73720-57-7Relevant academic research and scientific papers
(Acyloxy)benzophenones and (Acyloxy)-4-pyrones. A New Class of Inhibitors of Human Neutrophil Elastase
Miyano, Masateru,Deason, James R.,Nakao, Akira,Stealey, Michael A.,Villamil, Clara I.,et al.
, p. 1052 - 1061 (2007/10/02)
A series of 4-(acyloxy)- and 4,4'-bis(acyloxy)benzophenones were synthesized.Some of them, pivalates (trimethylacetates) and isobutyrates in particular, were found to be potent and selective inhibitors of human neutrophil (leukocyte) elastase.A series of 2--5-(acyloxy)-4-pyrones were synthesized regioselectively from kojic acid.The 4-pyrones bearing a long chain acyl group at the 2-position and either pivaloyloxy or isobutyryloxy at the 5-position were potent and selective inhibitors of the human elastase.A number of analogues and derivatives in both series were synthesized in order to study the structure-activity relationship as summarized in Tables I-VI and in Tables IX and X.The inhibition was selective to human neutrophil elastase.No inhibition of porcine pancreatic elastase or bovine pancreatic chymotrypsin (Tables VII and XI) was observed.The most likely mechanism of inhibition is discussed.The implication of these findings for the treatment of rheumatoid arthritis and emphysema is outlined.
Arylacetic acid derivatives
-
, (2008/06/13)
Arylacetic acid derivatives of the formula STR1 with R1, R2 and R3 specifically defined and which are useful as antirheumatic and antiinflammatory pharmaceuticals are practiced by catalytic hydrogenation of new compounds of the formula STR2 in which R and R10 are also specifically defined. The method of making the latter compound is also set forth.
