Chemical and Pharmaceutical Bulletin p. 1138 - 1147 (2000)
Update date:2022-09-26
Topics:
Liao
Hendrata
Sung Yong Bae
Wang
A coumarin-based prodrug system has been recently developed in our laboratory for the preparation of esterase-sensitive prodrugs of amines, peptides, and peptidomimetics. The drug release rates from this prodrug system were found to be dependent on the structural features of the drug moiety. In certain cases, the release can be undesirably slow for drugs that are secondary amines with relatively high pK(a)'s. Aimed at finding ways to manipulate the release rates to suit the need of different drugs, we have examined the effect of the phenyl ring substitutions on the release kinetics of such prodrugs and found that appropriately positioned alkyl substituents on the phenyl ring could help to facilitate the release by as much as 16-fold. Therefore, introduction of alkyl substituents on the phenyl ring should allow us to manipulate the release rates and, therefore, time profiles for different drugs.
View MoreShanghai Mintchem Development ., Ltd
Contact:0086 21 5190 8570
Address:R602,4#,89Nong, Mudan Road Pudong Shanghai China
Zhangjiagang Golden Reach Fine Chemical Co.,LTD.
Contact:+86-512-6585 6968
Address:Changfu Road， Dongsha Chemical Industry Park, Zhangjiagang City, Jiangsu Province, China
Puyang Huicheng Electronic Material Co., Ltd
website:http://huichengchem.weba.testwebsite.cn/index_en.html
Contact:+86-393-8910800
Address:West Section Shengli Road, Puyang457000, China
Shanghai Yuking Water Soluble Material Tech Co., Ltd
Contact:86-21-68286299
Address:4F, 13B, No. 600, South Xinyuan Road 201306, Shanghai, China
Contact:+86-533-3112891
Address:zibo
Doi:10.24820/ark.5550190.p010.820
(2019)Doi:10.1007/BF00755080
()Doi:10.1039/jr9630000410
(1963)Doi:10.1021/jo00818a017
(1971)Doi:10.1021/jo00818a019
(1971)Doi:10.1039/c1gc15457e
(2011)
