6,7-Dihydro-5H-pyrrolo[1,2-a] imidazoles as potent and selective α1A adrenoceptor partial agonists

Bioorganic and Medicinal Chemistry Letters

Volumn 19, Issue 11, 2009, Pages 3113-3117

  Roberts, Lee R ^a   Fish, Paul V ^a   Ian Storer, R ^a   Whitlock, Gavin A ^a  

^a PFIZER GLOBAL RESEARCH AND DEVELOPMENT   (United Kingdom)

Author keywords

Alpha1a adrenoceptor; CNS penetration; Partial agonist; Pyrroloimidazole; Selectivity

Indexed keywords

6,7 DIHYDRO 5H PYRROLO[1,2 A]IMIDAZOLE; ADRENERGIC RECEPTOR STIMULATING AGENT; ALPHA 1A ADRENERGIC RECEPTOR; ALPHA 1B ADRENERGIC RECEPTOR; ALPHA 1D ADRENERGIC RECEPTOR; ALPHA 2A ADRENERGIC RECEPTOR; GLYCOPROTEIN P; IMIDAZOLE DERIVATIVE; PARTIAL AGONIST; PYRIMIDINE; UNCLASSIFIED DRUG;

ARTICLE; DRUG SELECTIVITY; MEMBRANE PERMEABILITY; PROTEIN TRANSPORT;

ANIMALS; CELL LINE; DOGS; HUMANS; IMIDAZOLES; MICROSOMES, LIVER; P-GLYCOPROTEIN; PYRIMIDINES; RECEPTORS, ADRENERGIC, ALPHA-1; RECEPTORS, ADRENERGIC, ALPHA-2;

EID: 65149100537     PISSN: 0960894X     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmcl.2009.03.166     Document Type: Article

References (10)

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5. Conlon, K.; Christy, C.; Whitlock, G. A.; Roberts, L. R.; Stobie, A.; Thurlow, R. J.; McMurray, G. JPET, submitted for publication.
6. -1) for apical to basolateral (AB) and basolateral to apical (BA) directions. See reference:. Mahar Doan K.M., Humphreys J.E., Webster L.O., Wring S.A., Shampine L.J., Serabjit-Singh C.J., Adkison K.K., and Polli J.W. J. Pharm. Exp. Ther. 303 (2002) 1029
7. Caution should be exercised in the handling of nitro compounds. DSC analysis was determined on all alkyl nitro analogues.
8. + 263 (100%).
9. max calculated as a per relative to 10 μM phenylephrine response.
10. CCDC 724363 contains the supplementary crystallographic data for compound 6: This data can be obtained free of charge from The Cambridge Crystallographic Data Centre via www.ccdc.cam.ac.uk/data_request/cif.