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Design, synthesis and antimicrobial studies of some polymyxin analogues.
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-12-12 , DOI: 10.1038/s41429-019-0262-0 Hanqing Tang 1 , You Zhang 2 , Jie Ma 1 , Yuanzhen Dong 1 , Qi Gao 2 , Jun Feng 1, 2
The Journal of Antibiotics ( IF 2.1 ) Pub Date : 2019-12-12 , DOI: 10.1038/s41429-019-0262-0 Hanqing Tang 1 , You Zhang 2 , Jie Ma 1 , Yuanzhen Dong 1 , Qi Gao 2 , Jun Feng 1, 2
Affiliation
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To find novel polymycin analogues with high antimicrobial activities and low toxicity, 36 novel polymyxin analogues were synthesized, and in which TZ40-J and TZ40-K were evaluated for their antimicrobial activities using broth microdilution method and for their haemolytic toxicity with sterile sheep blood. Preliminary safety assessments of those two compounds were carried out via the MTT cell viability assay in vitro and acute toxicity assay in vivo. Experimental data demonstrated that TZ40-J and TZ40-K were less toxic and indicate higher activities against Pseudomonas aeruginosa than polymyxin B.
中文翻译：
一些多粘菌素类似物的设计，合成和抗菌研究。
为了找到具有高抗菌活性和低毒性的新型多霉素类似物，合成了36种新型多粘菌类似物，并使用肉汤微量稀释法评估了TZ40-J和TZ40-K的抗菌活性，以及用无菌羊血对它们的溶血毒性进行了评估。通过体外MTT细胞活力测定和体内急性毒性测定对这两种化合物进行了初步安全性评估。实验数据表明TZ40-J和TZ40-K的毒性较小，并表明其对铜绿假单胞菌的活性高于多粘菌素B。
更新日期：2019-12-12
中文翻译：
一些多粘菌素类似物的设计，合成和抗菌研究。
为了找到具有高抗菌活性和低毒性的新型多霉素类似物，合成了36种新型多粘菌类似物，并使用肉汤微量稀释法评估了TZ40-J和TZ40-K的抗菌活性，以及用无菌羊血对它们的溶血毒性进行了评估。通过体外MTT细胞活力测定和体内急性毒性测定对这两种化合物进行了初步安全性评估。实验数据表明TZ40-J和TZ40-K的毒性较小，并表明其对铜绿假单胞菌的活性高于多粘菌素B。
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