A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine p...A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine protease of T.cruzi..展开更多
BACKGROUND： Porphyromonas gingivalis is a periodontal pathogen, which is considered to be a keystone pathogen for periodontitis. A diverse conglomerate of P. gingivalis virulence factors including lipopolysaccharide,...BACKGROUND： Porphyromonas gingivalis is a periodontal pathogen, which is considered to be a keystone pathogen for periodontitis. A diverse conglomerate of P. gingivalis virulence factors including lipopolysaccharide, fimbriae, capsular polysaccharide, haemagglutinin and cysteine proteases （Arg-gingipains and Lys-gingipain） are considered to be involved in the pathogenesis ofperiodontitis. Leupeptin is a cysteine protease inhibitor which is specific for Arg gingipains. The present review focuses on action of leupeptin on Arg gingipains. METHOD： A search was carried out systematically from the start till September, 2016. The search was made in Medline database via PubMed. The keywords enlisted were ＂leupeptin＂; ＂gingipains＂; ＂periodontitis＂ using Boolean operator ＂and.＂ RESULTS： The result was selection of 58 articles which linked leupeptin to periodontitis and gingipains; pathogenesis of periodontitis, pathogenicity of gingipains and role of leupeptin. CONCLUSION： It was concluded that leupeptin inhibits and attenuates a number of destructive activities of Arg gingipains including inhibition ofplatelet aggregation; inhibit degradation of LL-37, which is an antimicrobial peptide; blocking inhibition ofmonocyte chemoattractant protein; restoring level ofinterleukin-2; inhibiting degradation of collagen type I and IV to name a few.展开更多
文摘A series of N1-substituted-3-aryl-4-alkyl-4, 5-dihydro-1H-1-pyrazolethiocarboxamide were prepared from the Mannich bases of aryl ketones in good yields. Some derivatives were found to be active against the cysteine protease of T.cruzi..
文摘BACKGROUND： Porphyromonas gingivalis is a periodontal pathogen, which is considered to be a keystone pathogen for periodontitis. A diverse conglomerate of P. gingivalis virulence factors including lipopolysaccharide, fimbriae, capsular polysaccharide, haemagglutinin and cysteine proteases （Arg-gingipains and Lys-gingipain） are considered to be involved in the pathogenesis ofperiodontitis. Leupeptin is a cysteine protease inhibitor which is specific for Arg gingipains. The present review focuses on action of leupeptin on Arg gingipains. METHOD： A search was carried out systematically from the start till September, 2016. The search was made in Medline database via PubMed. The keywords enlisted were ＂leupeptin＂; ＂gingipains＂; ＂periodontitis＂ using Boolean operator ＂and.＂ RESULTS： The result was selection of 58 articles which linked leupeptin to periodontitis and gingipains; pathogenesis of periodontitis, pathogenicity of gingipains and role of leupeptin. CONCLUSION： It was concluded that leupeptin inhibits and attenuates a number of destructive activities of Arg gingipains including inhibition ofplatelet aggregation; inhibit degradation of LL-37, which is an antimicrobial peptide; blocking inhibition ofmonocyte chemoattractant protein; restoring level ofinterleukin-2; inhibiting degradation of collagen type I and IV to name a few.
