کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10584228 | 981327 | 2014 | 19 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A1 adenosine receptor
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کلمات کلیدی
[3H]DPCPXERGN-bromosuccinimideEWGCCPANBSGPCRs2-chloro-N6-cyclopentyladenosine - 2-کلرو-N6-سیکلوپنتیلادنوئینcAMP - cAMPG protein-coupled receptors - G گیرنده های پروتئینی همراهCyclic adenosine monophosphate - آدنوزین مونوفسفات CyclicCho - برایChinese Hamster Ovary - تخمدان هامستر چینیCNS - دستگاه عصبی مرکزیCesium fluoride - سدیم فلورایدcentral nervous system - سیستم عصبی مرکزیCSF - مایع مغزی نخاعیAllosteric modulation - مدولاسیون آلوستریکelectron-withdrawing group - گروه اخراج الکترونA1 adenosine receptor - گیرنده آدنوزین A1
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A1 adenosine receptor Synthesis and biological evaluation of novel 2-amino-3-aroyl-4-neopentyl-5-substituted thiophene derivatives as allosteric enhancers of the A1 adenosine receptor](/preview/png/10584228.png)
چکیده انگلیسی
2-Amino-3-benzoyl thiophenes have been widely reported to act as allosteric enhancers at the A1 adenosine receptor. Their activity can be increased considerably by appropriate substitutions at the 4- and 5-positions of the thiophene ring. Substituent size at the thiophene C-4 position seemed to be a factor closely related to activity, with the 4-neopentyl (2,2-dimethylpropyl) substitution showing the greatest enhanced activity. A wide series of 2-amino-3-aroyl-4-neopentylthiophene derivatives with general structure 3, characterized by the presence of different substituents (bromine, aryl and heteroaryl) at the 5-position of the thiophene ring, have been identified as potent AEs at the A1AR. With only one exception, all of the synthesized compounds proved to be superior to the reference compound PD 81,723 in a functional assay. Derivatives 3p, 3u, 3am, 3ap and 3ar were the most active compounds in binding (saturation and competition) and functional cAMP studies, being able to potentiate agonist [3H]CCPA binding to the A1 receptor.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 1, 1 January 2014, Pages 148-166
Journal: Bioorganic & Medicinal Chemistry - Volume 22, Issue 1, 1 January 2014, Pages 148-166
نویسندگان
Romeo Romagnoli, Pier Giovanni Baraldi, Maria Dora Carrion, Olga Cruz-Lopez, Carlota Lopez Cara, Giulia Saponaro, Delia Preti, Mojgan Aghazadeh Tabrizi, Stefania Baraldi, Allan R. Moorman, Fabrizio Vincenzi, Pier Andrea Borea, Katia Varani,