Literature DB >> 16260110

Structure elucidation and conformational study of V8: a novel synthetic non peptide AT(1) antagonist.

Panagiotis Zoumpoulakis1, Aggeliki Politi, Simona Golic Grdadolnik, John Matsoukas, Thomas Mavromoustakos.   

Abstract

AT(1) antagonists constitute the most recent class of antihypertensive drugs which act through the Renin Angiotensin System (RAS). In an effort to comprehend their stereoelectronic features, a study was initiated to compare the conformational properties of drugs already marketed for the treatment of hypertension with synthetic ones, possessing common structural characteristics. In this study, the synthetic AT(1) antagonist V8 is structurally elucidated and its conformational properties are studied through a combination of NMR spectroscopy and computational analysis. Its conformational properties are compared with those of the structurally similar prototype AT(1) antagonist losartan.

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Year:  2005        PMID: 16260110     DOI: 10.1016/j.jpba.2005.09.016

Source DB:  PubMed          Journal:  J Pharm Biomed Anal        ISSN: 0731-7085            Impact factor:   3.935


  2 in total

1.  An efficient synthesis of a rationally designed 1,5 disubstituted imidazole AT(1) angiotensin II receptor antagonist: reorientation of imidazole pharmacophore groups in losartan reserves high receptor affinity and confirms docking studies.

Authors:  George Agelis; Panagiota Roumelioti; Amalia Resvani; Serdar Durdagi; Maria-Eleni Androutsou; Konstantinos Kelaidonis; Demetrios Vlahakos; Thomas Mavromoustakos; John Matsoukas
Journal:  J Comput Aided Mol Des       Date:  2010-07-10       Impact factor: 3.686

2.  Development of a CP 31P NMR broadline simulation methodology for studying the interactions of antihypertensive AT1 antagonist losartan with phospholipid bilayers.

Authors:  Charalambos Fotakis; Dionisios Christodouleas; Petros Chatzigeorgiou; Maria Zervou; Nikolas-Ploutarch Benetis; Kyriakos Viras; Thomas Mavromoustakos
Journal:  Biophys J       Date:  2009-03-18       Impact factor: 4.033

  2 in total

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