Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists.
A gamma-carboline series of cysLT(1) receptor antagonists has been prepared. Some of the compounds show good potencies both, in vitro and in vivo, compared to the standard compounds.
Bonjoch
Josep
J
Laboratori de Química Orgànica, Facultat de Farmàcia, Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII s/n, 08028-Barcelona, Spain.
Diaba
Faïza
F
Pagès
Lluís
L
Pérez
Daniel
D
Soca
Lidia
L
Miralpeix
Montserrat
M
Vilella
Dolors
D
Anton
Paquita
P
Puig
Carles
C
D000284:Administration, Oral; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000138:chemical synthesis / Q000494:pharmacology; D002243:Carbolines / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D015195:Drug Design; D006168:Guinea Pigs; D006801:Humans; D020128:Inhibitory Concentration 50; D020024:Leukotriene Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D008956:Models, Chemical; D018077:Receptors, Leukotriene / Q000737:chemistry*; D013329:Structure-Activity Relationship; D013997:Time Factors
D000893:Anti-Inflammatory Agents; D002243:Carbolines; D020024:Leukotriene Antagonists; D018077:Receptors, Leukotriene; C055572:gamma-carboline; C083169:leukotriene D4 receptor