New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.

Janusz JM; Young PA; Ridgeway JM; Scherz MW; Enzweiler K; Wu LI; Gan L; Chen J; Kellstein DE; Green SA; Tulich JL; Rosario-Jansen T; Magrisso IJ; Wehmeyer KR; Kuhlenbeck DL; Eichhold TH; Dobson RL

首页> 外文期刊>Journal of Medicinal Chemistry >New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.

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New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.

机译：新的环氧合酶-2 / 5-脂氧合酶抑制剂。 3. 7-叔丁基-2，3-二氢-3,3-二甲基苯并呋喃衍生物作为胃肠道安全的抗炎和止痛药：在5位上变化。

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We report an expansion of the scope of our initial discovery that 5-keto-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMBFs) are antiinflammatory and analgesic agents. Several other functional groups have been introduced at the 5 position: amides, amidines, ureas, guanidines, amines, heterocycles, heteroaromatics, and heteroaryl ethenyl substituents in the 5 position all provide active compounds. These compounds are dual cyclooxygenase (COX) and 5-lipoxygenase (5-LOX) inhibitors. They inhibit both COX-1 and COX-2 with up to 33-fold selectivity for COX-2.

机译：我们报道了我们最初发现的范围的扩大，即5-酮基取代的7-叔丁基-2,3-二氢-3,3-二甲基苯并呋喃（DHDMBFs）是抗炎药和镇痛药。在5位上引入了几个其他官能团：5位上的酰胺，am，脲，胍，胺，杂环，杂芳族化合物和杂芳基乙烯基取代基均提供活性化合物。这些化合物是双重环氧合酶（COX）和5-脂氧合酶（5-LOX）抑制剂。它们抑制COX-1和COX-2，对COX-2的选择性高达33倍。

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来源
《Journal of Medicinal Chemistry》 |1998年第18期|共15页
作者
Janusz JM; Young PA; Ridgeway JM; Scherz MW; Enzweiler K; Wu LI; Gan L; Chen J; Kellstein DE; Green SA; Tulich JL; Rosario-Jansen T; Magrisso IJ; Wehmeyer KR; Kuhlenbeck DL; Eichhold TH; Dobson RL;
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正文语种 eng
中图分类药学;
关键词
Analgesics; Anti-Inflammatory Agents; Non-Steroidal; Arachidonate 5-Lipoxygenase; 镇痛药; 消炎药; 非甾类; 花生四烯酸盐5-脂氧合酶; 苯呋喃类; 环加氧酶抑制药;

机译：Analgesics;Anti-Inflammatory Agents;Non-Steroidal;Arachidonate 5-Lipoxygenase;镇痛药;消炎药;非甾类;花生四烯酸盐5-脂氧合酶;苯呋喃类;环加氧酶抑制药;

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1. New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position. [J] . Janusz JM, Young PA, Ridgeway JM, Journal of Medicinal Chemistry . 1998,第18期

机译：新的环氧合酶-2 / 5-脂氧合酶抑制剂。 3. 7-叔丁基-2，3-二氢-3,3-二甲基苯并呋喃衍生物作为胃肠道安全的抗炎和止痛药：在5位上变化。
2. New cyclooxygenase-2/5-lipoxygenase inhibitors. 2. 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations of the dihydrobenzofuran ring (published erratum appears in J Me [J] . Janusz JM, Young PA, Scherz MW, Journal of Medicinal Chemistry . 1998,第7期

机译：新的环氧合酶-2 / 5-脂氧合酶抑制剂。 2. 7-叔丁基-2,3-二氢-3,3-二甲基苯并呋喃衍生物作为胃肠道安全的抗炎和止痛药：二氢苯并呋喃环的变异（发表于J Me。
3. New cyclooxygenase-2/5-lipoxygenase inhibitors. 1. 7-tert-buty1-2,3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: discovery and variation of the 5-keto substituent. [J] . Janusz JM, Young PA, Ridgeway JM, Journal of Medicinal Chemistry . 1998,第7期

机译：新的环氧合酶-2 / 5-脂氧合酶抑制剂。 1. 7-叔丁基1-2,3-二氢-3,3-二甲基苯并呋喃衍生物作为胃肠道安全的抗炎和镇痛药：5-酮取代基的发现和变化。

New cyclooxygenase-2/5-lipoxygenase inhibitors. 3. 7-tert-butyl-2, 3-dihydro-3,3-dimethylbenzofuran derivatives as gastrointestinal safe antiinflammatory and analgesic agents: variations at the 5 position.

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