Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists

Silvia Fonquerna; Montse Miralpeix; Lluís Pagès; Carles Puig; Arantxa Cardús; Francisca Antón; Dolors Vilella; Mónica Aparici; José Prieto; Graham Warrellow; Jorge Beleta; Hamish Ryder

doi:10.1016/j.bmcl.2004.12.008

Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists

Bioorg Med Chem Lett. 2005 Feb 15;15(4):1165-7. doi: 10.1016/j.bmcl.2004.12.008.

Authors

Silvia Fonquerna¹, Montse Miralpeix, Lluís Pagès, Carles Puig, Arantxa Cardús, Francisca Antón, Dolors Vilella, Mónica Aparici, José Prieto, Graham Warrellow, Jorge Beleta, Hamish Ryder

Affiliation

¹ Almirall Prodesfarma, Research Center, Cardener 68-74, 08024 Barcelona, Spain. sfonquerna@almirall.es

PMID: 15686934
DOI: 10.1016/j.bmcl.2004.12.008

Abstract

The synthesis and structure-activity relationships of piperidinylpyrrolopyridines as potent and selective H(1) antagonists are discussed. It was found that the nature of the acid chain bonded to piperidine was a key feature for maintaining both the duration of action in vivo and lack of sedative properties.

MeSH terms

Administration, Oral
Animals
Blood-Brain Barrier
Capillary Permeability
Guinea Pigs
Histamine H1 Antagonists / chemical synthesis*
Histamine H1 Antagonists / pharmacokinetics
Histamine H1 Antagonists / pharmacology
Humans
Inhibitory Concentration 50
Pyridines / chemical synthesis*
Pyridines / pharmacokinetics
Pyridines / pharmacology
Rats
Solubility
Structure-Activity Relationship

Substances

Histamine H1 Antagonists
Pyridines