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Design and synthesis of achiral 5-lipoxygenase inhibitors employing the cyclobutyl group |
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| Authors: | Simon T. Hodgson Peter J. Wates Geoffrey J. Blackwell Caroline Craig Michael Yeadon Nigel Boughton-Smith |
| Affiliation: | Wellcome Research Laboratories, Langley Court, Beckenham, Kent, BR3 3BS, UK |
| Abstract: | The cyclobutyl group is an effective replacement for the linking group required in hydroxyureas for good in vivo activity against 5-Lipoxygenase. The principle is illustrated in two 5-LO inhibitors: 858C, a more potent inhibitor than Zileuton and, 862C, a very poteng 5-LO inhibitor with good oral persistence. |
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