84727-35-5Relevant academic research and scientific papers
Design and synthesis of a series of glycerol-derived receptor mediated calcium entry (RMCE) blockers
Howson,Armstrong,Cassidy,Novelli,Tchorzewska,Jaxa-Chamiec,Dolle,Hallam,Leigh,Merritt,Moores,Rink
, p. 595 - 602 (2007/10/02)
Receptor mediated calcium entry (RMCE) is a now recognised mechanism by which the influx of Ca2+ into cells can occur. Agents which antagonise or block this mechanism are expected to possess anti-platelet aggregation and anti-inflammatory activities. The first series of RMCE blockers based upon the lead compound SC 38249, has been prepared. Their synthesis, activity against ADP evoked Ca2+ signals in human platelets and their anti-platelet aggregation activity is described. A trend between the c log P of these compounds and their activity as inhibitors of Ca2+ influx into human platelets stimulated by ADP was observed. This SAR study led to a 40-fold increase in activity over the initial lead compound.
Thromboxane synthase inhibitors. Synthesis and pharmacological activity of (R)-, (S)-, and (±)-2,2-dimethyl-6-[2-(1H-imidazol-1-yl)-1-[[(4 methoxyphenyl)-methoxy]methyl]ethoxy]hexanoic acids
Manley,Tuffin,Allanson,Buckle,Lad,Lai,Lunt,Porter,Wade
, p. 1812 - 1818 (2007/10/02)
A series of substituted ω-[2-(1H-imidazol-1-yl)ethoxy]alkanoic acid derivatives were synthesized and evaluated for their ability to inhibit thromboxane synthase both in vitro and in vivo. Compound 13 was identified as a potent and selective competitive in
Structure-Activity Relationships in an Imidazole-Based Series of Thromboxane Synthase Inhibitors
Manley, Paul W.,Allanson, Nigel M.,Booth, Robert F. G.,Buckle, Philip E.,Kuzniar, Edward J.,et al.
, p. 1588 - 1595 (2007/10/02)
Analogues of 4-methyl>ethoxy>methyl>benzoic acid (5m) were prepared and evaluated as thromboxane synthase inhibitors.A series of esters of 5m showed a parabolic relationship between lipophilicity and inh
Imidazole derivatives used in antithrombotic method
-
, (2008/06/13)
Compounds of the general formula: STR1 and acid addition salts thereof; in which Ar and Ar1 which may be the same or different, each represent an aromatic radical which may be substituted one or more times by substituents selected from the following: halogen; lower alkyl; lower alkoxy; alkylenedioxy; aralkoxy; aryloxy; trihalomethyl; carboxy; carboxyalkyl; cyano; carboxamido; di-lower alkylamino; nitro; and lower alkyl sulphonyl provided that one of the groups Ar and Ar1 carries at least one alkoxy, alkylenedioxy, carboxy or carboxyalkyl substituent; and Alk1 and Alk2, which may be the same or different, each represent an alkylene group containing from 1 to 8 carbon atoms which may be substituted one or more times by lower alkyl; X and Y which may be the same or different represent oxygen, nitrogen or sulphur; and in which the imidazole ring may be substituted by one or more lower alkyl substituents have antithrombotic activitiy. A representative compound is 1-[2-[(4-methoxyphenyl)methoxy]-3-[(4-methoxyphenyl)methoxy]propyl]-1H-imidazole.
Certain 1H-imidazol-1-yl-1-lower-alkanoic acid derivatives having anti-thrombotic activity
-
, (2008/06/13)
Compounds of the general formula STR1 and pharmaceutically acceptable salts thereof have antithrombotic activity. Het represents 1-[1H-imidazolyl], 1-N-morpholinyl or pyridyl. A representative compound is 6-[2-(1H-Imidazol-1-yl)-1-yl-1-[[(4-methoxyphenyl)methoxy]methyl]ethoxy]hexanoic acid.
