77-84-9Relevant articles and documents
Synthesis and evaluation of α,α -disubstituted-3-mercaptopropanoic acids as inhibitors for carboxypeptidase A and implications with respect to enzyme inhibitor design
Lee, Hyun Soo,Kim, Dong H.
, p. 4685 - 4691 (2007/10/03)
2-Ethyl-2-methyl-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.
Imidazopyridazines, their production and use
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, (2008/06/13)
Novel compound of the general formula: STR1 wherein R1 stands for a hydrogen atom, an optionally substituted lower alkyl group or a halogen atom; R2 and R3 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group, provided that either R2 or R3 is a hydrogen atom, the other being an optionally substituted lower alkyl group, or R2 and R3 may, taken together with the adjacent --C=C-- group, form a 5- to 7-membered ring; X stands for an oxygen atom or S(O)p (p stands for an integer from 0 to 2; Y stands for a group of the formula: STR2 (R4 and R5 respectively stand for a hydrogen atom or an optionally substituted lower alkyl group) or a divalent group derived from an optionally substituted 3- to 7-membered homocyclic or heterocyclic ring; R6 and R7 each stands for a hydrogen atom, an optionally substituted lower lakyl group, an optionally substituted cycloalkyl group or an optionally substituted aryl group, or R6 and R7 may, taken together with the adjacent nitrogen atom, form an optionally substituted nitrogen-containing heterocyclic group; m stands for an integer from 0 to 4; and n stands for an integer from 0 to 4, or a salt thereof, which has excellent anti-PAF activities, and is of value as an antiasthmatic agent, and their production, intermediates and pharmaceutical compositions.
2,2-disubstituted glycerol and glycerol-like compounds, compositions and methods of use
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, (2008/06/13)
Novel 2,2-disubstituted glycerol-like compounds are disclosed for use as anti-allergic and anti-inflammatory compounds. The compounds are antagonists of platelet activating factor ("PAF"). Also disclosed are methods of synthesizing and using the compounds of the invention as well as pharmaceutical compositions thereof. The compounds have the formula STR1 wherein R1, R2, R3, and R4 are as defined in the specification.