68095-16-9Relevant academic research and scientific papers
N-heterocyclic carbene-catalyzed enantioselective annulation of indolin-3-ones with bromoenals
Ni, Qijian,Song, Xiaoxiao,Raabe, Gerhard,Enders, Dieter
, p. 1535 - 1538 (2014/06/09)
N-Heterocyclic carbene-catalyzed reactions of indolin-3-ones with 2-bromoenals opened an asymmetric access to 3,4-dihydropyrano[3,2-b]indol-2(5 H)-ones in good yields and with good to excellent enantioselectivities. This protocol tolerates a broad substrate scope. In addition, a possible mechanism for the annulation reaction is presented. More NHC-organocatalysis: N-Heterocyclic carbene-catalyzed reactions of indolin-3-ones with 2-bromoenals opened an asymmetric access to 3,4-dihydropyrano[3,2-b]indol-2(5 H)-ones in good yields and with good to excellent enantioselectivities. This protocol tolerates a broad substrate scope. In addition, a possible mechanism for the annulation reaction is presented.
Indole-3-piperazinyl derivatives: Novel chemical class of 5-HT6 receptor antagonists
Nirogi, Ramakrishna V.S.,Deshpande, Amol D.,Kambhampati, Ramasastri,Badange, Rajesh Kumar,Kota, Laxman,Daulatabad, Anand V.,Shinde, Anil K.,Ahmad, Ishtiyaque,Kandikere, Vishwottam,Jayarajan, Pradeep,Dubey
scheme or table, p. 346 - 349 (2011/02/28)
N1-Arylsulfonyl-3-piperazinyl indole derivatives were designed and identified as a novel class of 5-HT6 receptors ligands. All the compounds have high affinity and antagonist activity towards 5-HT6 receptor. The compound 7a (Ki = 3.4 nM, functional assay IC 50 = 310 nM) shows enhanced cognitive effect when tested in NORT and Morris water maze models. Synthesis, SAR and PK profile of these novel compounds constitute the subject matter of this Letter.
Design, synthesis and pharmacological evaluation of conformationally restricted N-arylsulfonyl-3-aminoalkoxy indoles as a potential 5-HT6 receptor ligands
Nirogia, Ramakrishna V.S.,Kambhampati, Ramasastri,Daulatabad, Anand V.,Gudla, Parandhama,Shaikh, Mohammad,Achanta, Pramod Kumar,Shinde, Anil K.,Dubey, Pramod Kumar
scheme or table, p. 341 - 349 (2012/01/06)
A series of novel conformationally restricted N1-arylsulfonyl-3-aminoalkoxy indoles were designed and synthesized as 5-HT6 receptor (5-HT6R) ligands. Many of the synthesized compounds have moderate in vitro-binding affinities at 5-HT6R. The lead compound 8b (% inhibition=97.2 at 1 μM) from this series has good pharmacokinetic profile in male Wister rats and is active in animal model of cognition like Morris water maze. The details of chemistry, SAR, pharmacokinetics and pharmacological data constitute the subject matter of this report.
BENZYL-SUBSTITUTED TETRACYCLIC HETEROCYCLIC COMPOUNDS AS PDE5 INHIBITORS
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Page/Page column 107-108, (2010/04/03)
The present invention pertains to Benzyl-substituted tetracyclic heterocyclic compounds, as well as the resulting pharmaceutical compositions, and their use in the treatment or prophylaxis of diseases alleviated by inhibition of type 5 phosphodiesterases. Furthermore, the present invention pertains to the methods of manufacturing these Benzyl-substituted tetracyclic heterocyclic compounds.
