کد مقاله کد نشریه سال انتشار مقاله انگلیسی ترجمه فارسی نسخه تمام متن
1368529 981701 2016 3 صفحه PDF سفارش دهید دانلود کنید
عنوان انگلیسی مقاله
[Dmt1]DALDA analogues modified with tyrosine analogues at position 1
ترجمه فارسی عنوان
آنالوگ های [Dmt1]DALDA اصلاح شده با آنالوگ های تیروزین در موقعیت 1
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

Analogues of [Dmt1]DALDA (H-Dmt-d-Arg-Phe-Lys-NH2; Dmt = 2′,6′-dimethyltyrosine), a potent μ opioid agonist peptide with mitochondria-targeted antioxidant activity were prepared by replacing Dmt with various 2′,6′-dialkylated Tyr analogues, including 2′,4′,6′-trimethyltyrosine (Tmt), 2′-ethyl-6′-methyltyrosine (Emt), 2′-isopropyl-6′-methyltyrosine (Imt) and 2′,6′-diethyltyrosine (Det). All compounds were selective μ opioid agonists and the Tmt1-, Emt1 and Det1-analogues showed subnanomolar μ opioid receptor binding affinities. The Tmt1- and Emt1-analogues showed improved antioxidant activity compared to the Dmt1-parent peptide in the DPPH radical-scavenging capacity assay, and thus are of interest as drug candidates for neuropathic pain treatment.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 15, 1 August 2016, Pages 3629–3631
نویسندگان
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