摘要 |
<p>PURPOSE:To obtain the subject new compounds, having carboxymethylene group at the 1-position and useful as an immunopotentiator or an antitumor agent having activating actions on a macrophage or an antiinflammatory agent, an immunosuppressant, etc., having suppressing actions on the activities of the macrophage. CONSTITUTION:These new 4-phosphonoglucosamines are expressed by formula I [R<1> is H or a protecting group of carboxyl group; R<2> and R<3> each is a halogen, a (protected)hydroxyl group or a (halogen-substituted)6-20C alkanoyl; R<4> is H, a 1-4C alkoxy, a (substituted)benzyl or a (substituted)phenyl; R<5> is H or a protecting group of hydroxyl group; (n) is 1-18] and have activating actions on a macrophage or suppressing actions on the activities of the macrophage. The compounds having the former actions are useful as an immunopotentiator or an antitumor agent and the compounds having the latter actions are useful as an antiinflammatory agent, an antiautoimmune disease agent or an immunossuppressant. Furthermore, the compounds are obtained by carboxymethylenating hydroxyl group at the 1-position and phosphonylating hydroxyl group at the 4-position of protected glucosamines expressed by formula II (Ac is acetyl).</p> |