Literature DB >> 28430430

Design, Synthesis, and Evaluation of Novel 2,6-Disubstituted Phenol Derivatives as General Anesthetics.

Linlin Qin1, Lei Ren1, Songlin Wan1, Guoliang Liu1, Xinfeng Luo1, Zhenhong Liu1, Fangqiong Li1, Yan Yu1, Jianyu Liu1, Yonggang Wei1.   

Abstract

A novel series of optically active 2,6-disubstituted alkylphenols with improved anesthetic profiles compared to widely used propofol were synthesized. The incorporation of the cyclopropyl group not only increased the steric effect but also introduced stereoselective effects over their anesthetic properties. Compounds 1, 2, and 6 were selected as potential candidates for further preclinical development including studies of their water-soluble prodrugs. Clinical studies of candidate compound 6 (Haisco HSK3486) as a general anesthetic are being performed in Australia and China.

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Year:  2017        PMID: 28430430     DOI: 10.1021/acs.jmedchem.7b00254

Source DB:  PubMed          Journal:  J Med Chem        ISSN: 0022-2623            Impact factor:   7.446


  13 in total

1.  Pharmacokinetic and pharmacodynamic properties of ciprofol emulsion in Chinese subjects: a single center, open-label, single-arm dose-escalation phase 1 study.

Authors:  Yi Teng; Meng-Chan Ou; Xiao Wang; Wen-Sheng Zhang; Xiao Liu; Yong Liang; Yun-Xia Zuo; Tao Zhu; Bin Liu; Jin Liu
Journal:  Am J Transl Res       Date:  2021-12-15       Impact factor: 4.060

Review 2.  What's New in Intravenous Anaesthesia? New Hypnotics, New Models and New Applications.

Authors:  Remco Vellinga; Beatrijs I Valk; Anthony R Absalom; Michel M R F Struys; Clemens R M Barends
Journal:  J Clin Med       Date:  2022-06-17       Impact factor: 4.964

3.  Tandem Peterson olefination and chemoselective asymmetric hydrogenation of β-hydroxy silanes.

Authors:  Suppachai Krajangsri; Haibo Wu; Jianguo Liu; Wangchuk Rabten; Thishana Singh; Pher G Andersson
Journal:  Chem Sci       Date:  2019-02-04       Impact factor: 9.825

4.  Efficacy and Safety of Ciprofol Sedation in ICU Patients with Mechanical Ventilation: A Clinical Trial Study Protocol.

Authors:  Yongjun Liu; Chuanxi Chen; Ning Liu; Li Tong; Yao Nie; Jianfeng Wu; Xiao Liu; Wei Gao; Lei Tang; Xiangdong Guan
Journal:  Adv Ther       Date:  2021-08-21       Impact factor: 3.845

5.  Sedation Effects Produced by a Ciprofol Initial Infusion or Bolus Dose Followed by Continuous Maintenance Infusion in Healthy Subjects: A Phase 1 Trial.

Authors:  Chao Hu; Xiaofeng Ou; Yi Teng; Shiqing Shu; Ying Wang; Xiaohong Zhu; Yan Kang; Jia Miao
Journal:  Adv Ther       Date:  2021-09-24       Impact factor: 3.845

6.  Pharmacodynamics and Pharmacokinetics of HSK3486, a Novel 2,6-Disubstituted Phenol Derivative as a General Anesthetic.

Authors:  Juan Liao; Meiting Li; Chaoli Huang; Yan Yu; Yashu Chen; Jiaqi Gan; Jie Xiao; Guilin Xiang; Xizhi Ding; Rong Jiang; Peng Li; Mengchang Yang
Journal:  Front Pharmacol       Date:  2022-02-03       Impact factor: 5.810

7.  Efficacy and Safety of HSK3486 for Anesthesia/Sedation in Patients Undergoing Fiberoptic Bronchoscopy: A Multicenter, Double-Blind, Propofol-Controlled, Randomized, Phase 3 Study.

Authors:  Zhen Luo; Hong Tu; Xiang Zhang; Xiao Wang; Wen Ouyang; Xinchuan Wei; Xiaohua Zou; Zhaoqiong Zhu; Yalan Li; Wangning Shangguan; Hui Wu; Yaping Wang; Qulian Guo
Journal:  CNS Drugs       Date:  2022-02-14       Impact factor: 5.749

8.  Esketamine as an Adjuvant to Ciprofol or Propofol Sedation for Same-Day Bidirectional Endoscopy: Protocol for a Randomized, Double-Blind, Controlled Trial With Factorial Design.

Authors:  Yu-Qin Long; Chang-Dong Feng; Yun-Ying Ding; Xiao-Mei Feng; Hong Liu; Fu-Hai Ji; Ke Peng
Journal:  Front Pharmacol       Date:  2022-03-18       Impact factor: 5.810

9.  Comparison and Clinical Value of Ciprofol and Propofol in Intraoperative Adverse Reactions, Operation, Resuscitation, and Satisfaction of Patients under Painless Gastroenteroscopy Anesthesia.

Authors:  Xingqu Chen; Ping Guo; Li Yang; Zhuoling Liu; Deshui Yu
Journal:  Contrast Media Mol Imaging       Date:  2022-07-18       Impact factor: 3.009

Review 10.  Recent advances in intravenous anesthesia and anesthetics.

Authors:  Mohamed Mahmoud; Keira P Mason
Journal:  F1000Res       Date:  2018-04-17
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