Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Article Details
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Sheppard GS, Florjancic AS, Giesler JR, Xu L, Guo Y, Davidsen SK, Marcotte PA, Elmore I, Albert DH, Magoc TJ, Bouska JJ, Goodfellow CL, Morgan DW, Summers JB
Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.
Bioorg Med Chem Lett. 1998 Nov 17;8(22):3251-6.
- PubMed ID
- 9873712 [ View in PubMed]
- Abstract
A series of succinyl hydroxamate MMP inhibitors were prepared incorporating an aryl amino ketone moiety in place of the more typical C-terminal amino acid amides. Compounds of the C-terminal ketone series displayed potent inhibition of MMPs. Several compounds of the series were shown to be orally bioavailable.
DrugBank Data that Cites this Article
- Binding Properties
Drug Target Property Measurement pH Temperature (°C) Marimastat 72 kDa type IV collagenase IC 50 (nM) 0.85 N/A N/A Details Marimastat Interstitial collagenase IC 50 (nM) 1.1 N/A N/A Details Marimastat Matrilysin IC 50 (nM) 11 N/A N/A Details Marimastat Stromelysin-1 IC 50 (nM) 10 N/A N/A Details