Synthesis and structure-activity relationships of piperidinylpyrrolopyridine derivatives as potent and selective H1 antagonists.
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.
Fonquerna
Silvia
S
Almirall Prodesfarma, Research Center, Cardener 68-74, 08024 Barcelona, Spain. sfonquerna@almirall.es
Miralpeix
Montse
M
Pagès
Lluís
L
Puig
Carles
C
Cardús
Arantxa
A
Antón
Francisca
F
Vilella
Dolors
D
Aparici
Mónica
M
Prieto
José
J
Warrellow
Graham
G
Beleta
Jorge
J
Ryder
Hamish
H
D000284:Administration, Oral; D000818:Animals; D001812:Blood-Brain Barrier; D002199:Capillary Permeability; D006168:Guinea Pigs; D006634:Histamine H1 Antagonists / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D011725:Pyridines / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology; D051381:Rats; D012995:Solubility; D013329:Structure-Activity Relationship
D006634:Histamine H1 Antagonists; D011725:Pyridines