- Synthesis and in vitro activity of N-benzyl-1-(2,3-dichlorophenyl)-1H- tetrazol-5-amine P2X7 antagonists
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Synthesis and biological evaluation of a novel class of substituted N-benzyl-1-(2,3-dichlorophenyl)-1H-tetrazol-5-amine derivatives resulted in the identification of potent P2X7 antagonists. These compounds were assayed for activity at both the
- Perez-Medrano, Arturo,Donnelly-Roberts, Diana L.,Florjancic, Alan S.,Nelson, Derek W.,Li, Tongmei,Namovic, Marian T.,Peddi, Sridhar,Faltynek, Connie R.,Jarvis, Michael F.,Carroll, William A.
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p. 3297 - 3300
(2011/07/07)
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- Method of inhibiting neoplastic cells with imidazoquinazoline derivatives
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A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to imidazoquinazoline derivatives.
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- Aminoborohydrides. 12. Novel tandem SNAr amination-reduction reactions of 2-halobenzonitriles with lithium N,N-dialkylaminoborohydrides
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A novel tandem amination-reduction reaction has been developed in which 2-(N,N-dialkylamino)benzylamines are generated from 2-halobenzonitriles and lithium N,N-dialkylaminoborohydride (LAB) reagents. These reactions are believed to occur through a tandem SNAr amination-reduction mechanism wherein the LAB reagent promotes halide displacement by the N,N-dialkylamino group, and the nitrile is subsequently reduced. This one-pot procedure is complimentary to existing synthetic methods and is an attractive synthetic tool for the nucleophilic aromatic substitution of halobenzenes with less nucleophilic amines. The (N,N-dialkylamino)benzylamine products of this reaction are easily isolated after a simple aqueous workup procedure in very good to excellent yields.
- Thomas,Collins,Cuzens,Spiciarich,Goralski,Singaram
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p. 1999 - 2004
(2007/10/03)
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- Imidazoquinazoline derivatives
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PCT No. PCT/JP97/03023 Sec. 371 Date Apr. 27, 1998 Sec. 102(e) Date Apr. 27, 1998 PCT Filed Aug. 29, 1997 PCT Pub. No. WO98/08848 PCT Pub. Date Mar. 5, 1998Imidazoquinoline derivatives of the formula (wherein X may be O or S) provide selective cyclic guanosine 3',5' monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity. The compounds are useful for treating or ameliorating cardiovascular disease such as thrombosis, angina pectoris, hypertension, heart failure and arterial sclerosis, as well as asthma, impotence and the like.
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