Towards non-peptide ANG II AT1 receptor antagonists based on urocanic acid: rational design, synthesis and biological evaluation

A series of o-, m- and p-benzyl tetrazole derivatives 11a-c has been designed, synthesized and evaluated as potential Angiotensin II AT1 receptor antagonists, based on urocanic acid. Compound 11b with tetrazole moiety at the m-position showed moderate, however, higher activity compared to the o- and...

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Veröffentlicht in:	Amino acids 2011-02, Vol.40 (2), p.411-420
Hauptverfasser:	Agelis, George, Resvani, Amalia, Matsoukas, Minos-Timotheos, Tselios, Theodore, Kelaidonis, Konstantinos, Kalavrizioti, Dimitra, Vlahakos, Demetrios, Matsoukas, John
Format:	Artikel
Sprache:	eng
Schlagworte:	Analytical Chemistry Angiotensin Receptor Antagonists - chemical synthesis Angiotensin Receptor Antagonists - chemistry Angiotensin Receptor Antagonists - pharmacology Animals AT1 receptor Biochemical Engineering Biochemistry Biomedical and Life Sciences Cell Line Drug Design Humans Kinetics Life Sciences Male Models, Molecular Molecular modelling Neurobiology Original Article Pharmacophore Protein Binding Proteomics Rabbits Rats Receptors, Angiotensin - chemistry Receptors, Angiotensin - metabolism Structure-Activity Relationship Urocanic acid Urocanic Acid - chemistry
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Zusammenfassung:	A series of o-, m- and p-benzyl tetrazole derivatives 11a-c has been designed, synthesized and evaluated as potential Angiotensin II AT1 receptor antagonists, based on urocanic acid. Compound 11b with tetrazole moiety at the m-position showed moderate, however, higher activity compared to the o- and p-counterpart analogues. Molecular modelling techniques were performed in order to extract their putative bioactive conformations and explore their binding modes.
ISSN:	0939-4451 1438-2199
DOI:	10.1007/s00726-010-0651-y