title: Discovery and structure-activity study of a novel benzoxaborole anti-inflammatory agent (AN2728) for the potential topical treatment of psoriasis and atopic dermatitis.
abstract: A series of phenoxy benzoxaboroles were synthesized and screened for their inhibitory activity against PDE4 and cytokine release. 5-(4-Cyanophenoxy)-2,3-dihydro-1-hydroxy-2,1-benzoxaborole (AN2728) showed potent activity both in vitro and in vivo. This compound is now in clinical development for the topical treatment of psoriasis and being pursued for the topical treatment of atopic dermatitis.
authors.affiliation: Anacor Pharmaceuticals, Inc, Palo Alto, CA 94303, USA. takama@anacor.com
authors.forename: Tsutomu
authors.initials: T
authors.lastname: Akama
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Baker
authors.forename: Yong-Kang
authors.initials: YK
authors.lastname: Zhang
authors.forename: Vincent
authors.initials: V
authors.lastname: Hernandez
authors.forename: Huchen
authors.initials: H
authors.lastname: Zhou
authors.forename: Virginia
authors.initials: V
authors.lastname: Sanders
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Freund
authors.forename: Richard
authors.initials: R
authors.lastname: Kimura
authors.forename: Kirk R
authors.initials: KR
authors.lastname: Maples
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Plattner
mesh_terms: D000287:Administration, Topical; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry*; D001896:Boron Compounds / Q000008:administration & dosage / Q000737:chemistry*; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage / Q000737:chemistry*; D003876:Dermatitis, Atopic / Q000188:drug therapy* / Q000473:pathology; D003879:Dermatologic Agents / Q000008:administration & dosage / Q000737:chemistry*; D004487:Edema / Q000188:drug therapy / Q000473:pathology; D006801:Humans; D051379:Mice; D011565:Psoriasis / Q000188:drug therapy* / Q000473:pathology; D013329:Structure-Activity Relationship; D020298:U937 Cells
chemical_list: D000894:Anti-Inflammatory Agents, Non-Steroidal; D001896:Boron Compounds; D019086:Bridged Bicyclo Compounds, Heterocyclic; D003879:Dermatologic Agents; C543085:crisaborole