Kobayashi Intetsu, Muraoka Hiroe, Hasegawa Miyuki, Saika Takeshi, Nishida Minoru, Kawamura Makoto, Ando Ryoichi
Chemotherapy Division, Mitsubishi Kagaku Bio-Clinical Laboratories, 3-30-1 Shimura, Itabashi-ku, Tokyo 174-8555, Japan.
J Antimicrob Chemother. 2002 Jul;50(1):129-32. doi: 10.1093/jac/dkf106.
The antibacterial activity of BAS-118, a new benzamide derivative, against Helicobacter pylori and other species of bacteria was investigated, as was the in vitro ability of the compound to induce drug resistance in H. pylori. The MICs of BAS-118 for 155 isolates of H. pylori, including 30 clarithromycin (CAM)-resistant isolates (MIC > or= 1.56 mg/L) and 25 metronidazole (MNDZ)-resistant isolates (MIC >or = 6.25 mg/L), and 29 reference strains of other genera were determined by an agar dilution method. The MIC(50), MIC(90) and MIC range of BAS-118 for 100 randomly selected isolates of H. pylori were <or =0.003, 0.013 and < or =0.003-0.025 mg/L, respectively, with similar values obtained for CAM- and MNDZ-resistant isolates. Furthermore, MICs of BAS-118 for five H. pylori strains increased no more than two-fold after 10 serial passages in the presence of subinhibitory concentrations. BAS-118 exhibited a low antibacterial activity against the 29 non-H. pylori strains, with MICs of >or =8 mg/L. In summary, BAS-118 is a novel anti-H. pylori agent with a potent and selective antibacterial activity, which includes CAM- and MNDZ-resistant isolates. Furthermore, BAS-118 does not appear to induce drug resistance readily in vitro.
研究了新型苯甲酰胺衍生物BAS - 118对幽门螺杆菌及其他细菌的抗菌活性，以及该化合物在体外诱导幽门螺杆菌产生耐药性的能力。采用琼脂稀释法测定了BAS - 118对155株幽门螺杆菌（包括30株对克拉霉素（CAM）耐药菌株（MIC≥1.56 mg/L）和25株对甲硝唑（MNDZ）耐药菌株（MIC≥6.25 mg/L））以及29株其他属参考菌株的最低抑菌浓度（MIC）。随机选取的100株幽门螺杆菌菌株中，BAS - 118的MIC50、MIC90和MIC范围分别≤0.003、0.013和≤0.003 - 0.025 mg/L，对CAM和MNDZ耐药菌株也得到了类似的值。此外，在亚抑菌浓度存在下连续传代10次后，BAS - 118对5株幽门螺杆菌菌株的MIC增加不超过两倍。BAS - 118对29株非幽门螺杆菌菌株的抗菌活性较低，MIC≥8 mg/L。总之，BAS - 118是一种新型抗幽门螺杆菌药物，具有强大的选择性抗菌活性，包括对CAM和MNDZ耐药的菌株。此外，BAS - 118在体外似乎不容易诱导耐药性。
