title: Antileukotrienic N-arylethyl-2-arylacetamides in the treatment of ulcerative colitis.
abstract: A series of arylacetic acid derivatives bearing methyl(arylethyl)amino groups were prepared and their antileukotrienic activities involving LTB(4) were evaluated. Regression analysis has shown a strong dependence of these activities on lipophilicity for both LTB(4) receptor binding and inhibition of LTB(4) biosynthesis; parabolic relationships were derived. The values of slopes of the ascending linear parts of these dependences indicate various types of hydrophobic binding at the site of ligand interaction with relevant biomacromolecules. The anti-inflammatory effect of the compounds under study was also evaluated in three animal models of inflammation and their possible utilization in the treatment of ulcerative colitis (UC) was followed. The importance of antileukotrienic activities for the anti-inflammatory effect, especially in the model of UC was discussed, but further experiments are necessary to confirm the respective relations.
authors: Zentiva VUFB, a.s., 102 01 Prague 10, Czech Republic.
authors: Richard
authors: R
authors: Junek
authors: Bohumila
authors: B
authors: Brůnová
authors: Miloslav
authors: M
authors: Kverka
authors: Vladimíra
authors: V
authors: Panajotová
authors: Antonín
authors: A
authors: Jandera
authors: Miroslav
authors: M
authors: Kuchar
mesh_terms: D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D003093:Colitis, Ulcerative / Q000188:drug therapy*; D004195:Disease Models, Animal; D004487:Edema / Q000139:chemically induced / Q000188:drug therapy; D057927:Hydrophobic and Hydrophilic Interactions; D007975:Leukotriene B4 / Q000037:antagonists & inhibitors* / Q000096:biosynthesis; D009504:Neutrophils / Q000187:drug effects / Q000378:metabolism; D051381:Rats; D018102:Receptors, Leukotriene B4 / Q000037:antagonists & inhibitors / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D000081:Acetamides; D018102:Receptors, Leukotriene B4; D007975:Leukotriene B4