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Discovery of a series of potent arylthiadiazole H(3) antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2011 Jan 15; Vol. 21 (2), pp. 861-4. Date of Electronic Publication: 2010 Nov 21. - Publication Year :
- 2011
-
Abstract
- A series of 2-piperidinopiperidine-5-arylthiadiazoles was synthesized and subjected to a structure-activity relationship (SAR) investigation. The potency of this series was improved to the single digit nanomolar range. The key analogs were shown to be free of P450 issues, and they also maintained good ex vivo activity and brain penetration.<br /> (Copyright © 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Brain metabolism
Histamine Antagonists pharmacokinetics
Humans
Mice
Rats
Structure-Activity Relationship
Thiadiazoles pharmacokinetics
Histamine Antagonists chemistry
Histamine Antagonists pharmacology
Receptors, Histamine H3 metabolism
Thiadiazoles chemistry
Thiadiazoles pharmacology
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 21
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 21186123
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.11.065