1,2,3-Triazoles derived from olanzapine: their synthesis via an ultrasound assisted CuAAC method and evaluation as inhibitors of PDE4B

Abstract

An ultrasound assisted CuAAC method afforded novel 1,2,3-triazoles derived from olanzapine as inhibitors of PDE4B.

CuAAC-ensembled 1,2,3-triazole-linked isosteres as pharmacophores in drug discovery: review

“…The comparative results signify that the compounds having unsubstituted benzene ring attached with 1,2,3-triazole have better inhibition tendency as compared to mono-substituted benzene ring. 95 2,2,4-Trimethyl-1,2-dihydroquinolinyl substituted 1,2,3-triazole derivatives 57 were developed and were examined for their PDE4B inhibitor capacity as well as anticancer properties. The standard inhibition percentage of PDE4B at 30 mM is 58.2% and also has a notable value of IC 50 ¼ 8.7 AE 0.24 towards the A549 cancer cell line.…”

Synthesis of hybrid perillyl‐4H‐pyrans. Cytotoxicity evaluation against hepatocellular carcinoma HepG2/C3A cell line

“…[ 55 ] Heterogeneous catalysis, greener process or ultrasound‐promoted reaction also brought technical improvements performing this methodology. [ 56–58 ] Thus, the 4‐arylpropargyloxy‐4 H ‐pyrans 10a–o were used as substrate for the preparation of hybrid compounds by reaction with perillyl azide ( 14 ) under catalysis of CuSO 4 /Na‐ascorbate system (Scheme 5). The results are shown in Table , below.…”

Semi-synthesis of β-keto-1,2,3-triazole derivatives from ethinylestradiol and evaluation of the cytotoxic activity

“…Also there are studies in the literature describing the synthesis and evaluation of biological activity of other 1,2,3-triazole derivates [22, 23, 24, 25]. The coumarin-1,2,3-triazole-dithiocarbamate hybrids were designed, synthesized and evaluated for their inhibitory activity towards lysine specific demethylase 1 (LSD1).…”