Protease inhibitors: synthesis of bacterial collagenase and matrix metalloproteinase inhibitors incorporating succinyl hydroxamate and iminodiacetic acid hydroxamate moieties |
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Authors: | Santos M Amélia Marques Sérgio Gil Marco Tegoni Matteo Scozzafava Andrea Supuran Claudiu T |
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Institution: | Centro de Química Estrutural, Complexo I, Instituto Superior Técnico, 1049-001 Lisboa, Portugal. |
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Abstract: | A series of succinyl hydroxamates/bishydroxamates as well as a new structural type of matrix metalloproteinase (MMP)/bacterial protease (BP) inhibitors, incorporating iminodiacetic (IDA) hydroxamate/bishydroxamate moieties, has been synthesized and tested for interaction with four vertebrate proteases, MMP-1, MMP-2, MMP-8 and MMP-9, and a BP, the collagenase isolated from Clostridium histolyticum (ChC). The new derivatives generally showed inhibition constants in the range of 8-62 nM against the five proteases mentioned above. |
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