eng URI http://hdl.handle.net/10795/3343 φυσικές επιστήμες χημεία ιατρικές επιστήμες ασθένεια του νευρικού συστήματος προσομοίωση φαρμακευτική In the present work, a facile and efficient route for the synthesis of a series of N-substituted imidazole derivatives is described. Docking studies have revealed that N-substituted imidazole derivatives based on (E)-urocanic acid may be potential antihypertensive leads. Therefore, new AT1 receptor blockers bearing either the benzyl or the biphenylmethyl moiety at the N-1 or N-3 position, either the (E)-acrylate or the propanoate fragment and their related acids at the C-4 position as well as a halogen atom at the C-5 position of the imidazole ring, were synthesized. The newly synthesized analogues were evaluated for binding to human AT1 receptor. The biological results showed that this class of molecules possesses moderate or no activity, thus not always confirming high docking scores. Nonetheless, important conclusions can be derived for their molecular basis of their mode of action and help medicinal chemists to design and synthesize more potent ones. An aliphatic group as in losartan seems to be important for enhancing binding affinity and activity. 23 pp. LOMv1.0 creator LOMv1.0 publisher LOMv1.0 Scientific Coordinator LOMv1.0 Project Executing Organisation 2013-06-27 Digital Library of the Operational Programme "Education and Lifelong Learning" abstract types Text synthesis AT1 receptor blockers (E)-urocanic acid N-alkylation docking studies 2137570 application/pdf http://repository.edulll.gr/edulll/bitstream/10795/3343/2/3343_1.153_%ce%94%ce%97%ce%9c_18_6_14.pdf URI http://hdl.handle.net/10795/3343 LOMv1.0creator 2016-05-23T11:37:19Z LOMv1.0validator 2016-05-23T11:37:19Z LOMv1.0 gre no no Copyright EYD-EPEDBM (Operational Programme "Education and Lifelong Learning")