Synthesis of novel histamine H4 receptor antagonists

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1156-1159

  Lane, Charlotte A L ^a   Hay, Duncan ^a   Mowbray, Charles E ^a   Paradowski, Michael ^a   Selby, Matthew D ^a   Swain, Nigel A ^a   Williams, David H ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Amidine; Azaindole; Bicyclic; Histamine; Isostere

Indexed keywords

1 (5 CHLORO 2 BENZIMIDAZOLYLCARBONYL) 4 METHYLPIPERAZINE; 1 (5 CHLORO 2 INDOLYLCARBONYL) 4 METHYLPIPERAZINE; HISTAMINE H4 RECEPTOR ANTAGONIST;

ANIMAL EXPERIMENT; ARTICLE; DRUG BIOAVAILABILITY; DRUG DISTRIBUTION; DRUG STRUCTURE; DRUG SYNTHESIS; NONHUMAN; RAT;

ANIMALS; AZABICYCLO COMPOUNDS; CRYSTALLOGRAPHY, X-RAY; DOSE-RESPONSE RELATIONSHIP, DRUG; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRROLIDINES; RATS; RECEPTORS, G-PROTEIN-COUPLED; RECEPTORS, HISTAMINE; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84855666586     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.098     Document Type: Article

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27. CCDC 850451 contains the supplementary crystallographic data for this paper. These data can be obtained free of charge via www.ccdc.cam.ac.uk/data- request/cif, or by emailing data-request@ccdc.cam.ac.uk, or by contacting The Cambridge Crystallographic Data Centre, 12 Union Road, Cambridge CB2 1EZ, UK, fax: +44 1223 336033.
28. This work was first presented at the Gordon Research Conference on Medicinal Chemistry at Colby-Sawyer College, New London, NH, USA, August 12, 2010 in a presentation by Charles E. Mowbray titled: 'The Discovery and Evaluation of PF-3893787: A Novel Histamine H4 Receptor Antagonist'. The compounds described in this letter have been disclosed in Ref. 12a and the findings of in vivo toxicological investigations have been reported in detail by Mowbray, C. E.; Bell, A. S.; Clarke, N. P.; Collins, M; Jones, R. M.; Lane, C. A. L.; Liu, W. L.; Newman, S. D.; Paradowski, M.; Schenck, E. J.; Selby, M. D.; Swain, N. A.; Williams, D. H. Bioorg. Med. Chem. Lett. 2011, 21, 6596.