- Comparison of the effects of 5- and 6-HOAt on model peptide coupling reactions relative to the cases for the 4- and 7-isomers
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(equation presented) Synthesis of 5- and 6-HOAt has completed the full set of the four HOAt isomers derived from HOBt by insertion of a single nitrogen atom in the benzenoid nucleus. Comparison of the reactivity of all four isomers in model peptide coupling reactions has confirmed the unique character of the 7-isomer in promoting selectivity and maintaining configuration at the reactive carboxylic acid residue.
- Carpino, Louis A.,Imazumi, Hideko,Foxman, Bruce M.,Vela, Michael J.,Henklein, Peter,El-Faham, Ayman,Klose, Jana,Bienert, Michael
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p. 2253 - 2256
(2007/10/03)
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- Pyrido[3,4-e]-1,2,4-triazines and related heterocycles as potential antifungal agents
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The preparation and biological activities of a series of pyrido[3,4-e]-1,2,4-triazines, 1,2,4-triazino[5,6-c]quinolines, and related fused triazines are described. Methyl, amino, and acylamino substituents were placed in the pyridyl ring of the former system. Other structural modifications included various alkyl, cycloalkyl, substituted phenyl, and heterocyclic groups in the 3-position of these ring systems. In agar dilution assays, actives in this series inhibited strains of Candida, Aspergillus, Mucor, and Trychophyton species at MIC's of ≤ 16 μg/mL.
- Reich,Fabio,Lee,Kuck,Testa
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p. 2474 - 2485
(2007/10/02)
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