203186-20-3Relevant academic research and scientific papers
Synthesis and structure-Activity relationships of M2-Selective muscarinic receptor ligands in the 1-[4-(4-Arylsulfonyl)-phenylmethyl]-4-(4-piperidinyl)-piperazine family
McCombie, Stuart W.,Lin, Sue-Ing,Tagat, Jayaram R.,Nazareno, Dennis,Vice, Susan,Ford, Jennifer,Asberom, Theodros,Leone, Daria,Kozlowski, Joseph A.,Zhou, Guowei,Ruperto, Vilma B.,Duffy, Ruth A.,Lachowicz, Jean E.
, p. 795 - 798 (2007/10/03)
The synthesis and muscarinic binding properties of compounds based on the 1-[4-(4-arylsulfonyl)phenylmethyl]-4-(1-aroyl-4-piperidinyl)-piperazine skeleton are described. For compounds, substituted with appropriately configured methyl groups at the benzylic center and at the piperazine 2-position, high levels of selective, M2 subtype affinity could be obtained, particularly when the terminal N-aroyl residue was ortho-substituted.
Piperazine-based CCR5 antagonists as HIV-1 inhibitors. II. Discovery of 1-[(2,4-dimethyl-3-pyridinyl)carbonyl]-4methyl-4-[3(S)-methyl-4-[1(S)-[4- (trifluoromethyl) phenyl]ethyl]-1-piperazinyl]piperidine N1-oxide (Sch-350634), an orally bioavailable, poten
Tagat,Steensma,McCombie,Nazareno,Lin,Neustadt,Cox,Xu,Wojcik,Murray,Vantuno,Baroudy,Strizki
, p. 3343 - 3346 (2007/10/03)
Truncation of the original piperidino-2(S)-methyl piperazine lead structure 2, from a family of muscarinic antagonists, gave compound 8 which has improved selectivity for the HIV-1 co-receptor CCR5 over muscarinic receptors. Further optimization for pharm
