118875-18-6Relevant academic research and scientific papers
CYANOACRYLATE-BASED ULTRAVIOLET ABSORBING COMPOUND AND COMPOSITION COMPRISING THE SAME AS ULTRAVIOLET ABSORBER
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Paragraph 0055-0058, (2020/09/30)
The present invention relates to a cyanoacrylate-based ultraviolet absorbing compound represented by chemical formula 1 and a composition comprising the same as an ultraviolet absorber. (In the chemical formula 1, A1 is an ethyl group and A2 is a methyl g
Novel process for the synthesis of class I antiarrhythmic agent (±)-cibenzoline and its analogs
Gholap, Atul R.,Paul, Vincent,Srinivasan, Kumar V.
, p. 2967 - 2982 (2008/12/22)
Synthesis of (±)-cibenzoline and its analogs has been achieved by a simple sequence of reactions. The diaryl cyanoolefin intermediate 3 could be prepared by Knoevenagel condensation of benzophenone with ethylcyanoacetate to form the tetra-substituted olefin intermediate 2 followed by Krapcho deethoxycarbonylation or from β-hydroxynitrile intermediate 2' followed by the elimination of hydroxyl group respectively. The 2,2- diphenylcyclopropanecarbonitrile 4 was synthesized from intermediate 3 by cyclopropanation, which was converted to (±)-2-(2,2-diphenylcyclopropyl)- 2-imidazoline 5 by reaction with ethylenediamine in the presence of a catalytic amount of sulfur. Moreover, the obtained 2-imidazolines were smoothly oxidized to the corresponding imidazoles 6 in good to moderate yields. Copyright Taylor & Francis Group, LLC.
Synthesis, biological profile, and quantitative structure - Activity relationship of a series of novel 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors
Sit,Parker,Motoc,Han,Balasubramanian,Catt,Brown,Harte,Thompson,Wright
, p. 2982 - 2999 (2007/10/02)
A series of 9,9-bis(4-fluorophenyl)-3,5-dihydroxy-8-(alkyltetrazol-5-yl)-6,8-nonad ienoic acid derivatives 1 were synthesized and found to inhibit competitively the enzyme 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase. The analogues having 1N-methyltetrazol-5-yl attached to the C8-position (3a, 4a, R1 = R2 = F) are the most active in suppressing cholesterol biosynthesis in both in vitro and in vivo models: the IC50 for the chiral form of 3a is 19 nM, K(i) = 4.3 x 10-9 M when K(m) for HMG-CoA is 28 x 10-6 M; the ED50 (oral) value corresponding to the lactone derivative (4a, BMY 22089) is approximately 0.1 mg/kg. Further, BMY 21950 is nearly 2 orders of magnitude more active in parenchymal hepatocytes, from which most of the serum cholesterol originates, than in other cell preparations (such as spleen, testes, ileum, adrenal, and ocular lens epithelial cells; Table III). This apparent tissue specificity may be highly beneficial since the blocking of cholesterol biosynthesis in other vital organs could eventually lead to undesirable side effects. In addition to the chemical synthesis and biological evaluation, a theoretical study aimed at relating the HMG-CoA reductase inhibitory potency to the three-dimensional structure of the inhibitors was undertaken. With a combination of molecular mapping and 3D-QSAR techniques, it was possible to determine a logical candidate for the conformation of the bound inhibitor and to quantitatively relate inhibitory potency to the shape and size of both the binding site and the C8-substituent.
Antihypercholesterolemic tetrazole compounds
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, (2008/06/13)
Compounds of the formula STR1 wherein R1 and R4 each are independently hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy, or trifluoromethyl; R2, R3, R5 and R6 each are independently hydrogen, halogen C1-4 alkyl or C1-4 alkoxy; tet is STR2 n is an integer of from 0 to 2, inclusive; A is STR3 R7 is hydrogen, C1-4 alkyl, C1-4 alkoxy(lower) alkyl or (2-methoxyethoxy)methyl; X is --OH or =O; and R8 is hydrogen, a hydrolyzable ester group or a cation to form a non-toxic pharmaceutically acceptable salt, are novel antihypercholesterolemic agents which inhibit cholesterol biosynthesis. Intermediates and processes for their preparation are disclosed.
Antihypercholesterolemic nitrile compounds
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, (2008/06/13)
Compounds of the formula STR1 wherein R1, R2, R3 and R4 each are independently hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or trifluoromethyl; A is STR2 and R5 is hydrogen, a hydr
Intermediates for the preparation of antihypercholesterolemic tetrazole compounds
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, (2008/06/13)
This invention provides novel tetrazole intermediates of the formula STR1 wherein R1 and R4 each are independently hydrogen, halogen, C1-4 alkyl, C1-4 alkoxy or trifluoromethyl; R2,R3,Rsup
