74396-53-5Relevant academic research and scientific papers
Substituted conformationally restricted guanidine derivatives: Probing the α2-adrenoceptors’ binding pocket
McMullan, Michela,García-Bea, Aintzane,Miranda-Azpiazu, Patricia,Callado, Luis F.,Rozas, Isabel
supporting information, p. 48 - 57 (2016/08/01)
In this paper we report the design, synthesis and pharmacological evaluation of new N-substituted 2-amino-1,4-dihydroquinazolines, 2-amino-1,4-dihydropyridopyrimidines and 2-amino-4,5-dihydro-1,3-benzodiazepines as α2-adrenoceptors ligands. Computational studies show that the proposed substitutions and guanidine-containing ring size will probe an extensive area of the active site. Preparation of these molecules involved novel routes than those previously utilised in our laboratory for the preparation of the acyclic aryl-guanidine counterparts. Compounds 8b and 18c showed the highest affinity and antagonistic activity, within their series, towards the α2-adrenoceptor in human brain tissue in?vitro experiments. Structure-activity relationships have been established for the design and biological evaluation of novel α2-adrenoceptor ligands.
Rhodium(III)-Catalyzed Direct Cyanation of Aromatic C-H Bond to Form 2-(Alkylamino)benzonitriles Using N-Nitroso As Directing Group
Dong, Jiawei,Wu, Zhongjie,Liu, Zhengyi,Liu, Ping,Sun, Peipei
, p. 12588 - 12593 (2016/01/09)
2-(Alkylamino)benzonitriles were synthesized via a rhodium-catalyzed cyanation on the aryl C-H bond and subsequent denitrosation of N-nitrosoarylamines using a removable nitroso as the directing group, in which N-cyano-N-phenyl-p-methylbenzenesulfonamide (NCTS) was used as the "CN" source. Various substituents on the aryl ring and amino group of N-nitrosoarylamines tolerated the reaction, and the corresponding products were achieved in moderate to good yields.
4-Hydroxyquinol-2-ones. 86. Synthesis of methyl (ethyl) esters of 1-substituted 4-amino-2-oxoquinoline-3-carboxylic acids
Ukrainets,Sidorenko,Gorokhova
, p. 1151 - 1157 (2007/10/03)
Several variants of the synthesis of esters of 1-N-substituted 4-amino-2-oxoquinoline-3-carboxylic acids have been studied, one of which is recommended as preparative. 2005 Springer Science+Business Media, Inc.
Method of inhibiting neoplastic cells with imidazoquinazoline derivatives
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, (2008/06/13)
A method for inhibiting neoplasia, particularly cancerous and precancerous lesions by exposing the affected cells to imidazoquinazoline derivatives.
Imidazoquinazoline derivatives
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, (2008/06/13)
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.
Synthesis of 2-(alkylamino)benzonitriles from α-(bromoarylamino)nitriles
Cossy,Poitevin,Pardo,Peglion
, p. 1368 - 1370 (2007/10/02)
The treatment of α-(bromoarylamino)nitriles with Bu3SnH/AIBN induced 1,4-cyano group migration which led to 2-(alkylamino)benzonitriles.
