Dauksas V, Gaidelis P, Petrauskas O, Udrenaite E
Faculty of Chemistry, Vilnius University, Lithuania.
Arzneimittelforschung. 1995 May;45(5):581-4.
2-Methyl-5-(3-phenylpropionyl)-1-benzoxolane (CAS 159264-96-7) was synthesized and studied for anti-inflammatory properties. This new aryl ketone was more active than the previously reported 5-acyl substituted 1-benzoxolanes except 5-cinnamoyl-2-methyl-1-benzoxolane (the unsaturated analogue) which exhibited similar anti-inflammatory activity and similar toxicity but was more gastrotoxic. Anti-inflammatory and analgesic effects of 2-methyl-5-(3-phenylpropionyl)-1-benzoxolane were less pronounced than those of indometacin but greater than those of acetylsalicylic acid (ASA). The new ketone was less toxic and less gastrotoxic than both the reference drugs mentioned above. Therapeutic indices of the new compound were significantly greater than those of ASA and indometacin.
合成了2-甲基-5-(3-苯基丙酰基)-1-苯并恶唑烷（CAS 159264-96-7）并对其抗炎特性进行了研究。这种新的芳基酮比之前报道的5-酰基取代的1-苯并恶唑烷更具活性，但5-肉桂酰基-2-甲基-1-苯并恶唑烷（不饱和类似物）除外，该类似物具有相似的抗炎活性和相似的毒性，但胃肠毒性更强。2-甲基-5-(3-苯基丙酰基)-1-苯并恶唑烷的抗炎和镇痛作用不如吲哚美辛明显，但强于乙酰水杨酸（ASA）。这种新酮的毒性和胃肠毒性均低于上述两种对照药物。新化合物的治疗指数显著高于ASA和吲哚美辛。
