Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists

Josep Bonjoch; Faïza Diaba; Lluís Pagès; Daniel Pérez; Lidia Soca; Montserrat Miralpeix; Dolors Vilella; Paquita Anton; Carles Puig

doi:10.1016/j.bmcl.2009.05.094

Synthesis and structure-activity relationships of gamma-carboline derivatives as potent and selective cysLT(1) antagonists

Bioorg Med Chem Lett. 2009 Aug 1;19(15):4299-302. doi: 10.1016/j.bmcl.2009.05.094. Epub 2009 May 27.

Authors

Josep Bonjoch¹, Faïza Diaba, Lluís Pagès, Daniel Pérez, Lidia Soca, Montserrat Miralpeix, Dolors Vilella, Paquita Anton, Carles Puig

Affiliation

¹ Laboratori de Química Orgànica, Facultat de Farmàcia, Institut de Biomedicina (IBUB), Universitat de Barcelona, Av. Joan XXIII s/n, 08028-Barcelona, Spain.

PMID: 19505824
DOI: 10.1016/j.bmcl.2009.05.094

Abstract

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.

MeSH terms

Administration, Oral
Animals
Anti-Inflammatory Agents / chemical synthesis
Anti-Inflammatory Agents / pharmacology
Carbolines / chemistry*
Chemistry, Pharmaceutical / methods*
Drug Design
Guinea Pigs
Humans
Inhibitory Concentration 50
Leukotriene Antagonists / chemical synthesis*
Leukotriene Antagonists / pharmacology
Models, Chemical
Receptors, Leukotriene / chemistry*
Structure-Activity Relationship
Time Factors

Substances

Anti-Inflammatory Agents
Carbolines
Leukotriene Antagonists
Receptors, Leukotriene
gamma-carboline
leukotriene D4 receptor