## Abstract **Summary:** The controlled polymerisation of a bulky, peptide‐based monomer was investigated. The cyclic __β__‐sheet forming decapeptide gramicidin S was modified with a methacrylate handle and subsequently polymerised via atom transfer radical polymerisation (ATRP), to yield a well‐de
Synthesis and Biological Evaluation of Novel Gramicidin S Analogues
✍ Scribed by Adriaan Willem Tuin; Dimitrios Konstantinos Palachanis; Annelies Buizert; Gijsbert Marnix Grotenbreg; Emile Spalburg; Albert J. de Neeling; Roos H. Mars-Groenendijk; Daan Noort; Gijsbert A. van der Marel; Herman S. Overkleeft; Mark Overhand
- Publisher
- John Wiley and Sons
- Year
- 2009
- Tongue
- English
- Weight
- 624 KB
- Volume
- 2009
- Category
- Article
- ISSN
- 1434-193X
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Original 1,4-benzoxazine analogues of ellipticine were prepared using a general synthetic route that relied on an anionic ring annulation as the key transformation. The interest of this approach lies on the possibility of an easy entrance to a wide range of derivatives from the phenol intermediate.
## Abstract Gramicidin S (GS) is a cyclo‐decapeptide antibiotic isolated from __Bacillus brevis__. The structural studies have shown that GS forms a two‐stranded antiparallel β‐sheet imposed by two II′ β‐turns. Despite its wide Gram+ and Gram− antimicrobial spectrum, GS is useless in therapy becaus
## Abstract For Abstract see ChemInform Abstract in Full Text.
Three types of novel triptolide analogues with 9,11-olefin (3-5), five-membered unsaturated lactam ring (6-7) or A/B cis ring junction (8-14) were synthesized. Although with 9,11-olefin instead of 9,11-β-epoxide, compound 4a was much more active than the parent natural triptolide (1) with the lowest