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A number of novel imidazophenoxazine-4-sulfonamides have been designed as potential inhibitors of PDE4. All these compounds were readily prepared via an elegant multi-step method involving the initial construction of 1-nitro-10H-phenoxazine ring and then fused imidazole ring as key steps. Some of these compounds showed promising PDE4B and D inhibition when tested in vitro and good interactions with these proteins in silico. Three of these compounds showed dose dependent inhibition of PDE4B with IC50 value of 3.31 ± 0.62, 1.23 ± 0.18 and 0.53 ± 0.18 μM. Copyright © 2013 Elsevier Ltd. All rights reserved.


Seelam Venkata Reddy, Gangula Mohan Rao, Baru Vijaya Kumar, Chandana L T Meda, Girdhar Singh Deora, K Shiva Kumar, Kishore V L Parsa, Manojit Pal. Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4. Bioorganic & medicinal chemistry. 2013 Apr 1;21(7):1952-63

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PMID: 23415088

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