Adenosines bearing 5'-modification in conjunction with an N6-substituent have previously been shown to act as partial agonists at the A1 adenosine receptor. Our current work investigates the effect of modifying the 5'-position in conjunction with efficacious bicyclic and tricyclic N6-substituents. Several highly potent agonists for the A1 adenosine receptor were identified; however, all of these compounds behaved as full agonists. In keeping with previous reports, 5'-halogen and 5'-sulfide derivatives of N6-(endo-norborn-2-yl)adenosine were, in general, low nanomolar agonists of the A1 adenosine receptor. The known partial agonist, N6-cyclopentyl-5'-deoxy-5'-ethylthioadenosine (2), also behaved as a full agonist in our assay.

2005-09-01·Nucleic Acids Symposium Series

Development of potent and selective human A3 adenosine receptor agonists

Article

作者: Lee, Sang Kook ; Chun, Moon Woo ; Jacobson, Kenneth A. ; Lee, Hyuk Woo ; Jeong, Lak Shin

On the basis of bioisosteric rationale, structure-activity relationship of Cl-IB-MECA, which showed high binding affinity at the human A3 adenosine receptor, was studied. From this study, 2-chloro-4'-thioadenosine-5'-methyluronamide was discovered as the most potent and selective agonist at the human A3 adenosine receptor.

2003-01-01·Antibiotiki i khimioterapiia = Antibiotics and chemoterapy [sic]

[Efficacy of 4'-thio-5-ethyl-2'-deoxyuridine (TEDU) and its derivatives in experimental infection in mice caused by herpes simplex virus].

Article

作者: Andronova, V L ; Karpenko, I L ; Skoblov, Iu S ; Aleksandrova, L A

It was demonstrated that several 5'-phosphonates of 4'-thio-5-ethyl-2'-deoxyuridine possessed antiviral activity in vitro and in the murine model of herpes simplex virus type 1 infection. It was shown that the derivatives after intraabdominal administration penetrated effectively into the brain tissue. The agents provided statistically significant increase of the average life span, lower virus titre in the brain and lower lethality when compared to the control group of the animals. It is emphasized that the derivatives were less toxic than the original compound.

100 项与 4-S-EtdU 相关的药物交易

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