title: Novel imidazophenoxazine-4-sulfonamides: their synthesis and evaluation as potential inhibitors of PDE4.
abstract: 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.
authors: Medicinal Chemistry Laboratory, Research Centre, CKM Arts and Science College, Warangal 506 006, Andhra Pradesh, India.
authors: Seelam Venkata
authors: SV
authors: Reddy
authors: Gangula Mohan
authors: GM
authors: Rao
authors: Baru Vijaya
authors: BV
authors: Kumar
authors: Chandana L T
authors: CL
authors: Meda
authors: Girdhar Singh
authors: GS
authors: Deora
authors: K Shiva
authors: KS
authors: Kumar
authors: Kishore V L
authors: KV
authors: Parsa
authors: Manojit
authors: M
authors: Pal
mesh_terms: D000818:Animals; D002460:Cell Line; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4 / Q000378:metabolism; D062105:Molecular Docking Simulation; D010078:Oxazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D058988:Phosphodiesterase 4 Inhibitors / Q000737:chemistry* / Q000494:pharmacology*; D013449:Sulfonamides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D010078:Oxazines; D058988:Phosphodiesterase 4 Inhibitors; D013449:Sulfonamides; C039203:phenoxazine; D054703:Cyclic Nucleotide Phosphodiesterases, Type 4