- Amide compound, pharmaceutical composition, preparation method and application thereof
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The invention provides an amide compound, a pharmaceutical composition, a preparation method and application thereof and belongs to the field of medicine. Structure of the amide compound is shown as aformula I. The preparation method includes: in an alkaline condition and in an organic solvent, allowing a compound I and a compound II to be in condensation reaction. The amide compound or pharmaceutically acceptable salt thereof have long-acting sensory and/or motion blocking activity, can be used for preparing long-acting local anesthetic or analgesic and is long in efficacy lasting time, little side effect and high in medication safety.
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Paragraph 0236-0239
(2018/09/11)
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- Orally Active β-Lactam Inhibitors of Leukocyte Elastase-1. Activity of 3,3-Diethyl-2-azetidinones
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A thorough analysis of the mechanism of inhibition of human leukocyte elastase (HLE) by a monocyclic β-lactam and the mechanism of β-lactam hydrolysis led to the preparation of potent and highly stable inhibitors of HLE.This work led to the identification of 4--3,3-diethyl-1-carbonyl>-2-azetidinone (2) as the first orally active inhibitor of human leukocyte elastase (HLE).Analogs of 2 with different substituents on the urea N were synthesized and evaluated for their activity in vitro against HLE as well as in vivo in a hamster lung hemorrhage model.Compounds with a methyl or a methoxy group in the para position of the benzene ring were very potent in both assays.The results are discussed on the basis of the proposed model for the binding of this class of inhibitors to HLE and a possible mechanism of inhibition is presented.
- Shah, Shrenik K.,Dorn, Conrad P.,Finke, Paul E.,Hale, Jeffrey J.,Hagmann, William K.,et al.
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p. 3745 - 3754
(2007/10/02)
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- ARYLMETHYL ISOCYANATES
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Chloromethyl isocyanate reacts readily with aromatic hydrocarbons in the presence of anhydrous ferric chloride or other catalysts of the Friedel-Crafts reaction with the formation of arylmethyl isocyanates.The latter add alcohols and amines readily, being converted into the corresponding substituted urethanes and ureas.When heated in the presence of catalytic amounts of 1,3-dimethylphosphol-3-ene they give substituted carbodiimides.
- Kozhushko, B. N.,Lomakina, A. V.,Paliichuk, Yu. A.,Shokol, V. A.
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p. 654 - 660
(2007/10/02)
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