Khan K A, Khan S A, Khalid S M, Ahmed A, Siddiqui B S, Saleem R, Siddiqui S, Faizi S
Department of Microbiology, University of Karachi, Pakistan.
Arzneimittelforschung. 1994 Aug;44(8):972-5.
Twenty-one derivatives of 8-hydroxyquinoline (oxine, 8H, CAS 148-24-3) were prepared and characterized by UV, IR, MS and NMR spectroscopy. Four of these derivatives, N-butyl, 8-butyloxyquinolinium bromide (HBD), 8-pentyloxyquinoline (HPEM), N-pentyl, 8-pentyloxyquinolinium bromide (HPED) and N-benzyl, 8-benzyloxy quinolinium chloride (HBED) are new and reported for the first time. The antimicrobial activity of these compounds was carried out in vitro against 11 Gram positive and 18 Gram negative bacteria, and 18 fungi including 9 dermatophytes, 7 other filamentous fungi and 2 Candida species. Three compounds namely, HPRD, HPED and HBED were found to possess significant antibacterial activity in order of HPED > HPRD > HBED, whereas 4 were found to possess significant antifungal activity in order of 8H > HT > HPEM > 8B.
制备了21种8-羟基喹啉(8-羟基喹啉,8H,CAS 148-24-3)衍生物,并通过紫外、红外、质谱和核磁共振光谱对其进行了表征。其中四种衍生物,N-丁基-8-丁氧基喹啉溴化物(HBD)、8-戊氧基喹啉(HPEM)、N-戊基-8-戊氧基喹啉溴化物(HPED)和N-苄基-8-苄氧基喹啉氯化物(HBED)是新化合物,首次报道。对这些化合物的抗菌活性进行了体外测试,针对11种革兰氏阳性菌、18种革兰氏阴性菌以及18种真菌,包括9种皮肤癣菌、7种其他丝状真菌和2种念珠菌属。发现三种化合物,即HPRD、HPED和HBED具有显著的抗菌活性,活性顺序为HPED > HPRD > HBED,而发现4种化合物具有显著的抗真菌活性,活性顺序为8H > HT > HPEM > 8B。