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Can I read Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives on EtoBox?
Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives by Hiroyuki Hisamichi; Ryo Naito; Akira Toyoshima; Noriyuki Kawano; Atsushi Ichikawa; Akiko Orita; Masaya Orita; Noritaka Hamada; Makoto Takeuchi; Mitsuaki Ohta; Shin-ichi Tsukamoto is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives about?
Spleen tyrosine kinase (Syk) is a non-receptor-type tyrosine kinase which mediates diverse responses in haematopoietic cells. Therefore, Syk is an attractive therapeutic target, and in a study of Syk inhibitors as potentially new therapeutic agents, we discovered the 4-anilinopyrimidine-5-carboxamides. Enzyme screening indicated that an aminoethylamino moiety at the 2-position of the pyrimidine ring was important for Syk inhibitory activity, and an investigation of the substituents at the 4-position revealed that an anilino moiety substituted at the meta position was preferred. These compounds showed high selectivity for Syk, compared to other kinases, such as ZAP-70, c-Src, and PKC, and exhibited good inhibitory activities against 5-HT release from RBL-cells. Among them, compound 9a inhibited the passive cutaneous anaphylaxis reaction in mice, with an ID 50 of 13 mg/kg following subcutaneous administration. These results suggest that our compounds are worthy of further evaluation as new anti-allergic agents.
Who reads Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Hiroyuki Hisamichi; Ryo Naito; Akira Toyoshima; Noriyuki Kawano; Atsushi Ichikawa; Akiko Orita; Masaya Orita; Noritaka Hamada; Makoto Takeuchi; Mitsuaki Ohta; Shin-ichi Tsukamoto
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0968-0896)
- Published
- 2005
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)