Journal of Medicinal Chemistry
Journal of Medicinal Chemistry
4 years ago

Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle

Oral Delivery of Propofol with Methoxymethylphosphonic Acid as the Delivery Vehicle
Pengfei Liao, Yi Zhou, Xiaowei Zhang, Qingping Huang, Linlin Qin, Hongzhu Chu, Jianyu Liu, Xia Huang, Chen Zhang, Yonggang Wei, Pan Li, Aisheng Gong, Jia Ni, Pingming Tang, Guanpeng Qiu, Xinfeng Luo, Yan Yu, Guofei Qian, Pangke Yan, Guozhi Zhu, Yao Li, Qiu Gao, Yonghua Lu, Suxin Zheng, Bailin Lei
Phosphonamidate 3a of methoxymethylphosphonic acid (MMPA) with propofol (1) and l-alanine ethyl ester was found to be an efficient scaffold for the oral delivery of compound 1. The synthesis and evaluation of MMPA based phosphonamidates of compound 1, HSK3486 (2), and other phenolic drugs revealed the general application of MMPA as the effective delivery vehicle for phenolic drugs. On the basis of plasma concentrations of compound 1 and SN38 (14), the oral bioavailability of compound 3a and 15 in beagle dogs was found to be 97.6% and 34.1%, respectively.

Publisher URL: http://dx.doi.org/10.1021/acs.jmedchem.7b01133

DOI: 10.1021/acs.jmedchem.7b01133

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