1074-63-1Relevant articles and documents
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Surrey
, p. 3354 (1949)
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CARBAZOLE-CONTAINING AMIDES, CARBAMATES, AND UREAS AS CRYPTOCHROME MODULATORS
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Paragraph 0315, (2015/10/28)
The subject matter herein is directed to carbazole-containing amide, carbamate, and urea derivatives and pharmaceutically acceptable salts or hydrates thereof of structural formula I wherein the variable R1, R2, R3, R4, R5, R6, R7, A, D, E, G, J, L, M, Q, a, and b are accordingly described. Also provided are pharmaceutical compositions containing the compounds of formula I to treat a Cry-mediated disease or disorder, such as diabetes, complications associated with diabetes, Cushing's syndrome, NASH, NAFLD, asthma, and COPD.
Synthesis and antiplatelet activity of new imidazole-4-carboxylic acid derivatives
Rehse, Klaus,Steege, Jens
, p. 539 - 547 (2007/10/03)
1-Arylalkyl-5-phenylsulfonamino-imidazole-4-carboxylic acid esters and their carboxamides with an additional secondary amino group were synthesized and identified as antiplatelet agents in a low micromolar range (Born-test, inducer collagen). To describe the mechanism of action more precisely the Born-test was carried out as well with ADP, adrenaline or PAF, respectively. In addition, two compounds were investigated for their COX-1 inhibitory activities. Provided the essential structural criteria are met i.e. amide group or ester, sulfonylamino rest, hydrophobic moieties, and a secondary amino function, slight structural modifications are able to shift the pattern of activity among the above platelet receptors. So, the ester 5c exhibits PAF antagonistic activity at IC 50 = 1 μM and COX-1 inhibition (IC50 = 0.4 μM). The carboxamide 6c shows ADP antagonistic properties (IC50 = 2 μM). Compound 6g is as well PAF antagonistic (IC50 = 4 μM) and a COX-1 inhibitor (IC50 = 1 μM). The derivative 6i shows a strong antiadrenergic (IC50 = 0.15 μM) and PAF antagonistic (IC 50 = 0.66 μM) effect.