- Rapid synthesis of polyprenylated acylphloroglucinol analogs via dearomative conjunctive allylic annulation
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Polyprenylated acylphloroglucinols (PPAPs) are structurally complex natural products with promising biological activities. Herein, we present a biosynthesis-inspired, diversity-oriented synthesis approach for rapid construction of PPAP analogs via double decarboxylative allylation (DcA) of acylphloroglucinol scaffolds to access allyl-desoxyhumulones followed by dearomative conjunctive allylic alkylation (DCAA).
- Grenning, Alexander J.,Boyce, Jonathan H.,Porco, John A.
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supporting information
p. 11799 - 11804
(2014/10/16)
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- Arylalkyl ketones, benzophenones, desoxybenzoins and chalcones inhibit TNF-α induced expression of ICAM-1: Structure-activity analysis
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The interaction between leukocytes and the vascular endothelial cells (EC) via cellular adhesion molecules plays an important role in the pathogenesis of various inflammatory and autoimmune diseases. Small molecules that block these interactions have been targeted as potential therapeutic agents against acute and chronic inflammatory diseases. In an effort to identify potent intercellular cell adhesion molecule-1 (ICAM-1) inhibitors, a large number of arylalkyl ketones, benzophenones, desoxybenzoins and chalcones and their analogs (54 in total) have been synthesized and screened for their ICAM-1 inhibitory activity. The structure-activity relationship studies of these compounds identified three potent chalcone derivatives and also demonstrated the possible mechanism for their ICAM-1 inhibitory activities. The most active compound was found to be 79. A large number of arylalkyl ketones, benzophenones, desoxybenzoins and chalcones as well as their analogs (54 in total) were synthesized and screened for their ICAM-1 inhibitory activity. The structure-activity relationship studies of these compounds identified three potent chalcone derivatives and also demonstrated a possible mechanism of their ICAM-1 inhibitory activities. The most active compound was found to be 79. Copyright
- Kumar, Sarvesh,Reddy L, Chandra Shekhar,Kumar, Yogesh,Kumar, Amit,Singh, Brajendra K.,Kumar, Vineet,Malhotra, Shashwat,Pandey, Mukesh K.,Jain, Rajni,Thimmulappa, Rajesh,Sharma, Sunil K.,Prasad, Ashok K.,Biswal, Shyam,Van Der Eycken, Erik,Depass, Anthony L.,Malhotra, Sanjay V.,Ghosh, Balaram,Parmar, Virinder S.
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experimental part
p. 368 - 377
(2012/07/31)
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- Piperidyl organosiloxanes and polymer substrates light-stabilized therewith
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Novel piperidyl organosiloxanes, well adapted for the light/UV-stabilization of a wide variety of polymer substrates, e.g., polyolefins and polyalkadienes, have the structural formula (I): STR1
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- Benzofuran derivatives as ET(A)-selective, non-peptide endothelin antagonists
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The synthesis and SAR relationships of a series of 4-benzyloxy-3-methylbenzofuran-2-carboxylic acids are described. Compounds from this series show 2- to 16-fold selective binding to the ET(A) receptor in the micromolar range, and two compounds from this series (32 and 40) were demonstrated to exhibit ET(A) antagonist activity.
- Kaltenbronn,Quin III,Reisdorph,Klutchko,Reynolds,Welch,Flynn,Doherty
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p. 425 - 431
(2007/10/03)
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- Method of preparing 2-acylresorcinols
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A method of preparing a 2-acylresorcinol which comprises dehydrogenating a 2-acyl-1,3-cyclohexanedione of the general formula wherein R1 represents an alkyl, aralkyl or aryl group, and RZrepresents hydrogen, or an alkyl, alkoxy or acylamino group, in the presence of a dehydrogenation catalyst (such as a Group VIII metal) or a dehydrogenation agent (such as sulphur or selenium) at an elevated temperature, to provide a 2-acylresorcinol of the general formula wherein R1 and R2 are as defined.
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- A Convenient Synthesis of 2-Alkyl-mono-O-alkylated and 2-Alkyl Resorcinols
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The title C,O-dialkylated resorcinols have seldom been prepared.We have developed a practical synthesis of this class of compounds starting with cyclohexane-1,3-dione.The key features of the synthesis are mono-O-alkylation of a 2-alkyl cyclohexane-1,3-dio
- Stealey, M.A.,Shone, R.L.,Miyano, M.
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p. 1869 - 1876
(2007/10/02)
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- Synthesis of 1-(2,6-Dihydroxyphenyl)-1-alkanones and benzophenone by aromatization of 2-acyl-3-hydroxy-2-cyclohexene-1-ones with mercuric acetate
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1-(2,6-Dihydroxyphenyl)-1-alkanones, natural products identified from insects and from medicinal plants, are readily prepared from 1,3-cyclohexanedione and appropriate carboxylic acids. The final step involves aromatization using mercuric acetate.
- Oliver,Wilzer,Waters
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p. 1117 - 1119
(2007/10/02)
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