sch-442416 and pyrimidine

sch-442416 has been researched along with pyrimidine* in 2 studies

Other Studies

2 other study(ies) available for sch-442416 and pyrimidine

Article	Year
Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists. Bioorganic & medicinal chemistry letters, 2010, Oct-01, Volume: 20, Issue:19 Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A(2A) AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A(2A) AR ligands, based on the known antagonist, SCH 442416 (R=-Me), which have structural variability on the terminus (R=-Et, -i-Pr, -allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a K(i) value of 12.4 nM and was highly selective for the A(2A) AR in comparison to the A(1) and A(3) ARs. Topics: Adenosine A2 Receptor Antagonists; Binding Sites; Cell Line; Computer Simulation; Contrast Media; Fluorine Radioisotopes; Humans; Positron-Emission Tomography; Protein Structure, Tertiary; Pyrazoles; Pyrimidines; Receptor, Adenosine A2A; Triazoles	2010
Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands. Bioorganic & medicinal chemistry, 2010, Nov-15, Volume: 18, Issue:22 A series of pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones was synthesized and tested in radioligand binding assays to determine their affinities for the human adenosine A(1), A(2A), A(2B) and A(3) receptors. Results indicated that this scaffold is appropriate for adenosine receptor subtype A(1) ligands and that the best arranged groups around this scaffold are 3- and 4-pyridinyl at position 1, benzyl at position 3, hydrogen at position 6 and 3-thienyl or phenyl at position 9. The most interesting compounds showed K(i) for A1 in the nanomolar range and an appreciable selectivity for other receptor subtypes. Topics: Adenosine A1 Receptor Antagonists; Cell Line; Humans; Ligands; Protein Binding; Pyrazoles; Pyridazines; Pyrimidines; Receptor, Adenosine A1; Receptor, Adenosine A2A; Receptor, Adenosine A2B; Receptor, Adenosine A3	2010

Article

Year

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.

Bioorganic & medicinal chemistry letters, 2010, Oct-01, Volume: 20, Issue:19

Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A(2A) AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A(2A) AR ligands, based on the known antagonist, SCH 442416 (R=-Me), which have structural variability on the terminus (R=-Et, -i-Pr, -allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a K(i) value of 12.4 nM and was highly selective for the A(2A) AR in comparison to the A(1) and A(3) ARs.

Topics: Adenosine A2 Receptor Antagonists; Binding Sites; Cell Line; Computer Simulation; Contrast Media; Fluorine Radioisotopes; Humans; Positron-Emission Tomography; Protein Structure, Tertiary; Pyrazoles; Pyrimidines; Receptor, Adenosine A2A; Triazoles

2010

Pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones as selective human A(1) adenosine receptor ligands.

Bioorganic & medicinal chemistry, 2010, Nov-15, Volume: 18, Issue:22

A series of pyrazolo[1',5':1,6]pyrimido[4,5-d]pyridazin-4(3H)-ones was synthesized and tested in radioligand binding assays to determine their affinities for the human adenosine A(1), A(2A), A(2B) and A(3) receptors. Results indicated that this scaffold is appropriate for adenosine receptor subtype A(1) ligands and that the best arranged groups around this scaffold are 3- and 4-pyridinyl at position 1, benzyl at position 3, hydrogen at position 6 and 3-thienyl or phenyl at position 9. The most interesting compounds showed K(i) for A1 in the nanomolar range and an appreciable selectivity for other receptor subtypes.

Topics: Adenosine A1 Receptor Antagonists; Cell Line; Humans; Ligands; Protein Binding; Pyrazoles; Pyridazines; Pyrimidines; Receptor, Adenosine A1; Receptor, Adenosine A2A; Receptor, Adenosine A2B; Receptor, Adenosine A3

2010