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1,3,5‐Triazino Peptide Derivatives: Synthesis, Characterization, and Preliminary Antileishmanial Activity
ChemMedChem ( IF 3.4 ) Pub Date : 2018-02-20 , DOI: 10.1002/cmdc.201700770
Sherine N. Khattab 1, 2 , Hosam H. Khalil 1 , Adnan A. Bekhit 2, 3 , Mohamed M. Abd El-Rahman 1 , Beatriz G. de la Torre 4 , Ayman El-Faham 1, 5 , Fernando Albericio 5, 6, 7, 8
Affiliation  

A library of short di‐, tri‐, and tetra‐peptides with an s‐triazine moiety at the N terminus and either an amide or ethyl ester C terminus was prepared in solution and on the solid phase. The two remaining positions of the s‐triazine moiety were substituted with methoxy, morpholino, or piperidino groups. All the synthesized peptide derivatives were analyzed by HPLC and fully characterized by IR spectroscopy, 1H and 13C NMR spectroscopy, elemental analysis, and mass spectrometry (MALDI TOF/TOF). A preliminary study of the antileishmanial activity of the 1,3,5‐triazinyl peptide derivatives revealed that four dipeptide amide derivatives showed higher antipromastigote or antiamastigote activity than the reference standard drug miltefosine with no significance acute toxicity.

中文翻译:

1,3,5-Triazino肽衍生物:合成,表征和初步的抗leishmanial活动。

在溶液中和固相上制备了一个短的二肽,三肽和四肽文库,在N端带有s - triazine部分,在酰胺或乙酯C端都有一个。s-三嗪部分的其余两个位置被甲氧基,吗啉代或哌啶子基取代。所有合成的肽衍生物均通过HPLC进行分析,并通过红外光谱,1 H和13进行了全面表征13 C NMR光谱,元素分析和质谱(MALDI TOF / TOF)。对1,3,5-三嗪基肽衍生物的抗疟原虫活性的初步研究表明,四种二肽酰胺衍生物显示出比参比标准药物miltefosine更高的抗前鞭毛体或抗鞭毛体活性,而没有明显的急性毒性。
更新日期:2018-02-20
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