Synthesis of 2H-1,3-benzoxazin-4(3H)-one derivatives containing indole moiety: Their in vitro evaluation against PDE4B |
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| Institution: | 1. Dr. Reddys Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India;2. Department of Chemistry, Acharya Nagarjuna University, Guntur, Andhra Pradesh, India;3. Department of Chemistry, Krishna University, Krishna Dist., Andhra Pradesh, India;4. Doctoral Programme in Experimental Biology and Biomedicine, Center for Neuroscience and Cell Biology, University of Coimbra, 3004-517 Coimbra, Portugal;1. TU Bergakademie Freiberg, Institut für Anorganische Chemie, Leipziger Straße 29, 09599 Freiberg, Germany;2. TU Bergakademie Freiberg, Institut für Analytische Chemie, Leipziger Straße 29, 09599 Freiberg, Germany;1. Department of Chemistry, Taiyuan Normal University, Jinzhong 030619, PR China;2. College of Chemistry and Environmental Science, Hebei University, Baoding 071002, PR China;3. Key Laboratory of Advanced Energy Materials Chemistry (Ministry of Education), Nankai University, Tianjin 300071, PR China;4. Department of Biology, Taiyuan Normal University, Jinzhong 030619, PR China;1. School of Pharmacy, Sungkyunkwan University, Suwon 440-746, Republic of Korea;2. College of Pharmacy, Dongguk University-Seoul, Goyang 410-820, Republic of Korea;1. Department of Chemistry and Division of Natural and Applied Sciences, Hope College, Holland, MI 49422, USA;2. Department of Chemistry, John Carroll University, University Heights, OH 44118, USA |
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| Abstract: | A number of 2H-1,3-benzoxazin-4(3H)-one derivatives containing indole or benzofuran moieties were synthesized by using Pd/C–Cu mediated coupling-cyclization strategy as a key step. The o-iodoanilides or o-iodophenol were coupled with 3-{2-(prop-2-ynyloxy)ethyl}-2H-benzoe]1,3]oxazin-4(3H)-one using 10%Pd/C–CuI–PPh3 as a catalyst system and Et3N as a base to give the target compounds. All the synthesized compounds were tested for their PDE4B inhibitory potential in vitro using a cell based cAMP reporter assay. Some of them showed fold increase of the cAMP level when tested at 30 μM. A representative compound showed encouraging PDE4B inhibitory properties that were supported by its docking results. |
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| Keywords: | Indole Benzofuran Pd/C PDE4 |
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