Bioorganic & Medicinal Chemistry Letters 2005-11-15

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

Qiong Xie, Xiaolin Wang, Xinghai Wang, Zhiqiang Jiang, Zhuibai Qiu

Index: Bioorg. Med. Chem. Lett. 15(22) , 4953-6, (2005)

Full Text: HTML

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.

Related Compounds

Related Articles:

Bis(9)-(-)-nor-meptazinol as a novel dual-binding AChEI potently ameliorates scopolamine-induced cognitive deficits in mice.

2013-03-01

[Pharmacol. Biochem. Behav. 104 , 138-43, (2013)]

Reflex activity caused by laryngoscopy and intubation is obtunded differently by meptazinol, nalbuphine and fentanyl.

2007-01-01

[Eur. J. Anaesthesiol. 24(1) , 53-8, (2007)]

Lack of sensitization during place conditioning in rats is consistent with the low abuse potential of tramadol.

2002-08-23

[Neurosci. Lett. 329(1) , 25-8, (2002)]

Synthesis and relative bioavailability of meptazinol benzoyl esters as prodrugs.

2005-05-16

[Bioorg. Med. Chem. Lett. 15(10) , 2607-9, (2005)]

Protection of acetylcholinesterase by meptazinol in mice exposed to di-isopropyl fluorophosphate. Comparison with physostigmine.

1991-05-01

[J. Pharm. Pharmacol. 43(5) , 366-9, (1991)]

More Articles...