183371-93-9Relevant academic research and scientific papers
(Hetero)aryl-bicyclic heteroaryl derivatives, their preparation and their use as protease inhibitors
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Page/Page column 26, (2010/02/11)
The present invention provides novel compounds of the Formula (I): A-B, its prodrug forms, or pharmaceutically acceptable salts thereof, wherein A represents a saturated, unsaturated, or a partially unsaturated bicyclic heterocyclic ring structure, and B represents an aryl or a heteroaryl group. Preferred compounds of the present invention comprise a benzimidazole or indole nucleus. The compounds of this invention are inhibitors of serine proteases, Urokinase (uPA), Factor Xa (FXa), and/or Factor VIIa (FVIIa), and have utility as anti cancer agents and/or as anticoagulants for the treatment or prevention of thromboembolic disorders in mammals.
Labeling of (S)-des-4-amino-3-[125I]iodozacopride (DAIZAC), a high-affinity radioligand for the 5-HT-3 receptor
Mason,Hewlett,Ebert,Schmidt,De Paulis
, p. 955 - 961 (2007/10/03)
We have prepared (S)-5-chloro-3-[125I]iodo-2-methoxy-N-(1-azabicyclo[2.2.2]oct-3-yl) -benzamide ([125I]DAIZAC, [125I]-3) as a radioligand for characterization of the 5-HT-3 receptor. Preparation of the 3-tri-n-butylstannyl precursor was accomplished from the corresponding unlabeled DAIZAC by reaction with bis(tributyltin). Treatment of the precursor with 5 mCi of Na125I and chloramine-T in dilute HCl gave 2.58 ± 0.22 mCi (52%) of [125I]DAIZAC with >98% radiochemical purity and 1500 Ci/mmol specific activity. Saturation analysis of the binding of [125I]DAIZAC to rat brain homogenates showed a single binding site with a receptor density B(max) of 0.66 ± 0.03 pmol/g and a receptor affinity K(D) of 0.15 ± 0.01 nM. Compared to [125I]iodozacopride, we find the 20-fold higher affinity and easy preparation of [125I]DAIZAC to be advantageous for in vitro identification of brain 5-HT-3 receptors.
