摘要 |
<p>The invention relates to compounds of the formula <CHEM> wherein R is hydrogen, lower alkyl, -(CH2)2N(R<3>)2 or -CH2OOCR<3> wherein R3 is lower alkyl; R<1> is CH3(CH2)n-, wherein n is 9-17, or R<4>(CH2)p-, wherein p is 3-10 and R<4> is 1- or 2-naphthyloxy, 2,3- or 3,4-dihydroxyphenyl, 2,3- or 3,4-dibenzyloxyphenyl, phenyl, phenoxy, or substituted phenyl or phenoxy wherein the substituent is selected from the group consisting of hydroxy, benzyloxy, methylsulfinyl, methylsulfonyl or phenyl; R<2> is R<4>(CH2)p- , 1-adamantyl-CO- or diphenylmethyl-CO-, and, when R is hydrogen, a pharmaceutically acceptable salt with a base. The compounds of formula I are potent inhibitors of phospholipases A2 (PLA2's) and are therefore useful in the treatment of diseases, such as psoriasis, inflammatory bowel disease, asthma, allergy, arthritis, dermatitis, gout, pulmonary disease, myocardial ischemia, and trauma induced inflammation, such as spinal cord injury.</p> |