27 research outputs found
A New Method for Synthesizing Asymmetric Urea Containing Thiazolo[5,4-b]pyridine And Applications in Agriculture
No full textImproved Synthesis of Cefdinir and Its Polymorphic Form, an Antibacterial Active Pharmaceutical Ingredient
No full textStructure-activity relationships within a series of caspase inhibitors: effect of leaving group modifications
No full textVarious aryloxy methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A systematic study of their structure-activity relationship (SAR) related to caspases 1, 3, 6, and 8 is reported. Highly potent irreversible broad-spectrum caspase inhibitors have been identified. Their efficacy in cellular models of cell death and inflammation are also discussed
Hydrolytic Stability versus Ring Size in Lactams: Implications for the Development of Lactam Antibiotics and Other Serine Protease Inhibitors
No full textIMIDAZOLIDINONES STRUCTURALLY-RELATED TO PENICILLINS: SYNTHESIS, MOLECULAR MODELING AND BIOLOGICAL EVALUATION
No full textStructure-activity relationships within a series of caspase inhibitors. Part 2: Heterocyclic warheads
No full textVarious heterocyclic hetero-methyl ketones of the 1-naphthyloxyacetyl-Val-Asp backbone have been prepared. A study of their structure-activity relationship (SAR) related to caspase-1, -3, -6, and -8 is reported. Their efficacy in a cellular model of cell death is also discussed. Potent broad-spectrum caspase inhibitors have been identified
Acyl dipeptides as reversible caspase inhibitors. Part 2: further optimization
No full textA new structural class of broad spectrum caspase inhibitors was optimized for its activity against caspases 1, 3, 6, 7, and 8. The most potent compound had low nanomolar broad spectrum activity, in particular, single digit nanomolar inhibitory activity against caspase 8
Cross-Coupling of Highly Pyramidalized Alkenes: A Straightforward Access to Functionalized Tetrasecododecahedradienes
No full text
