Antimicrobial action of arylsulfonamides bearing (aza)norbornane and related motifs: evaluation of new promising anti-MRSA agents
作者:Vitalii Palchykov、Nazar Manko、Nataliya Finiuk、Rostyslav Stoika、Mykola Obushak、Nazariy Pokhodylo
DOI:10.1007/s00044-021-02827-1
日期:2022.2
possessed high antibacterial activity towards gram-negative bacteria P. aeruginosa (ATCC9027) with the MIC value of 460–555 µM. According to the results of toxicity studies of the compounds to HEK-293, HaCaT, Balb/c 3T3, red blood cells and normal mitogen-activated lymphocytes, three compounds - VP-4556, VP-4604 and VP-4509 - bearing azanorbornene, octahydro-3,5-methanocyclopenta[b]pyrrole and bio-isosteric
评估了带有(氮杂)降冰片烷和相关基序的芳基磺酰胺:(1)对五种关键 ESKAPE 致病菌、一种革兰氏阳性菌耐甲氧西林金黄色葡萄球菌(MRSA,ATCC 43300)、四种革兰氏阴性菌、大肠杆菌的抗菌活性(ATCC 25922)、肺炎克雷伯菌(ATCC 700603)、鲍曼不动杆菌(ATCC 19606) 和铜绿假单胞菌(ATCC 27853),以及 (2) 对两种致病真菌菌株的抗真菌活性 -新型假丝酵母念珠菌( Candida ATCC28853) 。格鲁比(H99; ATCC 208821)。四种具有 4-硝基苯磺酰胺基序的化合物 (VP-4556、VP-4604、VP-4605和VP-4509 ) 对耐甲氧西林金黄色葡萄球菌(ATCC 43300 ) 表现出高毒性,MIC 值为 14.7–49.3 µM。这些化合物还对革兰氏阴性菌铜绿假单胞菌(ATCC9027)具有高抗菌活性,MIC 值为