Zobrazeno 1 - 10
of 54
pro vyhledávání: '"Ronald C. Bernotas"'
Autor:
Ping Chen, Rajesh A. Shenoy, Albert J. Robichaud, Deborah F. Smith, Schuyler Adam Antane, Boyd L. Harrison, Van-Duc Le, Ronald C. Bernotas, Guo Ming Zhang, Lee E. Schechter
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:1657-1660
Novel 3-(arylsulfonyl)-1-(azacyclyl)-1H-indoles 6 were synthesized as potential 5-HT(6) receptor ligands, based on constraining a basic side chain as either a piperidine or a pyrrolidine. Many of these compounds had good 5-HT(6) binding affinity with
Autor:
Rebecca J. Dooley, Ronald C. Bernotas
Publikováno v:
Tetrahedron. 66:2273-2276
Expeditious routes to 1,2,3,4,4a,5-hexahydro-pyrazino[2,1-c][1,4]benzothiazine-6,6-dioxide, a methylenesulfone-constrained arylpiperazine, have been developed. The key step forms the tricyclic system in a cascade of reactions via a 1,4-addition, nitr
Autor:
Christine Huselton, David H. Kaufman, Annika Goos-Nilsson, Jay E. Wrobel, Irene Feingold, Ponnal Nambi, Ronald C. Bernotas, Elaine Quinet, Anna Wilhelmsson, Jeremy M. Travins
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 20:526-530
A series of 1-(3-aryloxyaryl)benzimidazoles incorporating a sulfone substituent (6) was prepared. High affinity LXR ligands were identified (LXRbeta binding IC(50) values
Autor:
Anna Wilhelmsson, Ronald C. Bernotas, David H. Kaufman, Rayomand J. Unwalla, Elaine Quinet, John W. Ullrich, Annika Goos-Nilsson, Ponnal Nambi, Robert R. Singhaus, Jay E. Wrobel
Publikováno v:
Bioorganic & Medicinal Chemistry. 17:8086-8092
A series of 4-(3-aryloxyaryl)quinolines with alcohol substituents on the terminal aryl ring was prepared as potential LXR agonists, in which an alcohol group replaced an amide in previously reported amide analogs. High affinity LXR ligands with excel
Autor:
Ronald C. Bernotas, Guo Ming Zhang, Lee E. Schechter, Schuyler Adam Antane, Steven Edward Lenicek, Deborah L. Smith, Boyd L. Harrison, Simon Haydar, Joseph Coupet, Albert J. Robichaud
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 19:6935-6938
1-(2-Aminoethyl)-3-(arylsulfonyl)-1H-pyrrolopyridines were prepared. Binding assays indicated they are 5-HT6 receptor ligands, among which 6f and 6g showed high affinity for 5-HT6 receptors with Ki = 3.9 and 1.7 nM, respectively.
Autor:
Ronald C. Bernotas, David Zenan Li, Hassan Mahmoud Elokdah, Lee E. Schechter, Geraldine Ruth Mcfarlane, Guo Ming Zhang, Deborah L. Smith, Albert J. Robichaud, Ronald L. Magolda
Publikováno v:
Bioorganic & Medicinal Chemistry. 15:6208-6226
1-Aminoethyl-3-arylsulfonyl-1H-indoles 1 are 5-HT(6) receptor ligands with modest activity in a 5-HT(6) cyclase assay. Introduction of an additional nitrogen in the indole ring provides 1-aminoethyl-3-arylsulfonyl-1H-pyrrolo[2,3-b]pyridines 2 with bo
Publikováno v:
Annals of the New York Academy of Sciences. 738:243-249
Many laboratory and clinical studies suggest that oxygen radical formation and resultant cell damage contribute to CNS injury following stroke and neurotrauma. Accordingly, antioxidants represent a viable therapeutic approach for management of CNS ox
Autor:
Deborah L. Smith, Albert J. Robichaud, Guo Ming Zhang, Boyd L. Harrison, Lee E. Schechter, Ronald C. Bernotas, Ping Zhou, Yinfa Yan, Donna M. Huryn
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:1393-1396
The preparation of a novel class of 4-(2-aminoethoxy)-N-(phenylsulfonyl)indoles which exhibit high affinity towards the 5-HT6 receptor is reported here. Among these compounds, 4-(2-methylaminoethoxy)-N-(phenylsulfonyl)indole 5g showed superior affini
Publikováno v:
Synthesis. 2005:465-469
The diastereoselectivity of the [2 +3]-cycloaddition of 1-benzyl-2-piperazinone nitrone with several alkenes has been examined. exo-Type cycloadducts predominated for most substrates.
Autor:
William Joseph Lennox, Hossein Mazandarani, John W. Ellingboe, Deborah L. Smith, Gregory J. Tawa, Joseph Coupet, Ronald C. Bernotas, Derek C. Cole, Guoming Zhang, Lee E. Schechter, Sabrina Lombardi
Publikováno v:
Journal of Medicinal Chemistry. 48:353-356
5-Arylsulfonylamido-3-(pyrrolidin-2-ylmethyl)-1H-indoles have been identified as high-affinity 5-HT(6) receptor ligands. Within this class, several of the (R)-enantiomers were potent agonists having EC(50) values of 1 nM or less and functioning as fu