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4-Alkylpiperidines related to SR-48968: Potent antagonists of the neurokinin-2 (NK2) receptor
- Source :
- Bioorganic & Medicinal Chemistry Letters. 8:1935-1940
- Publication Year :
- 1998
- Publisher :
- Elsevier BV, 1998.
-
Abstract
- A series of 4-alkylpiperidine derivatives related to the potent neurokinin-2 (NK2) receptor antagonist SR-48968 (1) is described. Simple aliphatic derivatives were found to be poorly active, but appropriate placement of an alcohol functional group afforded compounds that were of similar activity to 1. Several representatives in this series, such as the 4-(1-hydroxy-1-ethylpropyl)piperidine (14), were found to exhibit oral activity in a model of labored abdominal breathing in guinea pigs. These results expand the latitude of substituents available in this region of this series of NK2 receptor antagonists.
- Subjects :
- medicine.drug_class
Stereochemistry
Guinea Pigs
Organic Chemistry
Clinical Biochemistry
Antagonist
Pharmaceutical Science
Carboxamide
Receptors, Neurokinin-2
Receptor antagonist
Biochemistry
Chemical synthesis
Guinea pig
chemistry.chemical_compound
Piperidines
chemistry
Oral administration
Benzamides
Drug Discovery
medicine
Animals
Molecular Medicine
Piperidine
Receptor
Molecular Biology
Subjects
Details
- ISSN :
- 0960894X
- Volume :
- 8
- Database :
- OpenAIRE
- Journal :
- Bioorganic & Medicinal Chemistry Letters
- Accession number :
- edsair.doi.dedup.....d2426db85fd98af51dfc7c4f118529f5