دورية أكاديمية
Synthesis and structure–activity relationships of novel arylpiperazines as potent antagonists of α1-adrenoceptor
| العنوان: | Synthesis and structure–activity relationships of novel arylpiperazines as potent antagonists of α1-adrenoceptor |
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| المؤلفون: | R. O. Silva, A. S. de Oliveira, L. F. Nunes Lemes, L. de Camargo Nascente, P. Coelho do Nascimento Nogueira, E. R. Silveira, G. D. Brand, A. Cilia, E. Poggesi, M. Buccioni, G. Marucci, M. L. Bolognesi, L. A. S. Romeiro, G. Vistoli |
| المساهمون: | R.O. Silva, A.S. de Oliveira, L.F. Nunes Leme, L. de Camargo Nascente, P. Coelho do Nascimento Nogueira, E.R. Silveira, G.D. Brand, G. Vistoli, A. Cilia, E. Poggesi, M. Buccioni, G. Marucci, M.L. Bolognesi, L.A.S. Romeiro |
| بيانات النشر: | Elsevier Masson SAS |
| سنة النشر: | 2016 |
| المجموعة: | The University of Milan: Archivio Istituzionale della Ricerca (AIR) |
| مصطلحات موضوعية: | Adrenergic receptors subtype, Arylpiperazine, BPH, α1-Adrenergic antagonist, Drug Discovery3003 Pharmaceutical Science, Organic Chemistry, Pharmacology, Settore CHIM/08 - Chimica Farmaceutica |
| الوصف: | Arylpiperazines 2–11 were synthesized, and their biological profiles at α1-adrenergic receptors (α1-ARs) assessed by binding assays in CHO cells expressing human cloned subtypes and by functional experiments in isolated rat vas deferens (α1A), spleen (α1B), and aorta (α1D). Modifications at the 1,3-benzodioxole and phenyl phamacophoric units resulted in the identification of a number of potent compounds (moderately selective with respect to the α1b-AR), in binding experiments. Notably, compound 7 (LDT451) showed a subnanomolar pKi of 9.41 towards α1a-AR. An encouragingly lower α1B-potency was a general trend for all the series of compounds, which showed α1A/D over α1B selectivity in functional assays. If adequately optimized, such peculiar selectivity could have relevance for a potential LUTS/BPH therapeutic application. |
| نوع الوثيقة: | article in journal/newspaper |
| اللغة: | English |
| العلاقة: | info:eu-repo/semantics/altIdentifier/pmid/27448917; info:eu-repo/semantics/altIdentifier/wos/WOS:000383003900051; volume:122; firstpage:601; lastpage:610; numberofpages:10; journal:EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY; http://hdl.handle.net/2434/451508Test; info:eu-repo/semantics/altIdentifier/scopus/2-s2.0-84978524277; http://www.journals.elsevier.com/european-journal-of-medicinal-chemistryTest/ |
| DOI: | 10.1016/j.ejmech.2016.06.052 |
| الإتاحة: | https://doi.org/10.1016/j.ejmech.2016.06.052Test http://hdl.handle.net/2434/451508Test http://www.journals.elsevier.com/european-journal-of-medicinal-chemistryTest/ |
| رقم الانضمام: | edsbas.F66F45A6 |
| قاعدة البيانات: | BASE |
| DOI: | 10.1016/j.ejmech.2016.06.052 |
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