Synthesis and evaluation of α,α-disubstituted-3-mercaptopropanoic acids as inhibitors for carboxypeptidase A and implications with respect to enzyme inhibitor design
摘要:
2-Ethyl-2-meth% 1-3-mercaptopropanoic acid (6) and 2-benzyl-2-methyl-3-mercaptopropanoic acid (7) were synthesized and evaluated as inhibitors for carboxypeptidase A (CPA), a prototypical zinc protease with the expectation that the binding affinities of these inhibitors would be augmented over those of 2-ethyl-3-methylsuccinic acid (2) and 2-benzyl-3-methylsuccinic acid (3), respectively, in light of the fact that the sulfhydryl group is a better zinc coordinating moiety than the carboxylate group. Contrary to the expectation. however. the inhibitory potency of 6 was not improved and that of 7 was rather attenuated by the replacement. A probable explanation for the unexpected results is offered. (C) 2003 Elsevier Ltd. All rights reserved.
Synthesis and evaluation of α,α-disubstituted-3-mercaptopropanoic acids as inhibitors for carboxypeptidase A and implications with respect to enzyme inhibitor design
摘要:
2-Ethyl-2-meth% 1-3-mercaptopropanoic acid (6) and 2-benzyl-2-methyl-3-mercaptopropanoic acid (7) were synthesized and evaluated as inhibitors for carboxypeptidase A (CPA), a prototypical zinc protease with the expectation that the binding affinities of these inhibitors would be augmented over those of 2-ethyl-3-methylsuccinic acid (2) and 2-benzyl-3-methylsuccinic acid (3), respectively, in light of the fact that the sulfhydryl group is a better zinc coordinating moiety than the carboxylate group. Contrary to the expectation. however. the inhibitory potency of 6 was not improved and that of 7 was rather attenuated by the replacement. A probable explanation for the unexpected results is offered. (C) 2003 Elsevier Ltd. All rights reserved.
RETARDATION FILM, POLARIZING PLATE, LIQUID CRYSTAL DISPLAY AND MANUFACTURING METHOD OF RETARDATION FILM
申请人:TAMAGAWA Minori
公开号:US20080233311A1
公开(公告)日:2008-09-25
A retardation film comprising a cellulose derivative and a plasticizer, wherein a total haze, Htotal, of the retardation film meets the following condition: 0.1%≦Htotal≦0.4%; and a ratio of a internal haze, Hi, to the total haze, Hi/Htotal, of the retardation film meets the following condition: Hi/Htotal≦0.5.
US8840973B2
申请人:——
公开号:US8840973B2
公开(公告)日:2014-09-23
Synthesis and evaluation of α,α-disubstituted-3-mercaptopropanoic acids as inhibitors for carboxypeptidase A and implications with respect to enzyme inhibitor design
作者:Hyun Soo Lee、Dong H Kim
DOI:10.1016/j.bmc.2003.08.017
日期:2003.11
2-Ethyl-2-meth% 1-3-mercaptopropanoic acid (6) and 2-benzyl-2-methyl-3-mercaptopropanoic acid (7) were synthesized and evaluated as inhibitors for carboxypeptidase A (CPA), a prototypical zinc protease with the expectation that the binding affinities of these inhibitors would be augmented over those of 2-ethyl-3-methylsuccinic acid (2) and 2-benzyl-3-methylsuccinic acid (3), respectively, in light of the fact that the sulfhydryl group is a better zinc coordinating moiety than the carboxylate group. Contrary to the expectation. however. the inhibitory potency of 6 was not improved and that of 7 was rather attenuated by the replacement. A probable explanation for the unexpected results is offered. (C) 2003 Elsevier Ltd. All rights reserved.