- Biotransformation of one monoterpene by sporulated surface cultures of Aspergillus niger and Penicillium sp.
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In this study, biotransformation of menthol by sporulated surface culture of Aspergillus niger and Penicillium sp. was studied. The main bioconversion product obtained from menthol of A. niger was cis-p-menthan-7-ol and the main products obtained by surfa
- Esmaeili, Akbar,Sharafian, Shirin,Safaiyan, Shila,Rezazadeh, Shamsali,Rustaivan, Abdolhossein
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- 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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- Terpinenol compound, and preparation method and application thereof
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The invention discloses a terpinenol compound and a preparation method and application thereof. The terpinenol compound has a structure as shown in a formula (I) or (II) which is defined in the specification. In the formula (I), R is independently selected from a group consisting of C12-16 alkyl groups, -NRR, -SR and -OR; and R, R, R and R are independently selected from a group consisting of C1-6 alkyl groups and -NO2, and the C1-6 alkyl groups can be substituted by OH; or R, R and N connected with R and R form a five-membered ring or six-membered ring together, and the five-membered ring or six-membered ring may contain one O or C=O. Activity test results show that the terpinenol compound has good anti-asthma effect, anti-inflammatory action and pulmonary arterial hypertension resistance and is of important pharmaceutical significance.
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Page/Page column 0051; 0052; 0053; 0091; 0092; 0093
(2017/03/08)
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- meng Wanchun products and to a method for preparing the same
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The invention discloses a 1-isopropyl-4-methylcyclohexane product and a preparation method thereof. The method includes utilizing mixed gas composed of normal pressure air, oxygenized air or oxygen and inert gas as an oxidizing agent with the flowing speed as 10-100mL/min and the reaction temperature as 70-180 DEG C, utilizing metalloporphyrin or a solid carrier of the metalloporphyrin as a catalyst, conducting reaction under the condition that no additional solvent or oxidation reductant exists with the catalyst mass fraction as 1-100mg/kg and the reaction time as 1-24h and conducting rectification separation after reaction to obtain an the 1-isopropyl-4-methylcyclohexane product. Main components of the product include 1-isopropyl-4-methylcyclohexane-1-alcohol, 1-isopropyl-4-methylcyclohexane-2-alcohol, 1-isopropyl-4-methylcyclohexane-3-alcohol, 1-isopropyl-4-methylcyclohexane-4-alcohol, 1-isopropyl-4-methylcyclohexane-8-alcohol and a small amount of 1-isopropyl-4-methylcyclohexane-2-ketone and 1-isopropyl-4-methylcyclohexane-3-ketone. The method is less in catalyst usage, simple in reaction process, low in temperature, high in triggering speed, good in selectivity, capable of conducting homogeneous catalysis and also capable of conducting heterogeneous catalysis after immobilization.
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Paragraph 0027; 0028; 0029; 0030
(2016/10/09)
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- P450-catalyzed regio- and stereoselective oxidative hydroxylation of disubstituted cyclohexanes: Creation of three centers of chirality in a single CH-activation event This paper is dedicated to the memory of Harry H. Wasserman
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Wild-type P450-BM3 is able to catalyze in a highly regio- and diastereoselective manner the oxidative hydroxylation of non-activated disubstituted cyclohexane derivatives lacking any functional groups, including cis- and trans-1,2-dimethylcyclohexane, cis- and trans-1,4-dimethylcyclohexane, and trans-1,4-methylisopropylcyclohexane. In all cases except chiral trans-1,2-dimethylcyclohexane as substrate, the single hydroxylation event at a methylene group induces desymmetrization with simultaneous creation of three centers of chirality. Certain mutants increase selectivity, setting the stage for future directed evolution work.
- Ilie, Adriana,Agudo, Rubén,Roiban, Gheorghe-Doru,Reetz, Manfred T.
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p. 470 - 475
(2015/02/02)
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- Selective aerobic hydroxylation of p-menthane to dihydroterpineols catalyzed by metalloporphyrins in solvent and additive free system
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Metallodeuteroporphyrins (MDPs) were employed as the catalysts for aerobic hydroxylation of p-menthane in absence of solvents and additives under ambient pressure. Tertiary C-H bonds were found to be more active than secondary and primary C-H bonds. Thus,
- Xu, Shichao,Zhao, Zhendong,Bi, Liangwu,Chen, Yuxiang,Li, Dongmei,Wang, Jing,Gu, Yan,Lu, Yanju
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- Aminothiazole substituted penicillins and antibacterial compositions thereof
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The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt or in-vivo hydrolysable ester thereof: STR1 wherein R1 is hydrogen or an amino protecting group and R is substituted methyl; optionally substituted C2-12 alkyl, alkenyl or alkynyl; carbocyclyl; aryl or heterocyclyl. These compounds have antibacterial properties, and therefore are of use in the treatment of bacterial infections in humans and animals caused by a wide range of organisms.
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- COMPOUNDS OF THE MENTHANE SERIES. XV. CONFIGURATION AND CONFORMATION OF 2- AND 4-METHYL-1-(ETHOXYCARBONYL)CYCLOHEXANES, THEIR DYNAMIC STEREOCHEMISTRY, AND EFFECTS OF NMR SHIFT REAGENT Eu(fod)3
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The steric structure of the stereoisomeric 2- and 4-methyl-1-(ethoxycarbonyl)cyclohexanes was established by an analysis of their 1H and 13C NMR spectra.It was shown that in cis-4-methyl-1-(ethoxycarbonyl)cyclohexane the ethoxycarbonyl group occupies an axial position with a chairlike conformation of the ring, whereas in th other compounds this group is equatorial.A correlation of the configurations of the compounds and their physical constants in accordance with the Auwers-Skita rule is discussed.The activation parameters of the conformational isomerization were determined and the obtained data were used when studying the reaction of methyl(ethoxycarbonyl)cyclohexanes with CH3MgI.
- Chernov, P. P.,Bazyl'chik, V. V.,Samitov, Yu. Yu.
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p. 1055 - 1061
(2007/10/02)
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- REARRANGEMENTS OF MONOTERPENES IN FUSED ORGANIC ACID
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Rearrangements of terpenic alcohols are significantly influenced by the nature of the organic acid used as the reaction medium.The formation of neoisothujyl alcohol is a highly favoured process in abietic acid.
- Angelis, Francesco De,Ferretti, Gabriella,Botta, Maurizio,Nicoletti, Rosario
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p. 499 - 500
(2007/10/02)
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