Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
通式I的酚酸酯化合物##STR1##可用于预防、治疗或缓解弹性蛋白酶介导的疾病或症状。
(Acyloxy)benzophenones and (acyloxy)-4-pyrones. A new class of inhibitors of human neutrophil elastase
作者:Masateru Miyano、James R. Deason、Akira Nakao、Michael A. Stealey、Clara I. Villamil、Daniel D. Sohn、Richard A. Mueller
DOI:10.1021/jm00400a030
日期:1988.5
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-[(acyloxy)methyl]-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.
Mechano-isomerization of azobenzene
作者:Sravan K. Surampudi、Harik R. Patel、G. Nagarjuna、D. Venkataraman
DOI:10.1039/c3cc43797c
日期:——
We show that ultrasound-induced mechanical force isomerizes an azobenzene centered within a poly(methyl acrylate) polymer from cis to trans configuration without cleaving the azo bond. The isomerization rate was not altered by the polarity of the solvent indicating that the isomerization occurs through a non-polar, inversion transition state.