Olgen Süreyya, Ozkan Semiha
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Ankara University, 06100, Tandogan, Ankara, Turkey.
Z Naturforsch C J Biosci. 2009 Mar-Apr;64(3-4):155-62. doi: 10.1515/znc-2009-3-401.
3-Substituted benzylidene-1,3-dihydro-indoline derivatives were tested for their in vitro antibacterial activity against the Gram-negative bacteria Klebsiella pneumoniae, Pseudomonas aeruginosa, Escherichia coli, and the Gram-positive bacteria Bacillus subtilis, Staphylococcus aureus, and for their their in vitro antifungal activity against Candida krusei and Candida albicans. The minimum inhibitory concentration (MIC) values were determined by the 2-fold serial dilution technique in Mueller Hinton broth and Sabouraud dextrose agar using antibacterial and antifungal assays, respectively. For comparison of the antimicrobial activity, rifampicin, ampicillin trihydrate, gentamicin sulfate, and ofloxacin were used as reference antibacterial agents, and fluconazole and amphotericin B were employed as reference antifungal agents. The most active compound 10 showed notable inhibition against Bacillus subtilis, Staphylococcus aureus, and Candida krusei. Compounds 1 and 6 were found slightly effective against Klebsiella pneumoniae and Escherichia coli. In addition, compounds 13 and 14 showed inhibition against Bacillus subtilis and Staphylococcus aureus. Indole derivatives were also tested in vitro for replication of the HepAD38 cell line and compared with lamivudine (3TC, L-2',3'-dideoxy-3'-thiacytidine). The IC50 values of the compounds were found to be >1000 microM against HBV except for compound 13 which exhibited activity with an IC50 value of 500 microM.
对3-取代亚苄基-1,3-二氢吲哚衍生物进行了体外抗菌活性测试,测试对象包括革兰氏阴性菌肺炎克雷伯菌、铜绿假单胞菌、大肠杆菌,以及革兰氏阳性菌枯草芽孢杆菌、金黄色葡萄球菌,还测试了其对克鲁斯念珠菌和白色念珠菌的体外抗真菌活性。最低抑菌浓度(MIC)值分别通过在 Mueller Hinton肉汤和沙氏葡萄糖琼脂中采用抗菌和抗真菌试验的2倍系列稀释技术来确定。为了比较抗菌活性,使用利福平、三水合氨苄西林、硫酸庆大霉素和氧氟沙星作为参考抗菌剂,使用氟康唑和两性霉素B作为参考抗真菌剂。活性最高的化合物10对枯草芽孢杆菌、金黄色葡萄球菌和克鲁斯念珠菌表现出显著抑制作用。发现化合物1和6对肺炎克雷伯菌和大肠杆菌有轻微效果。此外,化合物13和14对枯草芽孢杆菌和金黄色葡萄球菌有抑制作用。还在体外测试了吲哚衍生物对HepAD38细胞系复制的影响,并与拉米夫定(3TC,L-2',3'-二脱氧-3'-硫代胞苷)进行比较。除化合物13的IC50值为500 microM表现出活性外,其他化合物对乙肝病毒的IC50值均>1000 microM。