Kondo Y, Toida T, Kusano G, Imai J
J Pharmacobiodyn. 1980 Jan;3(1):41-5. doi: 10.1248/bpb1978.3.41.
The relationships between the structure and inhibitory activity against the formation of acid-fastness in mycobacterial organisms were investigated in naturally occurring or synthetic coumarins and cinnamates. The presence of an OH-group at C7 in the coumarin nucleus proved to be essential for the inhibitory activity. Likewise, the presence of a para-OH-group in cinnamates is also essential. Reduction of a conjugated alpha, beta-double bond in both series resulted in a decrease of the ininhibitory activity. Shortening of the side chain of cinnamates resulted in total loss of the activity. The grouping -C-C-CO2R appeared to be necessary for retaining the inhibitory activity.
在天然存在的或合成的香豆素和肉桂酸酯中，研究了其结构与对分枝杆菌抗酸性形成的抑制活性之间的关系。香豆素核中C7位存在羟基被证明对抑制活性至关重要。同样，肉桂酸酯中对羟基的存在也是必不可少的。两个系列中共轭α，β-双键的还原导致抑制活性降低。肉桂酸酯侧链的缩短导致活性完全丧失。-C-C-CO2R基团似乎是保持抑制活性所必需的。
