The synthesis of alternative diketopiperazines as potential RGD mimetics
✍ Scribed by Nikolett Mihala; Antal Csámpai; Janez Ilaš; Danijel Kikelj; Robert Kiss; Helga Süli-Vargha
- Publisher
- John Wiley and Sons
- Year
- 2006
- Tongue
- English
- Weight
- 216 KB
- Volume
- 12
- Category
- Article
- ISSN
- 1075-2617
- DOI
- 10.1002/psc.776
No coin nor oath required. For personal study only.
📜 SIMILAR VOLUMES
RGD analogs bind to integrin receptors with high affinity and therefore have the potential to be used as vectors for the targeted delivery of pharmaceutical agents to designated sites. Critical to this application is the ability to synthesize RGD analogs with different side chain functional groups t
AIImraet The ~ of two ~ mimetics of RGD, ct-Tfm-Arg-Gly-Asp-Phe-NHz 9 anti ct-Tfm-Arg431y-Asp-NH-(CH2h-C6Hs 13, is desmb~ The precursor of ct-Tfin-omithine was obtained in two s~ steps from 2-N-C~-2-T[m-hexkncdiaO\_ " \_\_'d\_-l-all~-! ester and introduced into the peptide chain by tz-catboxy-group
The flmt short syntheds of the @eptIde mimetic (3s. 8S. SS)-8-amlnc-6-oxctndotiridiW-cafhoxyfk add 1 and its zpmtected dedvatlve 9 is described, empkyfng the Schoallkcpf bkkctim-ether methodokgy, folkwed by a highly specific lntramokcufar reductive afnfnatkn and spontaneous kctamizatlon. These W-fus
Short syntheses are presented of the pseudo-dipeptide (3S,6S)-6-[(benzyloxy)carbonyl]amino-5-oxo-1,2,3,5,6,7-hexahydro-3-indolizinecarboxylic acid (1a) and of its (3S,6R) diastereoisomer (1b). The key step involves adding vinylogous b-enaminoester derived from pyroglutamic acid on an acrylate deriva
The lower molecular weight analog 12 of sialyl Lewis x was prepared and effected equal binding affinity to E-and P-selectin compared to the parent tetrasaccharide. If 12 was prepared using acidic ion exchange resins, false positive test were produced, especially binding to P-selectin seemed to be co