49786-89-2Relevant academic research and scientific papers
Design and synthesis of fused soluble epoxide hydrolase/peroxisome proliferator-activated receptor modulators
Bl?cher,Lamers,Wittmann,Diehl,Hanke,Merk,Steinhilber,Schubert-Zsilavecz,Kahnt,Proschak
, p. 1209 - 1216 (2016/07/06)
Metabolic syndrome (MetS) is a widespread, complex disease cluster which consists of hypertension, atherosclerosis, dyslipidaemia and type II diabetes. The treatment of MetS requires multiple pharmaceutical agents leading to complex polypharmacy. Multi-ta
Structure-activity studies on a 1,2,3-triazole derivative, a potent in vitro inhibitor of prostaglandin synthesis: The role of the heterocyclic ring
Biagi,Dell'Omodarme,Ferretti,Giorgi,Livi,Scartoni
, p. 335 - 344 (2007/10/02)
This paper reports further structural modifications concerning the 1,2,3- triazole ring of the compound A, an effective in vitro inhibitor of prostaglandin synthesis. The introduction of different heterocyclic rings provided further information about of t
Synthesis of isosteres of p-amidinophenylpyruvic acid. Inhibitors of trypsin thrombin, and pancreatic kallikrein.
Loeffler et al.
, p. 287,288 (2007/10/06)
A series of amino acids, amidino acids, and amidino esters was synthesized and the compounds were evaluated for their inhibitory activity against bovine trypsin, bovine thrombin, and porcine pancreatic kallikrein and as anticoagulants. Among these compounds, ethyl 4-amidino-2-iodophenoxyacetate was found to be the most effective inhibitor of the enzymes in question, with a potency (Ki = 3.16 x 10-6 M vs. trypsin; Ki = 4.8 x 10-5 M vs. thrombin) similar to that of p-amidinophenylpyruvic acid (Ki = 6.0 x 10-6 M vs. trypsin; Ki = 2.0 x 10-5 M vs. thrombin). Ethyl 4-amidino-2-iodophenoxyacetate was also found to be the most effective in blocking the clotting activity of plasma, as indicated by significant prolongation of the partial thromboplastin time. This paper reports the synthetic methods, the enzyme inhibitory activity, and the structure-activity relationships observed.
