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Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A₁ and A_2A Receptors, and Efficacy in Animal Models of Depression.

ABSTRACT: New compounds with a 7-amino-2-arylmethyl-thiazolo[5,4-d]pyrimidine structure were synthesized and evaluated in vitro for their affinity and/or potency at the human (h) A₁, hA_2A, hA_2B, and hA₃ adenosine receptors (ARs). Several compounds (5, 8-10, 13, 18, 19) were characterized by nanomolar and subnanomolar binding affinities for the hA₁ and the hA_2A AR, respectively. Results of molecular docking studies supported the in vitro results. The 2-(2-fluorobenzyl)-5-(furan-2yl)-thiazolo[5,4-d]pyrimidin-7-amine derivative 18 (hA₁ K_i = 1.9 nM; hA_2A K_i = 0.06 nM) was evaluated for its antidepressant-like activity in in vivo studies, the force

SUBMITTER: Varano F

PROVIDER: S-EPMC8308585 | biostudies-literature | 2021 Jul

REPOSITORIES: biostudies-literature

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Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A₁ and A_2A Receptors, and Efficacy in Animal Models of Depression.

OmicsDI is part of the ELIXIR infrastructure

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Dataset Information

Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A1 and A2A Receptors, and Efficacy in Animal Models of Depression.

OmicsDI is part of the ELIXIR infrastructure

Tweets

Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A₁ and A_2A Receptors, and Efficacy in Animal Models of Depression.