Synthesis and bioactivity of 3,5-dimethylpyrazole derivatives as potential PDE4 inhibitors

Hu, De-Kun; Zhao, Dongsheng; He, Min; Jin, Hongwei; Tang, Yongmei; Zhang, Lian-Hui; Song, Gaopeng; Cui, Zi‐Ning

doi:10.1016/j.bmcl.2018.03.031

Cited by 9 publications

(1 citation statement)

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“…On the basis of related materials, pyrazoles, especially 3, 5-dimethylpyrazol, occupy a distinct niche in heterocyclic chemistry and represent a key motif in medicinal chemistry because of their capability to exhibit an array of properties and bioactivities, including fungicidal (Wang et al, 2012), anticancer (Ganga-Reddy et al, 2016), anti-inflammatory (Hu et al, 2018), anticonvulsant (Kaymakcioğlu et al, 2003), and nitrification inhibitor (Şahan et al, 2017) activities. Furthermore, we also demonstrated that the benzothiazole nucleus is a unique scaffold for further molecular exploration to synthesize novel compounds.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and Biological Evaluation of Benzo[D]Thiazole with Dimethylpyrazol Derivatives

Liu

Cheng

Wang

2019

Asian Pac J Cancer Prev

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A series of new benzothiazole derivatives containing dimethylpyrazole were synthesized and evaluated for their anticonvulsant activity, neurotoxicity and cytotoxicity by using the maximal electroshock (MES), rotarod neurotoxicity (TOX) and MTT colorimetric assay. Among the compounds studied, four compounds (6a, 6b, 6g and 6m) showed better anticonvulsant than the others at 300 mg/kg and they also showed anticonvulsant activity at the dose of 100 mg/ kg. All the synthetic compounds showed lower neurotoxicity and little cytotoxicity, so that the compounds, which with better activities, also had higher protective index. In particular, the compound 6g, 2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-((2-fluorobenzyl)oxy)benzo[d]thiazole showed better activity with an ED 50 value of 160.4 mg/kg and higher protective index (PI) values of 2.74 in the MES test than the standard drugs sodium valproate, which used as positive controls in this study. After that the compound 6g demonstrated antagonistic activity against seizures induced by pentylenetetrazol, which proved 6g maybe exert activity through effecting GABAergic neurotransmission.

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Section: Introductionmentioning

confidence: 99%