Brown R A, Fischer R, Blunk J, Durham N N, Remalingam K, Wong L F, Berlin K D
J Med Chem. 1977 May;20(5):664-9. doi: 10.1021/jm00215a009.
Pyrazole-, pyrazolone- and isoxazole-containing systems were prepared from 3,4-dihydro-6-(hexyloxy)-1(2H)-naphthalenone, 3,4-dihydro-6-(hexadecyloxy)-1(2H)-naphthalenone,3,4-dihydro-6(2-dimethylaminoethyloxy)-1-(2H)-naphthalenone, 3,4-dihydro-7-hexyloxy-1(2H)-phenanthrone, and 3,4-dihydro-7-(2-dimethylaminoethyloxy)-1(2H)-phenanthrone. A number of compounds derived from 7, 8-dihydro-5(6H)-quinolinone were also synthesized and characterized. Both hydrophilic and lipophilic groups were incorporated into certain systems as well as cidal groups. The compounds were screened for their in vitro inhibitory activity against Bacillus subtilis and Pseudomonas fluorescens. Structure-acitivity relationships among the molecular systems are discussed.
含吡唑、吡唑啉酮和异恶唑的体系由3,4-二氢-6-(己氧基)-1(2H)-萘酮、3,4-二氢-6-(十六烷氧基)-1(2H)-萘酮、3,4-二氢-6-(2-二甲基氨基乙氧基)-1-(2H)-萘酮、3,4-二氢-7-己氧基-1(2H)-菲酮以及3,4-二氢-7-(2-二甲基氨基乙氧基)-1(2H)-菲酮制备而成。还合成并表征了许多源自7,8-二氢-5(6H)-喹啉酮的化合物。亲水性基团和亲脂性基团以及杀菌基团都被引入到某些体系中。对这些化合物针对枯草芽孢杆菌和荧光假单胞菌的体外抑制活性进行了筛选。讨论了分子体系之间的构效关系。
