| Autor: |
Penning, T. D., Chandrakumar, N. S., Chen, B. B., Chen, H. Y., Desai, B. N., Djuric, S. W., Docter, S. H., Gasiecki, A. F., Haack, R. A., Miyashiro, J. M., Russell, M. A., Yu, S. S., Corley, D. G., Durley, R. C., Kilpatrick, B. F., Parnas, B. L., Askonas, L. J., Gierse, J. K., Harding, E. I., Highkin, M. K., Kachur, J. F., Kim, S. H., Krivi, G. G., Villani-Price, D., Pyla, E. Y., Smith, W. G., Ghoreishi-Haack, N. S. |
| Zdroj: |
Journal of Medicinal Chemistry; February 24, 2000, Vol. 43 Issue: 4 p721-735, 15p |
| Abstrakt: |
Leukotriene B4 (LTB4) is a pro-inflammatory mediator that has been implicated in the pathogenesis of a number of diseases including inflammatory bowel disease (IBD) and psoriasis. Since the action of LTA4 hydrolase is the rate-limiting step for LTB4 production, this enzyme represents an attractive pharmacological target for the suppression of LTB4 production. From an in-house screening program, SC-22716 (1, 1-[2-(4-phenylphenoxy)ethyl]pyrrolidine) was identified as a potent inhibitor of LTA4 hydrolase. Structure−activity relationship (SAR) studies around this structural class resulted in the identification of a number of novel, potent inhibitors of LTA4 hydrolase, several of which demonstrated good oral activity in a mouse ex vivo whole blood assay. |
| Databáze: |
Supplemental Index |
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