title: Cyclosulfamide-based derivatives as inhibitors of noroviruses.
abstract: An optimization campaign focused on improving pharmacological activity and physicochemical properties of a recently-identified class of cyclosulfamide-based norovirus inhibitors has been carried out. Dimeric compound 4 was found to be a ∼10-fold more potent norovirus inhibitor (ED(50) 0.4 μM) compared to the original hit, however, isonipecotic acid ester derivatives 7e and 10a were shown to have superior therapeutic indices.
authors: Department of Chemistry, Wichita State University, Wichita, KS 67260, USA.
authors: Dengfeng
authors: D
authors: Dou
authors: Sivakoteswara R
authors: SR
authors: Mandadapu
authors: Kevin R
authors: KR
authors: Alliston
authors: Yunjeong
authors: Y
authors: Kim
authors: Kyeong-Ok
authors: KO
authors: Chang
authors: William C
authors: WC
authors: Groutas
mesh_terms: D000577:Amides / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D000998:Antiviral Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D002460:Cell Line; D020128:Inhibitory Concentration 50; D029322:Norovirus / Q000187:drug effects*; D000077489:Piperazine; D010879:Piperazines / Q000737:chemistry; D013329:Structure-Activity Relationship
chemical_list: D000577:Amides; D000998:Antiviral Agents; D010879:Piperazines; D000077489:Piperazine