| Title | From angiotensin to non-peptide angiotensin II receptor antagonists | |
| Authors | J. Hondrelis¹, J. Smith², A. Wahhab², R. Ganter², D. Moore², G. Moore² and J. Matsoukas¹
1. Department of Chemistry, University of Patras, Patras, Greece 2. Department of Pharmacology and Therapeutics, University of Calgary, Calgary Alberta, Canada |
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| Citation | Hondrelis, J., Smith, J., Wahhab, A., Ganter, R., Moore, D. et al.: From angiotensin to non-peptide angiotensin II receptor antagonists, Epitheorese Klin. Farmakol. Farmakokinet. 9(2-3): 71-73 (1995) | |
| Publication Date | 1995 | |
| Full Text Language | English | |
| Order – Buy | Ηλεκτρονική Μορφή: pdf (10 €) – Digital Type: pdf (10 €)
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| Keywords | Angiotensin II antagonists, peptidomimetic drugs, losartan derivatives. | |
| Other Terms | review article | |
| Summary | Since the first reported non-peptidic Angiotensin II (ANGII) receptor antagonists in 1982 much work has been published describing the design, synthesis and bioactivities of such antagonists. All these approaches focus on the same juxtaposition of substituents about the imidazole nucleus and maintain the same orientation of the imidazole ring. This has clearly defined the range of substituents tolerable for good antagonist activity and has provided valuable insights into the possible active conformation of ANGII. Understanding in this field will no doubt be broadened with the development of novel ANGII antagonists that utilize a heterocyclic nucleus other than the imidazole ring e.g. pyrrole, triazole, pyrimidine, imidazopyridine, imidazolone, but that maintain a similar pattern of substitution. However, no studies to date have examined the effect of changing the orientation of the imidazole nucleus in such antagonists. In the study, non-peptide ANGII antagonists related to DuP 753 were prepared and evaluated for antagonist activity in the rat isolated uterus assay. | |
| References | 1. A. Giannis, T. Kolter: Peptidomimetics for Receptor Ligands-Discovery, Development and Medical Perspectives. Angew. Chem. Int. Ed. Engl. 32.1244-1267 (1993)
2. A. Wahhab, J. Smith, R. Ganter, D. Moore, J. Hondrelis, J. Matsoukas, G. Moore: Imidazole based non-peptide Angiotensin II Receptor Antagonists: An investigation of the Effect of the Orientation of the Imidazole Ring on Biological Activity. Drug Res. 43: 1157-1168 (1993) 3. J. Smith, A. Wahhab, H. Hondrelis, R. G. Bater, D. Moore, G. Moore, J. Matsoukas: A new generation of antihypertensives: non-peptide angiotensin II receptor antagonists. BIOMED Euroworkshop proceedings, Oct. 14-15, Patras, Greece (1993) 4. J. Matsoukas, G. Agelis, J. Hondrelis, R. Yamdagni, Q. Wu, R. Ganter, J. Smith, D. Moore, G. Moore. Synthesis and biological activities of Angiotensin II, Sarilesin, and Sarmesin analogues containing Aze of Pip at position 7: Conformational properties of (Sar¹, Aze7] ANG 11 determined by Nuclear Overhauser Effect (NOE) En-hancement Spectroscopy. J. Med. Chem. 36: 904-911 (1993) 5. J. Matsoukas, J. Hondrelis, M. Keramida, T. Mavromoustakos, A. Makriyannis, R. Yamdagni, Q. Wu, G. J. Moore. Role of the NH2-terminal Domain of Angiotensin II (ANG II) and [Sar¹] Angiotensin II on Conformation and Activity. J. Biol. Chem.: (1994) |
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| Relative Papers |
Online ISSN 1011-6575
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Articles published in this Journal are Indexed or Abstracted in: • Chemical Abstracts • Elsevier’s Bibliographic Databases: Scopus, EMBASE, EMBiology, Elsevier BIOBASE SCImago Journal and Country Rank Factor
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| ΕΤΗΣΙΑ ΣΥΝΔΡΟΜΗ 1995 – ANNUAL SUBSCRIPTION 1995 | |
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