- Discovery of a novel series of α-terpineol derivatives as promising anti-asthmatic agents: Their design, synthesis, and biological evaluation
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A series of novel α-terpineol derivatives were designed and synthesized through structural derivatization of the tertiary hydroxyl moiety or reduction of the double bond. Of the resulting compounds, eight compounds enhanced relaxation of airway smooth muscle (ASM) compared to the α-terpineol precursor, and four compounds (4a, 4d, 4e, and 4i)were superior or comparable to aminophylline at a concentration of 0.75 mmol/L. Assays for 3′-5′-Cyclic adenosine monophpsphate (cAMP) activation revealed that some representative α-terpineol derivatives in this series were capable of upregulating the level of cAMP in ASM cells. Further in vivo investigation using the asthmatic rat model, illustrated that treatment with the compounds 4a and 4e resulted in significantly lowered lung resistance (RL) and enhanced dynamic lung compliance (Cldyn), two important parameters for lung fuction. Moreover, treatment with 4e downregulated the levels of both IL-4 and IL-17. Due to its several favorable physiological functions, including ASM relaxation activity, cAMP activation capability, and in vivo anti-asthmatic efficacy, 4e is a promising remedy for bronchial asthma, meriting extensive development.
- Zhu, Wanping,Liu, Xia,Wang, Yuji,Tong, Yeling,Hu, Yongzhou
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p. 419 - 425
(2017/12/07)
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- Α-terpineol fatty acid ester derivatives and use
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The invention belongs to the technical field of medicine and discloses alpha-terpineol aliphatic ester and a preparation with the compound. The alpha-terpineol aliphatic ester is formed by alpha-terpineol and fatty acid after esterification reaction. According to a method, first, fatty acid and thionyl chloride react to prepare acyl chloride, and then acyl chloride and alpha-terpineol react to prepare the alpha-terpineol aliphatic ester. The alpha-terpineol ester can be used as penetration enhancers to be used for external preparations of patching agents, Cataplasm, ointment agents, gel agents and the like, accordingly, the percutaneous absorptive amount of medicine is improved, and the alpha-terpineol aliphatic ester is good percutaneous absorptive penetration enhancers and has wide application prospect.
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Paragraph 0043; 0044
(2017/03/18)
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- Α- [...] enol derivative and its preparation method and application
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The invention discloses alpha-terpineol derivatives, the structure of which is shown as the formula (II), wherein R or H is C1-C5 alkyl. The alpha-terpineol derivatives can be obtained by performing esterification reaction on a raw material alpha-terpineol with acid or acid anhydride at the temperature of 18-30DEG C under the action of 4-methylbenzenesulfonyl chloride. The invention further discloses applications of the alpha-terpineol derivatives in preparing antiasthmatic drugs, carboxylic ester prodrug formed by introducing carboxylic ester on the hydroxyl of the alpha-terpineol derivatives can be slowly hydrolyzed in a human body to release parent drug and further prolong the curative effect and the acting time, in addition the bioavailability can be improved, and the antiasthma activity can be further enhanced.
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Paragraph 0039; 0040
(2017/05/03)
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- ANTIMICROBIAL COMPOSITION COMPRISING THYMOL AND A TERPINYL DERIVATIVE
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The present invention relates to an antimicrobial composition and a method for disinfection involving the antimicrobial composition. It particularly relates to an antimicrobial composition for personal cleaning, oral care or hard surface cleaning applications. It was found that compositions comprising thymol, selected terpinyl derivatives and a carrier provide synergistic antimicrobial action. In a preferred aspect the composition also comprises 1 to 80 %-wt of surfactant.
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Page/Page column 355
(2013/03/26)
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- SOLVOLYTIC DISPLACEMENT OF ALKYL HALIDES BY METAL SALTS. PREPARATIVE PROCEDURES FOR ALLYL-, BENZYL- AND TERTIARY ALKYL-OXY DERIVATIVES USING THE ZINC SALTS
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Reaction of allylic, benzylic and tertiary alkyl halides with zinc oxide in protic solvents leads to the formation of the corresponding alcohols, ethers and esters in good yields.The scope and limitations of this reaction have been examined.The possible involvement of ion quadruplets in the reaction is suggested.
- Gurudutt, K. N.,Ravindranath, B.,Srinivas, P.
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p. 1843 - 1846
(2007/10/02)
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