Synthesis and 尾-glucuronidase inhibitory activity of 2-arylquinazolin-4(3H)-ones

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• 作者：Khalid Mohammed Khan^a ; ^{hassaan2@super.net.pk" class="auth_mail} ; ^{khalid.khan@iccs.edu" class="auth_mail} ; Syed Muhammad Saad^a ; Nimra Naveed Shaikh^a ; Shafqat Hussain^a ; Muhammad Imran Fakhri^a ; Shahnaz Perveen^b ; Muhammad Taha^d ; Muhammad Iqbal Choudhary^a ; ^c
• 关键词：2-Arylquinazolin-4(3H)-ones ; 尾-Glucuronidase inhibition ; Structure&ndash ; activity relationship ; Cytotoxicity
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：1 July 2014
• 年：2014
• 卷：22
• 期：13
• 页码：3449-3454
• 全文大小：2285 K

文摘

2-Arylquinazolin-4(3H)-ones 1–25 were synthesized by reacting anthranilamide with various benzaldehydes using CuCl₂·2H₂O as a catalyst in ethanol under reflux. Synthetic 2-arylquinazolin-4(3H)-ones 1–25 were evaluated for their 尾-glucuronidase inhibitory potential. A trend of inhibition IC₅₀ against the enzyme in the range of 0.6–198.2 渭M, was observed and compared with the standard d-saccharic acid 1,4-lactone (IC₅₀ = 45.75 ± 2.16 渭M). Compounds 13, 19, 4, 12, 14, 22, 23, 25, 15, 8, 17, 11, 21, 1, 3, 18, 9, 2, and 24 with the IC₅₀ values within the range of 0.6–44.0 渭M, indicated that the compounds have superior activity than the standard. The compounds showed no cytotoxic effects against PC-3 cells. A structure–activity relationship is established.