Synthesis, Conformational Studies and Biological Profiles of Tetrahydrofuran Amino‐Acid‐Containing Cationic Antitubercular Peptides,Asian Journal of Organic Chemistry

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Synthesis, Conformational Studies and Biological Profiles of Tetrahydrofuran Amino‐Acid‐Containing Cationic Antitubercular Peptides
Asian Journal of Organic Chemistry ( IF 2.8 ) Pub Date : 2017-06-08 , DOI: 10.1002/ajoc.201700183
Sudip Pal ₁ , Uttam Ghosh ₂ , Gajendra Singh _{3,

4} , Faiyaz Alam _{3,

4} , Shyam Singh ₅ , Sidharth Chopra ₆ , Sudhir Sinha ₅ , Ravi Sankar Ampapathi _{3,

4} , Tushar Kanti Chakraborty _{1,

2}

Affiliation

Linear cationic tetra‐ and octapeptides containing a tetrahydrofuran amino acid were synthesised, a conformational analysis performed, and their structure–activity relationships explored by evaluating their antibacterial, antitubercular and cytotoxic properties. Only the octapeptides showed activities, which was weak to moderate against Gram‐positive and Gram‐negative bacteria for only two peptides, but was very significant against Mycobacterium tuberculosis, and peptides were devoid of toxicity towards mammalian Vero cells. N‐Terminus‐deprotected esters showed the best results with excellent selectivity for M. tuberculosis and these peptides promise to be potential leads.

中文翻译：

含四氢呋喃氨基酸的阳离子抗结核肽的合成，构象研究和生物学特征

合成了包含四氢呋喃氨基酸的线性阳离子四肽和八肽，进行了构象分析，并通过评估其抗菌，抗结核和细胞毒性特性探索了它们的结构-活性关系。仅八肽显示出活性，仅对两种肽对革兰氏阳性菌和革兰氏阴性菌具有弱至中度的活性，但对结核分枝杆菌却具有非常显着的活性，并且该肽对哺乳动物的Vero细胞没有毒性。N-末端脱保护的酯对结核分枝杆菌显示出最佳结果，并具有出色的选择性，这些肽有望成为潜在的先导。

更新日期：2017-06-08

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