title: Synthesis of substituted 6-amino-4-(2,4-dimethoxyphenyl)-[1,2]dithiolo[4,3-b]pyrrol-5-ones and their raising leukocyte count activities.
abstract: The design and synthesis of a series of substituted 6-amino-4-(2,4-dimethoxyphenyl)-[1,2]dithiolo[4,3-b]pyrrol-5-ones are described. All the synthesized compounds were evaluated for raising leukocyte count activities in normal mice. Four compounds (8a, b, d, h) exhibited raising leukocyte count activities close or higher than positive control recombinant human granulocyte colony stimulating factor (rhG-CSF), and some (8e-g, k, p, r) had a moderate effect. Among them, the most potent compound 8a was evaluated for its antileukopenia activity in cyclophosphamide (CTX) treated mice. Interestingly, 8a exhibited significant antileukopenia activity as compared to rhG-CSF. The results suggest that this kind of compounds might be utilized for the development of new candidate for treatment of leukocytopenia.
authors.affiliation: Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, Shanghai, P.R. China.
authors.forename: Xiangduan
authors.initials: X
authors.lastname: Tan
authors.forename: Chungang
authors.initials: C
authors.lastname: Li
authors.forename: Zhenpeng
authors.initials: Z
authors.lastname: Yu
authors.forename: Panfeng
authors.initials: P
authors.lastname: Wang
authors.forename: Siyun
authors.initials: S
authors.lastname: Nian
authors.forename: Yifang
authors.initials: Y
authors.lastname: Deng
authors.forename: Wei
authors.initials: W
authors.lastname: Wu
authors.forename: Guoping
authors.initials: G
authors.lastname: Wang
mesh_terms: D000818:Animals; D003520:Cyclophosphamide / Q000494:pharmacology; D016179:Granulocyte Colony-Stimulating Factor / Q000378:metabolism; D007958:Leukocyte Count; D007962:Leukocytes / Q000166:cytology / Q000187:drug effects* / Q000378:metabolism; D007970:Leukopenia / Q000097:blood / Q000188:drug therapy*; D051379:Mice; D008807:Mice, Inbred BALB C; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D011994:Recombinant Proteins / Q000378:metabolism
chemical_list: D011758:Pyrroles; D011994:Recombinant Proteins; D016179:Granulocyte Colony-Stimulating Factor; D003520:Cyclophosphamide