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新型二氢嘧啶类及其吡唑衍生物的合成与药理筛选。

Novel dihydropyrimidines and its pyrazole derivatives: synthesis and pharmacological screening.

机构信息

Department of Pharmaceutical Chemistry, S.A.C. College of Pharmacy, B.G. Nagara 571448, Nagamangala (tq), Mandya (dist), Karnataka, India.

出版信息

Eur J Med Chem. 2011 May;46(5):1882-91. doi: 10.1016/j.ejmech.2011.02.052. Epub 2011 Feb 26.

Abstract

In the present study, we have synthesized novel dihydropyrimidines (1a-j), their dimethylated adducts (2a-j), and hydrazine derivatives (3a-j) of 2a-j and subsequently their pyrazole derivatives (4a-j). Elemental analysis, IR, 1H NMR and mass spectral data elucidated structure of newly synthesized compounds. Some of these novel derivatives showed moderate to potent in vitro antioxidant, anti-inflammatory, antibacterial, antifungal and anthelmintic activity.

摘要

在本研究中,我们合成了新型的二氢嘧啶(1a-j)、它们的二甲加成物(2a-j)以及它们的肼衍生物(3a-j),随后还合成了它们的吡唑衍生物(4a-j)。元素分析、IR、1H NMR 和质谱数据阐明了新合成化合物的结构。这些新型衍生物中的一些表现出中等至较强的体外抗氧化、抗炎、抗菌、抗真菌和驱虫活性。

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