Conception et synthèse de nouvelles molécules bioactives duales : vers des composés antagonistes AT1 et agonistes PPAR[gamma]

Abstract : Some angiotensin II-type 1 receptor (AT1) antagonists, used for blood pressure control, exhibit also an activity on peroxisome proliferator activated receptor [gamma] (PPAR[gamma]), which is involved in the control of glucose metabolism. Such compounds could be promising drugs for the treatment of both hypertension and type II diabetes, which are often concomitant. Therefore, we have rationally designed molecules potentially able to interact with both receptors involved in these diseases. We used the "design multiple ligands" concept, as previously developed by industrial pharmacists, to build up a diversified molecule set via combination of both pharmacophores of AT1 and PPAR[gamma] receptor antagonists and agonists, respectively. Molecular modeling experiments (docking) on PPAR[gamma] were conducted to rationalise the synthesis and allow us to predict in some extent the agonistic activity of the studied compounds
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Theses
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http://docnum.univ-lorraine.fr/prive/DDOC_T_2013_0221_MEYER.pdf
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https://hal.univ-lorraine.fr/tel-01750517
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Submitted on : Thursday, March 29, 2018 - 12:48:10 PM
Last modification on : Friday, March 30, 2018 - 1:28:45 AM

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Maxime Meyer. Conception et synthèse de nouvelles molécules bioactives duales : vers des composés antagonistes AT1 et agonistes PPAR[gamma]. Autre. Université de Lorraine, 2013. Français. ⟨NNT : 2013LORR0221⟩. ⟨tel-01750517⟩

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