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Can I read 3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor on EtoBox?
3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor by Lawrence A. Reiter; Lawrence S. Melvin Jr.; Geraldine L. Crean; Henry J. Showell; Kevin Koch; Michael S. Biggers; John B. Cheng; Robbin Breslow; Maryrose J. Conklyn; Cathy A. Farrell; William A. Hada; Ellen R. Laird; John J. Martin; G. Todd Miller; Joanne S. Pillar is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is 3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor about?
The SAR of a series of 7-chromanylacetic acids has been investigated with the aim of identifying potent and selective LTB4 receptor antagonists. We found optimal activity in derivatives with c~,c~-disubstitution on the acetic acid and a C-4 hydroxy group and a C-3 lipophilic group on the chromane ring. CP-105696 (43), which contains a 4-phenylbenzyl C-3 substituent, was selected for development. ~ 1997 Elsevier Science lad. LTB4 is a potent chemoattractant for granulocytes (e.g., neutrophils and eosinophils) and stimulates functional responses such as secretion and cytokine synthesis in these cells as well as in mononuclear cells and lymphocytes. Its presence in relevant tissues has implicated it to be a likely mediator in a number of inflammatory diseases such as rheumatoid arthritis, inflammatory bowel disease, psoriasis, and asthma. Receptor antagonists of LTB4 are thus expected to be useful therapeutics tbr these diseases. To date, compounds from several structural classes have been discovered to display LTB4 antagonismJ During the course of our investigations on leukotriene D4 antagonists, we observed that certain chromanol derivatives displayed modest LTB4 antagonism in addit
Who reads 3-Substituted-4-hydroxy-7-chromanylacetic acid derivatives as antagonists of the leukotriene B4 (LTB4) receptor?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Lawrence A. Reiter; Lawrence S. Melvin Jr.; Geraldine L. Crean; Henry J. Showell; Kevin Koch; Michael S. Biggers; John B. Cheng; Robbin Breslow; Maryrose J. Conklyn; Cathy A. Farrell; William A. Hada; Ellen R. Laird; John J. Martin; G. Todd Miller; Joanne S. Pillar
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 1997
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)