Moore G G, Harrington J K, Swingle K F
J Med Chem. 1975 Apr;18(4):386-91. doi: 10.1021/jm00238a013.
A series of isosteres of 3-benzoyltrifluoromethanesulfonanilide involving alternatives to the carbonyl linking group was synthesized and screened for antiinflammatory activity in the carrageenan rat paw edema test. The systems examined were of the type m-CF3SO2NH-C6H4-X-C6H5, where X was -CROH-, -CHR-, -CH(OH)CH2-, -COCH2-, -CH2CO-, greater than C equal to CR2, -CR equal to CH, -C identical to C-, -CH2CH2-, CONH-, -NR-, -O-, -S(O)n- (n equal to 0,1,2), and carbon-carbon single bond. Many ortho and para derivatives were also tested. Several of these new trifluoromethanesulfonanilides proved equipotent with phenylbutazone. The effects on the anticarrageenan activity of both the nature and ring position of X are discussed.
合成了一系列3-苯甲酰基三氟甲磺酸苯胺的电子等排体，其中羰基连接基团被其他基团替代，并在角叉菜胶致大鼠足趾肿胀试验中筛选其抗炎活性。所研究的体系为m-CF3SO2NH-C6H4-X-C6H5类型，其中X为-CROH-、-CHR-、-CH(OH)CH2-、-COCH2-、-CH2CO-、大于C等于CR2、-CR等于CH、-C≡C-、-CH2CH2-、CONH-、-NR-、-O-、-S(O)n-（n等于0、1、2）以及碳-碳单键。还测试了许多邻位和对位衍生物。这些新型三氟甲磺酸苯胺中的几种被证明与保泰松具有同等效力。讨论了X的性质和环位置对角叉菜胶活性的影响。
