title: Discovery of novel benzoxaborole-based potent antitrypanosomal agents.
abstract: We report the discovery of benzoxaborole antitrypanosomal agents and their structure-activity relationships on central linkage groups and different substitution patterns in the sulfur-linked series. The compounds showed in vitro growth inhibition IC50 values as low as 0.02 μg/mL and in vivo efficacy in acute murine infection models against Tryapnosoma brucei.
authors.affiliation: School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Dazhong
authors.initials: D
authors.lastname: Ding
authors.affiliation: School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Yaxue
authors.initials: Y
authors.lastname: Zhao
authors.affiliation: School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Qingqing
authors.initials: Q
authors.lastname: Meng
authors.affiliation: School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Dongsheng
authors.initials: D
authors.lastname: Xie
authors.affiliation: SCYNEXIS, Inc., P.O. Box 12878, Research Triangle Park, North Carolina 27709.
authors.forename: Bakela
authors.initials: B
authors.lastname: Nare
authors.affiliation: SCYNEXIS, Inc., P.O. Box 12878, Research Triangle Park, North Carolina 27709.
authors.forename: Daitao
authors.initials: D
authors.lastname: Chen
authors.affiliation: Haskins Laboratory, Pace University, New York, New York 10038.
authors.forename: Cyrus J
authors.initials: CJ
authors.lastname: Bacchi
authors.affiliation: Haskins Laboratory, Pace University, New York, New York 10038.
authors.forename: Nigel
authors.initials: N
authors.lastname: Yarlett
authors.affiliation: Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
authors.forename: Yong-Kang
authors.initials: YK
authors.lastname: Zhang
authors.affiliation: Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
authors.forename: Vincent
authors.initials: V
authors.lastname: Hernandez
authors.affiliation: Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
authors.forename: Yi
authors.initials: Y
authors.lastname: Xia
authors.affiliation: Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
authors.forename: Yvonne
authors.initials: Y
authors.lastname: Freund
authors.affiliation: Small Molecule Discovery Center and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158.
authors.forename: Maha
authors.initials: M
authors.lastname: Abdulla
authors.affiliation: Small Molecule Discovery Center and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158.
authors.forename: Kean-Hooi
authors.initials: KH
authors.lastname: Ang
authors.affiliation: Small Molecule Discovery Center and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158.
authors.forename: Joseline
authors.initials: J
authors.lastname: Ratnam
authors.affiliation: Small Molecule Discovery Center and Sandler Center for Basic Research in Parasitic Diseases, University of California, San Francisco, California 94158.
authors.forename: James H
authors.initials: JH
authors.lastname: McKerrow
authors.affiliation: SCYNEXIS, Inc., P.O. Box 12878, Research Triangle Park, North Carolina 27709.
authors.forename: Robert T
authors.initials: RT
authors.lastname: Jacobs
authors.affiliation: School of Pharmacy and E-Institute of Chemical Biology, Shanghai Jiao Tong University, Shanghai, 200240, China.
authors.forename: Huchen
authors.initials: H
authors.lastname: Zhou
authors.affiliation: Anacor Pharmaceuticals Inc., 1020 East Meadow Circle, Palo Alto, California 94303.
authors.forename: Jacob J
authors.initials: JJ
authors.lastname: Plattner
keywords: African trypanosomiasis; Tryapnosoma brucei; benzoxaborole