Literature DB >> 16154745

Design, synthesis, and bioavailability evaluation of coumarin-based prodrug of meptazinol.

Qiong Xie1, Xiaolin Wang, Xinghai Wang, Zhiqiang Jiang, Zhuibai Qiu.   

Abstract

Based on the known coumarin-based prodrug system, a new meptazinol (Z)-3-[2-(propionyloxy) phenyl]-2-propenoic ester (3) was designed and synthesized as prodrug to minimize the first-pass effect of meptazinol (1) and improve the oral bioavailability. The prodrug (3) showed a 4-fold increase in oral bioavailability over the parent drug meptazinol in rats.

Entities:  

Mesh:

Substances:

Year:  2005        PMID: 16154745     DOI: 10.1016/j.bmcl.2005.08.016

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  A novel prodrug strategy to improve the oral absorption of O-desmethylvenlafaxine.

Authors:  Mingyuan Liu; Yantong Sun; Sen Zhao; Youxin Li; Riyang Piao; Yan Yang; Jingkai Gu
Journal:  Exp Ther Med       Date:  2016-06-14       Impact factor: 2.447

2.  A prochelator with a modular masking group featuring hydrogen peroxide activation with concurrent fluorescent reporting.

Authors:  Andrew T Franks; Katherine J Franz
Journal:  Chem Commun (Camb)       Date:  2014-10-07       Impact factor: 6.222

Review 3.  Natural Coumarins: Exploring the Pharmacological Complexity and Underlying Molecular Mechanisms.

Authors:  Javad Sharifi-Rad; Natália Cruz-Martins; Pía López-Jornet; Eduardo Pons-Fuster Lopez; Nidaa Harun; Balakyz Yeskaliyeva; Ahmet Beyatli; Oksana Sytar; Shabnum Shaheen; Farukh Sharopov; Yasaman Taheri; Anca Oana Docea; Daniela Calina; William C Cho
Journal:  Oxid Med Cell Longev       Date:  2021-08-23       Impact factor: 6.543

  3 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.