- Substituted carboxamide analogues as a new class of local anesthetic agents: Synthesis and bio-evaluation
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A series of N-(2-oxo-2-(phenylamino) ethyl) substituted-4-carboxamide derivatives were synthesized as local anesthetic agents. The structures of carboxamide derivatives were established on the basis of IR, and1H spectral data. All the compounds were subjected to surface local anesthetic activity assay and infiltration local anesthetic activity assay. Among the tested compounds, N-(2-oxo-2-(p-tolylamino) ethyl) piperidine-1-carboxamide (4h) and N-(2-((4-methoxyphenyl) amino)-2-oxoethyl) piperidine-1-carboxamide (4m) were most promising compounds in terms of surface local anaesthetic and infiltration local anaesthetic activity on rats having considerably lower liver toxicity.
- Al-Otaibi, Faisal
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p. 649 - 658
(2018/08/03)
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- Novel water-soluble sedative-hypnotic agents: Isoindolin-1-one derivatives
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We developed new intravenous sedative-hypnotic compounds with the isoindolin-1-one skeleton focusing on the water-soluble property and in vivo safety. We synthesized approximately 170 derivatives and evaluated their hypnotic effects by intravenous administration of the compounds to mice. A series of the 2-phenyl-3-[2-(4-methyl-1-piperazinyl)-2-oxoethyl]isoindolin-1-one analogs, 3(-), 5(-), 27(-), and 47(-) [JM-1232(-)], showed potent sedative-hypnotic activity with good water solubility and a wide safety margin. The hypnotic doses (HD50s) of these 4 compounds when administered to mice were 2.35, 1.90, 2.17, and 3.12 mg/kg, respectively, and the lethal doses (LD50s) were 88.67, 64.69, >120, and >120 mg/kg, respectively. The therapeutic indexes (LD50/HD50) were 37.73, 34.05, >55.30, and >38.46, respectively. Among these compound, 47(-) [JM-1232(-)] is being considered as the most potential candidate for clinical trials in humans.
- Kanamitsu, Norimasa,Osaki, Takashi,Itsuji, Yutaka,Yoshimura, Masakazu,Tsujimoto, Hisashi,Soga, Manabu
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p. 1682 - 1688
(2008/12/21)
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- Titanium(IV) Isopropoxide and Sodium Borohydride: A Reagent of Choice for Reductive Amination
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The preliminary results on the novel use of titanium(IV) isopropoxide and sodium borohydride in reductive amination reactions are reported.A highly efficient and mild procedure for reductive aminations of formaldehyde with a variety of primary and secondary amines is described.
- Bhattacharyya, Sukanta
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p. 2401 - 2404
(2007/10/02)
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- A NOVEL SYNTHESIS OF PYRIDINECARBOXYLIC ACID PIPERAZIDES
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N-Substituted piperazides of pyridinecarboxylic acids were synthesized in the following way: the pyridinecarboxylic acids were converted into (alkoxy-formic acid-pyridinecarboxylic acid) mixed anhydrides by means of alkyl chloroformates, and these were th
- Budai, Z.,Mezei, T.,Lay, A.
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p. 241 - 246
(2007/10/02)
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