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Yeni Bir Kolesistokinin Dipeptoid Analoğunun ve Stereoizomerlerinin Sentezi, Antidepresan ve Antinosiseptif Etkilerinin İncelenmesi

Year 2004, Issue: 2, 57 - 64, 01.06.2004

Abstract

Bu çalışmada, yeni CCK-analoglarının geliştirilmesinde öncü bileşik olarak belirlenmiş olan R,S -Boc-Trp-Phe-NH2 M0 bileşiğinin yapısı moleküle sterik etki ve ek hidrojen bağlanma bölgesi kazandırmak amacıyla modifiye edilerek, R,R , S,S , R,S ve S,R -Boc-Trp-Phe-COmorfolidid M1-M4 türevleri konvensiyonel sıvı faz peptit sentez metodu kullanılarak sentezlenmiş ve yapıları spektral analizlerle açıklanmıştır. Elde edilen bileşiklerin antinosiseptif etkileri tail clip, tail flick ve hot plate testleri ile, antidepresan etkileri ise Porsolt’un zorlu yüzdürme testi ile farelerde değerlendirilmiştir. Sonuçlar yapı-aktivite ilişkileri yönünden incelenmiştir.

Synthesis and Investigation of Antinociceptive and Antidepressant Effects of the Stereoisomers of a New Dipeptoid Analog of Cholecystokinin

Year 2004, Issue: 2, 57 - 64, 01.06.2004

Abstract

In this study, the dipeptide M0, R,S -Boc-Trp-Phe-NH2, designated as the chemical lead for the development of new CCK analogues, and the stereoisomers of its analog modified at the N-terminal by morpholine moiety which brings about sterical effect and adds an additional hydrogen binding site to the molecule. R,R , S,S , R,S and S,R -Boc-Trp-Phe- CO-morpholidide M1-M4 were synthesized by conventional solution –phase peptide synthesis and structures elucidated by spectral analysis. The compounds thus obtained were subjected to antinociceptive tests including mouse tail clip, tail flick and hot plate and antidepressant effects were evaluated by Porsolt’s Forced Swimming Test. The results elucidated by SAR Structure activity relationship studies .

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Details

Primary Language English
Journal Section Research Article
Authors

Akgül Yeşilada This is me

M.berna Asal Altıparmak This is me

Engin Yıldırım This is me

Kevser Erol This is me

Publication Date June 1, 2004
Published in Issue Year 2004 Issue: 2

Cite

Vancouver Yeşilada A, Altıparmak MA, Yıldırım E, Erol K. Synthesis and Investigation of Antinociceptive and Antidepressant Effects of the Stereoisomers of a New Dipeptoid Analog of Cholecystokinin. HUJPHARM. 2004(2):57-64.