title: Development of a novel class of pyrrolo-[1,2,5]benzothiadiazepine derivatives as potential anti-schistosomal agents.
abstract: Analogues of pyrrolo-[1,2,5]benzothiadiazepine were prepared and evaluated against Schistosoma japonica. The biological data revealed that most benzothiazepine derivatives show anti-schistosomal activity to some extent, while α-chloronation of the title compound and another bioisosteric derivative pyrrolo-[1,2,5]benzodiazepine displayed the most distinct worm killing activity. This study proved that benzodiazepine may serve as a novel structural skeleton for the development of anti-schistosomal agents.
authors.affiliation: College of Pharmaceutical Science, Soochow University, 199 Ren Ai Road, Suzhou 215123, China.
authors.forename: Jinglei
authors.initials: J
authors.lastname: Chen
authors.forename: Weizhen
authors.initials: W
authors.lastname: Sun
authors.forename: Jingjing
authors.initials: J
authors.lastname: Yang
authors.forename: Huan
authors.initials: H
authors.lastname: Sun
authors.forename: Zhixia
authors.initials: Z
authors.lastname: Wang
authors.forename: Lanlan
authors.initials: L
authors.lastname: Dong
authors.forename: Chunhua
authors.initials: C
authors.lastname: Qiao
authors.forename: Chao-ming
authors.initials: CM
authors.lastname: Xia
mesh_terms: D000818:Animals; D015195:Drug Design; D015394:Molecular Structure; D011758:Pyrroles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D012549:Schistosoma japonicum / Q000187:drug effects*; D013329:Structure-Activity Relationship; D013841:Thiazepines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D011758:Pyrroles; D013841:Thiazepines