Abdel Monaim Shimaa A H, Ramchuran Estelle J, El-Faham Ayman, Albericio Fernando, de la Torre Beatriz G
Catalysis and Peptide Research Unit, School of Health Sciences, University of KwaZulu-Natal , Durban 4001, South Africa.
Department of Chemistry, College of Science, King Saud University , P.O. Box 2455, Riyadh 11451, Saudi Arabia.
J Med Chem. 2017 Sep 14;60(17):7476-7482. doi: 10.1021/acs.jmedchem.7b00834. Epub 2017 Aug 23.
Teixobactin is a head to side chain cyclodepsipeptide that contains two positive charges. One is found in the cycle, as a result of the presence of the guanidino-unusual amino acid L-allo-End, while the other is at the N-terminal. Here we introduce 26 new Teixobactin analogues with an increasing number of positive charges. In an attempt to fine-tune the biological activity of Teixobactin, we examined the effect of cationicity on the SAR of these analogues. The maximum number of positive charges to maintain the activity are three to four. Analogues with five positive charges show the lowest activity.
替考拉宁是一种含有两个正电荷的头对侧链环缩肽。其中一个正电荷存在于环中，这是由于胍基不寻常的氨基酸L-别异亮氨酸的存在，而另一个正电荷位于N端。在此，我们引入了26种带正电荷数量递增的新型替考拉宁类似物。为了微调替考拉宁的生物活性，我们研究了阳离子性对这些类似物构效关系的影响。维持活性的正电荷最大数量为三到四个。带有五个正电荷的类似物活性最低。
