Synthesis and biological effects of a new series of 2-amino-3-benzoylthiophenes as allosteric enhancers of A1-adenosine receptor was written by Baraldi, P. G.;Zaid, A. Z.;Lampronti, I.;Fruttarolo, F. F.;Pavani, M. G.;Tabrizi, M. A.;Shryock, J. C. S.;Leung, E.;Romagnoli, R.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2000.Product Details of 33439-27-9 This article mentions the following:
New derivatives of PD 81,723, an allosteric enhancer of agonist binding to the A1-adenosine receptor, have been synthesized and evaluated in an intact cell assay. Compounds I (R1-R3 = H; R1 = 4-Cl, 4-Br, R2R3 = (CH2)4) appeared to be more potent than PD 81,723 and at a concentration of 0.1 μM caused significant reductions of cAMP content of CHO cells expressing the human A1-adenosine receptor. Compounds II (R1 = 4-Cl, R4 = PhCH2CH2, CH2CO2Et) appeared to be allosteric enhancers at a low concentration and antagonists at a higher concentration, whereas compounds I (R1 = H, R2 = R3 = Me; R2R3 = CH2CH2S; (CH2)5) and II (R1 = H, R4 = 4-O2NC6H4CH2CH2) appeared to be weak antagonists that are also allosteric enhancers at the higher concentration of 10 μM. In the experiment, the researchers used many compounds, for example, 1-Tosylpiperidin-4-one (cas: 33439-27-9Product Details of 33439-27-9).
1-Tosylpiperidin-4-one (cas: 33439-27-9) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.Product Details of 33439-27-9
Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem