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- Title
Synthesis, radioiodination and biological evaluation of novel dipeptide attached to triazole-pyridine moiety.
- Authors
Abdel-Ghany, I.; Moustafa, K.; Abdel-Bary, H.; Shamsel-Din, H.
- Abstract
A new dipeptide derivative, ethyl 2-(3-(4-hydroxyphenyl)-2-(2-(4-phenyl-5-((pyridin-4-ylamino)methyl)-4H-1,2,4-triazol-3-ylthio)acetamido)propanamido)-3-(1H-indol-3-yl)propanoate (EHPTIP) was successfully synthesized and radiolabeled with I by the direct electrophilic substitution method. The non radiolabeled compound (EHPTIP) was tested as an antimicrobial agent and the radiolabeled derivative was tested as a new imaging agent. The study results showed a good antimicrobial activity of EHPTIP and a good in vitro and in vivo stability of I-EHPTIP. The biodistribution of the radiolabeled compound showed a high brain uptake of 7.60 ± 0.01 injected activity/g tissue organ at 30 min post-injection and retention in brain remained high up to 1 h, whereas the clearance from the normal mice appeared to proceed via the renal system. Such brain uptake is better than that of currently used radiopharmaceuticals for brain imaging (Tc-ECD and Tc-HMPAO). As a conclusion, EHPTIP is a newly synthesized dipeptide with a good antimicrobial activity and the radioiodinated EHPTIP which is labeled with I could be used as a novel agent for brain SPECT.
- Subjects
CHEMICAL synthesis; DIPEPTIDES; RADIOIODINATION; TRIAZOLES; PYRIDINE; SUBSTITUTION reactions; ANTI-infective agents; RADIOLABELING; BRAIN imaging
- Publication
Journal of Radioanalytical & Nuclear Chemistry, 2013, Vol 295, Issue 2, p1273
- ISSN
0236-5731
- Publication type
Article
- DOI
10.1007/s10967-012-2237-5