Saleh N A, Zwiefak A, Mordarski M, Pulverer G
Department of Microbiology, Polish Academy of Sciences, Wroclaw.
Zentralbl Bakteriol Mikrobiol Hyg A. 1988 Nov;270(1-2):160-70. doi: 10.1016/s0176-6724(88)80153-6.
The antibacterial activity of 33 substituted and unsubstituted seven-member ring tropones and tropolones was examined on 14 reference strains representing Gram-positive and Gram-negative bacteria. It was shown that the chemical character and position of the substituent plays a distinct role in the biological activity of investigated compounds. Depending on the substituent the antibacterial effect may be either increased or diminished. C-1 thio and C-2 nitro derivatives of tropone are significantly more active than tropone. The dibenzotropone derivatives display no antibacterial activity. Hydroxymethyl derivatives of tropolone are more active than tropolone, while hydroxy-, isopropyl-, methyl- as well as tropolone acetates are equipotent.
研究了33种取代和未取代的七元环卓酮和托酚酮对14种代表革兰氏阳性菌和革兰氏阴性菌的参考菌株的抗菌活性。结果表明，取代基的化学性质和位置对所研究化合物的生物活性起着显著作用。根据取代基的不同，抗菌效果可能增强或减弱。卓酮的C-1硫代和C-2硝基衍生物比卓酮活性显著更高。二苯并卓酮衍生物没有抗菌活性。托酚酮的羟甲基衍生物比托酚酮活性更高，而羟基、异丙基、甲基以及托酚酮乙酸酯的活性相当。
