 , potent in vivo activity.
Shigeki Seto - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists.
Bioorganic & Medicinal Chemistry, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract A series of novel bicyclic pyrimidine Derivatives was prepared as part of a search for NK 1 antagonist aimed at the treatment of urinary incontinence. Among them, 3g , a pyrimido[4,5- b ][1,5]Oxazocine Derivative, bearing a 4-acetylpiperazinyl group and a 2-methylphenyl group, was shown to have potent NK 1 antagonist activity with a K B value of 0.105 nM and markedly increased the effective bladder capacity of guinea pigs (59.4% at 0.3 mg/kg iv and 62.8% at 3 mg/kg id). Furthermore, the effect of 3g on bladder function appeared to differ from that of tolterodine, another classical anti-pollakiuria agent, as determined by the distention-induced rhythmic bladder contraction assay using a urethane-anesthetized guinea pig model. Compound 3g is expected to be a promising agent for the treatment of urinary incontinence.
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2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist.
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract The structurally novel pyrimido[4,5- b ][1,5]Oxazocine Derivative 3 , a hybrid compound of pyrido[4,3- b ]- and [2,3- b ]-1,5-Oxazocine ( 1 and 2 , respectively), was designed and synthesized. We examined the atropisomeric property and the NK 1 antagonist activity of 3 . Compound 3 was found to possess both a feature of 1 , free rotation about the biaryl bond, and a feature of 2 , potent in vivo activity.
Asao Tanioka - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists.
Bioorganic & Medicinal Chemistry, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract A series of novel bicyclic pyrimidine Derivatives was prepared as part of a search for NK 1 antagonist aimed at the treatment of urinary incontinence. Among them, 3g , a pyrimido[4,5- b ][1,5]Oxazocine Derivative, bearing a 4-acetylpiperazinyl group and a 2-methylphenyl group, was shown to have potent NK 1 antagonist activity with a K B value of 0.105 nM and markedly increased the effective bladder capacity of guinea pigs (59.4% at 0.3 mg/kg iv and 62.8% at 3 mg/kg id). Furthermore, the effect of 3g on bladder function appeared to differ from that of tolterodine, another classical anti-pollakiuria agent, as determined by the distention-induced rhythmic bladder contraction assay using a urethane-anesthetized guinea pig model. Compound 3g is expected to be a promising agent for the treatment of urinary incontinence.
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2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist.
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract The structurally novel pyrimido[4,5- b ][1,5]Oxazocine Derivative 3 , a hybrid compound of pyrido[4,3- b ]- and [2,3- b ]-1,5-Oxazocine ( 1 and 2 , respectively), was designed and synthesized. We examined the atropisomeric property and the NK 1 antagonist activity of 3 . Compound 3 was found to possess both a feature of 1 , free rotation about the biaryl bond, and a feature of 2 , potent in vivo activity.
Makoto Ikeda - One of the best experts on this subject based on the ideXlab platform.
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Design, synthesis, and evaluation of novel 2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-ones as NK1 antagonists.
Bioorganic & Medicinal Chemistry, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract A series of novel bicyclic pyrimidine Derivatives was prepared as part of a search for NK 1 antagonist aimed at the treatment of urinary incontinence. Among them, 3g , a pyrimido[4,5- b ][1,5]Oxazocine Derivative, bearing a 4-acetylpiperazinyl group and a 2-methylphenyl group, was shown to have potent NK 1 antagonist activity with a K B value of 0.105 nM and markedly increased the effective bladder capacity of guinea pigs (59.4% at 0.3 mg/kg iv and 62.8% at 3 mg/kg id). Furthermore, the effect of 3g on bladder function appeared to differ from that of tolterodine, another classical anti-pollakiuria agent, as determined by the distention-induced rhythmic bladder contraction assay using a urethane-anesthetized guinea pig model. Compound 3g is expected to be a promising agent for the treatment of urinary incontinence.
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2-substituted-4-aryl-6,7,8,9-tetrahydro-5H-pyrimido[4,5-b][1,5]oxazocin-5-one as a structurally new NK1 antagonist.
Bioorganic & Medicinal Chemistry Letters, 2005Co-Authors: Shigeki Seto, Asao Tanioka, Makoto Ikeda, Shigeru IzawaAbstract:Abstract The structurally novel pyrimido[4,5- b ][1,5]Oxazocine Derivative 3 , a hybrid compound of pyrido[4,3- b ]- and [2,3- b ]-1,5-Oxazocine ( 1 and 2 , respectively), was designed and synthesized. We examined the atropisomeric property and the NK 1 antagonist activity of 3 . Compound 3 was found to possess both a feature of 1 , free rotation about the biaryl bond, and a feature of 2 , potent in vivo activity.
Khaled M. Elattar - One of the best experts on this subject based on the ideXlab platform.
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Role of novel Oxazocine Derivative as corrosion inhibitor for 304 stainless steel in acidic chloride pickling solutions
Research on Chemical Intermediates, 2013Co-Authors: Mahmoud N. El-haddad, Khaled M. ElattarAbstract:Inhibition of 304 stainless steel corrosion in acidic chloride pickling (1.0 M HCl) solutions by newly synthesized Oxazocine Derivative 4 as a corrosion inhibitor have been studied using weight loss, potentiodynamic polarization, and atomic absorption spectroscopy investigations. Potentiodynamic polarization curves show that the inhibitor behaves as a mixed-type. The adsorption of the inhibitor on the metal surface in the acid solution was found to obey Langmuir’s adsorption isotherm. The inhibition mechanism of the investigated inhibitor was discussed in terms of its adsorption on the metal surface. The relationship between the molecular structure and the inhibition efficiency was elucidated by quantum chemical calculations.
