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Novel derivatives of 3-alkyl-1,5-diaryl-1 H -1,2,4-triazoles and their pharmacological evaluation as CB1 cannabinoid ligands

机译:3-烷基-1,5-二芳基-1 H -1,2,4-三唑的新型衍生物及其作为CB1大麻素配体的药理评价

摘要

Abstract In a previous study, we have identified 3- udalkyl-1,5-diaryl-1H-1,2,4-triazoles to be a novel class udof cannabinoid type-1 (CB1) receptor antagonists. udHowever, the synthesis yields for the ligands were udlow. Here we present an alternative synthesis pathway udwith improved yields. In addition, we have syn- udthezised new structural derivatives and studied their udresults in competitive radioligand binding assays for udcannabinoid receptors.
机译:摘要在先前的研究中,我们已经确定3- ud烷基-1,5-二芳基-1H-1,2,4-三唑是一种新型的 udof大麻素1型(CB1)受体拮抗剂。然而,配体的合成产率是低的。在这里,我们提出了具有提高的产率的替代合成途径。另外,我们合成了新的结构衍生物,并在竞争性的放射性核素结合测定中对大麻素受体进行了研究。

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