Aryl ketones as novel replacements for the C-terminal amide bond of succinyl hydroxamate MMP inhibitors.

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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

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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