Synthesis and Antimuscarinic Activity of Derivatives of 2-Substituted-1,3-Dioxolanes

被引:0
|
作者
Gabriella Marucci
Angeli Piero
Livio Brasili
Michela Buccioni
Dario Giardinà
Ugo Gulini
Alessandro Piergentili
Gianni Sagratini
机构
[1] University of Camerino,Department of Chemical Sciences
[2] University of Modena and Reggio Emilia,Department of Pharmaceutical Sciences
来源
关键词
Trans Isomer; Functional Test; Trimethylammonium; Dioxolanes; Methiodides;
D O I
暂无
中图分类号
学科分类号
摘要
Geometric cis, trans isomers, derivatives of 2-substituted-1,3-dioxanes were designed and studied as antimuscarinic agents. The synthesized compounds were evaluated as perchlorides and methiodides by functional tests with rabbit vas deferens (putative M1), guinea-pig heart (M2) and guinea-pig ileum (M3). The effect of the replacement of a trimethylammonium group with a dimethysulfonium in the two rings was also evaluated. Pharmacological results indicate that the 1,3-dioxane nucleus shows the highest stereoselective values on the studied receptors.
引用
收藏
页码:274 / 296
页数:22
相关论文
共 50 条
  • [1] Synthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes
    Marucci, Gabriella
    Angeli, Piero
    Brasili, Livio
    Buccioni, Michela
    Giardinà, Dario
    Gulini, Ugo
    Piergentili, Alessandro
    Sagratini, Gianni
    MEDICINAL CHEMISTRY RESEARCH, 2005, 14 (05) : 274 - 296
  • [2] Synthesis and antimuscarinic activity of derivatives of 2-substituted-1,3-dioxolanes
    Marucci, Gabriella
    Angeli, Piero
    Brasili, Livio
    Buccioni, Michela
    Giardina, Dario
    Gulini, Ugo
    Piergentili, Alessandro
    Sagratini, Gianni
    Franchini, Silvia
    MEDICINAL CHEMISTRY RESEARCH, 2005, 14 (06) : 309 - 331
  • [3] Synthesis and Antimuscarinic Activity of Derivatives of 2-Substituted-1,3-Dioxolanes
    Gabriella Marucci
    Piero Angeli
    Livio Brasili
    Michela Buccioni
    Dario Giardinà
    Ugo Gulini
    Alessandro Piergentili
    Gianni Sagratini
    Silvia Franchini
    Medicinal Chemistry Research, 2005, 14 : 309 - 331
  • [4] ANTIMUSCARINIC ACTIVITY IN A SERIES OF 2-SUBSTITUTED 1,3-DIOXOLANES
    ANGELI, P
    GULINI, U
    MELONI, MT
    PAPARELLI, F
    QUAGLIA, W
    MEDICINAL CHEMISTRY RESEARCH, 1995, 5 (04) : 271 - 280
  • [5] Synthesis of monoprotected 1,4-diketones by photoinduced alkylation of enones with 2-substituted-1,3-dioxolanes
    Mosca, R
    Fagnoni, M
    Mella, M
    Albini, A
    TETRAHEDRON, 2001, 57 (52) : 10319 - 10328
  • [6] Antibacterial Activity of Substituted 1,3-Dioxolanes
    M. N. Ovsyannikova
    V. B. Vol’eva
    I. S. Belostotskaya
    N. L. Komissarova
    A. V. Malkova
    L. N. Kurkovskaya
    Pharmaceutical Chemistry Journal, 2013, 47 : 142 - 145
  • [7] Antibacterial Activity of Substituted 1,3-Dioxolanes
    Ovsyannikova, M. N.
    Vol'eva, V. B.
    Belostotskaya, I. S.
    Komissarova, N. L.
    Malkova, A. V.
    Kurkovskaya, L. N.
    PHARMACEUTICAL CHEMISTRY JOURNAL, 2013, 47 (03) : 142 - 145
  • [8] SYNTHESIS OF SOME SUBSTITUTED 1,3-DIOXOLANES
    KUZNETSO.NV
    MYRSINA, RA
    UKRAINSKII KHIMICHESKII ZHURNAL, 1970, 36 (10): : 1050 - &
  • [9] SYNTHESIS OF 2-ALKOXY-1,3-DIOXOLANES AND 2-ARYLOXY-1,3-DIOXOLANES
    SOULIER, J
    FARINES, M
    AUTHIER, RM
    FOURNIER, M
    JOURNAL OF HETEROCYCLIC CHEMISTRY, 1976, 13 (05) : 1125 - 1128
  • [10] Synthesis, NMR spectroscopy study, and antimuscarinic activity of a series of 2-(acyloxymethyl)-1,3-dioxolanes
    Malmusi, L
    Mucci, A
    Schenetti, L
    Gulini, U
    Marucci, G
    Livio, B
    BIOORGANIC & MEDICINAL CHEMISTRY, 1996, 4 (12) : 2071 - 2080