Zołnowska Beata, Sławiński Jarosław, Grzonek Aleksandra, Kędzia Anna, Kwapisz Ewa, Kawiak Anna
Pol J Microbiol. 2015;64(3):299-305.
A series of N-substituted N'-(2-alkylthio-4-chloro-5-methylbenzenesulfonyl)guanidine derivatives bearing sulfonamide moiety have been screened in vitro for antibacterial activity against isolates from patients with infections of oral cavity, respiratory tract and intestinal tract. The majority of compounds exhibited good antibacterial potency. 1-[4-Chloro-5-methyl-2-(4-trifluoromethylbenzylthio)benzenesulfonyl]-3-(3-sulfamoylphenyl)guanidine (13) showed very strong activity, with MIC ≤ 6.2 μg/ml against eleven bacteria strains belonged to Gram-positive anaerobes and aerobes. Furthermore, compound 13 exhibited promising activity toward highly resistant microorganisms such as methicillin-resistant Staphylococcus aureus and Enterococcusfaecalis. It was found that Parvimonas micra, Finegoldia magna, Peptostreptococcus anaerobius, Propionibacterium acnes showed the highest susceptibility toward the investigated guanidines.
一系列带有磺酰胺部分的N-取代N'-(2-烷硫基-4-氯-5-甲基苯磺酰基)胍衍生物已在体外针对来自口腔、呼吸道和肠道感染患者的分离株进行了抗菌活性筛选。大多数化合物表现出良好的抗菌效力。1-[4-氯-5-甲基-2-(4-三氟甲基苄硫基)苯磺酰基]-3-(3-氨磺酰基苯基)胍(13)表现出非常强的活性，对11种革兰氏阳性厌氧菌和好氧菌的最低抑菌浓度≤6.2μg/ml。此外，化合物13对耐甲氧西林金黄色葡萄球菌和粪肠球菌等高耐药微生物表现出有前景的活性。发现微小消化链球菌、巨大卟啉单胞菌、厌氧消化链球菌、痤疮丙酸杆菌对所研究的胍类表现出最高的敏感性。
