TY - JOUR ID - 39770 TI - Synthesis of Some Analogues of Polymyxin E1 Antibiotic Using Automated Solid Phase Peptide Synthesis Assisted With Microwave Irradiation JO - Egyptian Journal of Chemistry JA - EJCHEM LA - en SN - 0449-2285 AU - Hamza, Asmaa Mohamed AU - Kalmouch, Atef Abdel Monem AU - El-Mowafi, Shaima Ahmed AU - Rabie, Abdel gawad Mohamed AU - Zewail, Mohamed AD - Peptide Chemistry Department, Chemical Industries Research Division, National Research Centre, Cairo, Egypt AD - Faculty of Science, Ain Shams University, Cairo, Egypt Y1 - 2019 PY - 2019 VL - 62 IS - Special Issue (Part 2) Innovation in Chemistry SP - 505 EP - 522 KW - Amino acids KW - Polymyxin E1 KW - Automated Solid Phase Peptide Synthesis KW - Microwave irradiation KW - Fmoc- strategy DO - 10.21608/ejchem.2019.13547.1839 N2 - Five analogues of Polymyxin E1 antibiotic were synthesized via Fmoc- solid phase peptide synthesis (SPPS) strategy using Biotage® Initiator+Alstra™ microwave peptide synthesizer. The aim of this work is to study the importance of the cyclization conditions of the lactam ring on the purity and yield of the final compounds. For this purpose, replacing L-Thr10 with L-Asp allowed the application of different cyclization methodologies. In all analogues, the Dab5,8,9 residues were replaced with Arg, while the Dab4 residue involved in lactam cyclization was replaced with Lys. Modification of the linear tripeptide tail was applied to two of the analogues. The obtained compounds were characterized with different spectroscopic techniques and will be tested for their antimicrobial activity. UR - https://ejchem.journals.ekb.eg/article_39770.html L1 - https://ejchem.journals.ekb.eg/article_39770_64776f9072958fe863ae34f6e9c0cce4.pdf ER -