- CANNABINOID DERIVATIVES
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The present disclosure relates to a carmabinoid derivative, a pharmaceutical composition comprising it, as well as its use in the treatment and prevention of diseases associated with a carmabinoid receptor in a subject in need thereof, such as acute pain, ADHD/ ADD, alcohol use disorder, allergic asthma, ALS, Alzheimer's, anorexia, etc. The carmabinoid derivative has the following formula:
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- METHOD FOR SYNTHESIS OF LOBARIC ACID AND ANALOG THEREOF
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The present invention can synthesize lobaric acid and four analogues thereof, which are five phenolic lichen metabolites isolated from an extract of the Antarctic lichen Stereocaulon alpinum and selectively inhibit PTP1B, by a simple, economic and efficient chemical synthesis method.
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- Total Syntheses of Lobaric Acid and Its Derivatives from the Antarctic Lichen Stereocaulon alpinum
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The first total syntheses of the natural products lobaric acid (1) and its derivatives isolated from the Antarctic lichen Stereocaulon alpinum are reported in this study. Lobarin (3), with a pseudodepsidone structure, was synthesized first in 11 steps by utilizing an Ullmann aryl ether coupling reaction, and lobaric acid was synthesized in an additional three steps by a seven-membered lactonization reaction. Various derivatives were also obtained from the prepared lobaric acid, and the synthetic compounds exhibited significant PTP1B inhibitory activities.
- Kim, Tai Kyoung,Kim, Joung Eun,Youn, Ui Joung,Han, Se Jong,Kim, Il-Chan,Cho, Cheon-Gyu,Yim, Joung Han
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p. 1460 - 1467
(2018/06/29)
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- CANNABICHROMENIC ACID SYNTHASE FROM CANNABIS SATIVA
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Nucleic acid molecules from cannabis have been isolated and characterized and encode polypeptides having cannabichromenic acid synthase activity. Expression or over-expression of the nucleic acids alters levels of cannabinoid compounds. The polypeptides may be used in vivo or in vitro to produce cannabinoid compounds.
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- Synthesis and antibacterial evaluation of anziaic acid and its analogues as topoisomerase i inhibitors
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Naturally occurring anziaic acid has very recently been reported as a topoisomerase I inhibitor with antibacterial activity. Herein total synthesis of anziaic acid and its structural analogues is described and the preliminary structure-activity relationship (SAR) has been developed based on topoisomerase inhibition and whole cell antibacterial activity.
- Lin, Hao,Annamalai, Thirunavukkarasu,Bansod, Priyanka,Tse-Dinh, Yuk-Ching,Sun, Dianqing
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supporting information
p. 1613 - 1618
(2013/12/04)
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- TERT-BUTANOLYSIS OF LICHEN DEPSIDES
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The scope and limit of the tert-butanolysis of 12 lichen depsides is described.Neither 2-O-methylated nor 2-O-acylated compounds are cleaved by heating with tert-butanol.Key Word Index - Depsides: tert-butanolysis.
- Huneck, Siegfried
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p. 2697 - 2698
(2007/10/02)
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- Inhibition of prostaglandin biosynthesis by 4-O-methylcryptochlorophaeic acid; synthesis of monomeric arylcarboxylic acids for inhibitory activity testing and X-ray analysis of 4-O-methylcryptochlorophaeic acid
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In order to clarify the structure-activity relationship of 4-O-methylcryptochlorophaeic acid (1), which is a lichen meta-depside and a potent inhibitor of prostaglandin (PG) biosynthesis found in our previous screening work, arylcarboxylic acids (5-8) corresponding to the monomeric moieties of 4-O-methylcryptochlorophaeic acid (1) were synthesized and tested for inhibitory effect against PG biosynthesis by an enzyme system prepared from rabbit renal medulla. They were a hundred times less active that 4-O-methylcryptochlorophaeic acid (1), indicating that the dimeric structure of the meta-depside is essential for inhibitory activity against PG biosynthesis. Kinetic studies on the mechanism of inhibition revealed that 4-O-methylcryptochlorophaeic acid (1) inhibits PG biosynthesis competitively with respect to the substrate, arachidonic acid. The three dimensional structure of 4-O-methylcryptochlorophaeic acid (1), which is expected to have a molecular structure able to fit into an active site that accommodates arachidonic acid, was determined by single crystal X-ray analysis with the direct approach. The obtained structure reveals that 4-O-methylcryptochlorophaeic acid (1) maintains a rigid conformation by forming a strong hydrogen bond between a hydroxy group and a methoxy group. Based on these findings, a new active site model of fatty acid cylooxygenase is proposed in order to explain the inhibition by the meta-depside and acidic non-steroidal antiinflammatory drugs.
- Shibuya,Ebizuka,Noguchi,Iitaka,Sankawa
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p. 407 - 413
(2007/10/02)
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