Synthesis and in vitro evaluation of S-acyl-3-thiopropyl prodrugs of Foscarnet
摘要:
A new enzyme-labile group called S-acyl-3-thiopropyl group (SATP) has been synthesized from allylic esters of phosphonate. After demonstration of the enzyme-labile character of the SATP in cellular extracts, it has been introduced onto the phosphonate moiety of PFA (Foscarnet) to obtain potential lipophilic prodrugs. To ponder the lipophilicity of the triesters of PFA, esters of monomethylether of polyethyleneglycols and of thioglycerol were introduced on the PFA carboxylate moiety. The SATP groups were introduced in an attempt to deliver PFA after bioactivation inside the cells. The PFA prodrugs were evaluated in vitro for their activity against human immunodeficiency viruses (HIV-1 and HIV-2). (C) 2004 Elsevier Ltd. All rights reserved.
Synthesis and in vitro evaluation of S-acyl-3-thiopropyl prodrugs of Foscarnet
摘要:
A new enzyme-labile group called S-acyl-3-thiopropyl group (SATP) has been synthesized from allylic esters of phosphonate. After demonstration of the enzyme-labile character of the SATP in cellular extracts, it has been introduced onto the phosphonate moiety of PFA (Foscarnet) to obtain potential lipophilic prodrugs. To ponder the lipophilicity of the triesters of PFA, esters of monomethylether of polyethyleneglycols and of thioglycerol were introduced on the PFA carboxylate moiety. The SATP groups were introduced in an attempt to deliver PFA after bioactivation inside the cells. The PFA prodrugs were evaluated in vitro for their activity against human immunodeficiency viruses (HIV-1 and HIV-2). (C) 2004 Elsevier Ltd. All rights reserved.
NONAQUEOUS ELECTROLYTE SOLUTION, ELECTRICITY STORAGE DEVICE USING SAME, AND PHOSPHONOFORMIC ACID COMPOUND USED IN SAME
申请人:UBE INDUSTRIES, LTD
公开号:US20160315351A1
公开(公告)日:2016-10-27
The present invention provides a nonaqueous electrolytic solution capable of suppressing worsening of heat stability of a negative electrode and improving safety of an energy storage device while maintaining high-load charging and discharging cycle properties at a high temperature, an energy storage device using the same, and a phosphonoformic acid compound to be used for the same. The nonaqueous electrolytic solution having an electrolyte salt dissolved in a nonaqueous solvent contains 0.001 to 5% by mass of at least one selected from a phosphonoformic acid compound having at least one carbon-carbon unsaturated bond, which is represented by the following general formula (I), and a phosphonoformic acid compound having a carbon-carbon unsaturated bond or two phosphonocarbonyl groups, which is represented by the following general formula (II).
In the formula (I), each of R
1
to R
3
is an aliphatic organic group, provided that at least one of R
1
to R
3
represents a carbon-carbon unsaturated bond-containing aliphatic organic group.
In the formula (II), each of R
4
and R
5
represents an alkyl group, a cycloalkyl group, or an aryl group, and R
4
and R
5
may be bonded to each other to form a ring structure. m represents 1 or 2; when m is 1, then R
6
represents an aryl group; when m is 2, then R
6
represents an alkylene group, an alkenylene group, or an alkynylene group; and a part of hydrogen atoms of R
4
to R
6
may be substituted with a halogen atom.