1. Medicinal Chemistry Laboratory, Research Centre, C.K.M. Arts and Science College, Warangal 506 006, Andhra Pradesh, India;2. Institute of Life Sciences, University of Hyderabad Campus, Gachibowli, Hyderabad 500 046, India
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.