117740-75-7Relevant academic research and scientific papers
Structure and activity relationships of novel uracil derivatives as topical anti-inflammatory agents
Isobe, Yoshiaki,Tobe, Masanori,Inoue, Yoshifumi,Isobe, Masakazu,Tsuchiya, Masami,Hayashi, Hideya
, p. 4933 - 4940 (2007/10/03)
In order to create novel, topical anti-inflammatory compounds exhibiting more potent activities than lead compound CX-659S (1), we designed and synthesized various derivatives of 1 focusing on the uracil N(1)- and N(3)-substituents, and evaluated their an
Synthesis and biological evaluation of CX-659S and its related compounds for their inhibitory effects on the delayed-type hypersensitivity reaction
Tobe, Masanori,Isobe, Yoshiaki,Goto, Yuso,Obara, Fumihiro,Tsuchiya, Masami,Matsui, Junko,Hirota, Kosaku,Hayashi, Hideya
, p. 2037 - 2047 (2007/10/03)
In order to find novel nonsteroidal compounds possessing an inhibitory activity against delayed-type hypersensitivity (DTH) reactions, we conducted random screening using a picryl chloride (PC)-induced contact hypersensitivity reaction (CHR) in mice, and found compound 1 as a lead compound. Then we synthesized and evaluated an extensive series of 5-carboxamidouracil derivatives focused on both the uracil and the antioxidative moieties. Among them, we found that the hindered phenol moiety was necessary to exhibit the activities; especially, compounds 28a-28c having the partial structure of vitamin E were found to exert potent activities against the DTH reaction by both oral and topical administration. And compound 28c showed antioxidative activity against lipid peroxidation with an IC50 of 5.9μM. Compound 28c (CX-659S) was chosen as a candidate drug for the treatment of cutaneous disorders such as atopic dermatitis and allergic contact dermatitis. Copyright (C) 2000 Elsevier Science Ltd.
1-arylpyrimidine derivatives and pharmaceutical use thereof
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, (2008/06/13)
The present invention relates to 1-arylpyrimidine derivatives represented by general formula (I): STR1 wherein R1 is H, alkyl or aralkyl; Ar is 1-naphthyl, or a substituted or unsubstituted phenyl group; R4 is a substituted phenyl, a substituted styryl, 1-methylcyclohexyl, 4-methylcyclohexyl, 4-oxo-4H-pyran-2-yl or 2-oxo-2H-pyran-5-yl group; R5 and R6 are each independently H or alkyl; R3 is H, and R7 and R8 are combined together to be oxo, or else R3 and R7 are combined together to be another direct bond, and R5 and R8 are combined together to be a direct bond, or pharmaceutically acceptable salts thereof; and methods for treating allergic diseases with such compounds.
8-azaxanthine derivatives, and pharmaceutical compositions containing them
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, (2008/06/13)
The present invention relates to 8-azaxanthines derivatives having antiasthmatic activity and the general formula: STR1 wherein: R1 is a hydrogen or a lower alkyl of from one to six carbon atoms or an arylalkyl group; R2 is a lower a
8-Azaxanthines alkylaminoalkyl or heterocyclylalkyl-substituted on the triazole ring, the salts thereof which are physiologically acceptable, their pharmaceutical compositions having antibronchospastic acivity, and the process for preparing the same
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, (2008/06/13)
The present invention relates to 8-azaxanthine derivatives having the general formula: wherein R1 = H; CnH2n+1wherein n = 1 or 3;, R2 = CnH2n+1wherein n = 1 or 5; or C6H5/s
