Preparation of arylsulfonamide-based matrix metalloprotease inhibitors.

Abstract

The present invention provides a compd. I [R1 = (un)substituted (hetero)aryl, heterocycloalkyl; R2, R3 = H or alkyl; X = H, NH2, CN, etc.] which is inhibitor of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-2, and/or MMP-8, and/or MMP-9, and/or MMP-12 and/or MMP- 13. Thus, reacting 3-chlorosulfonylbenzoyl chloride with anisole followed by treating 3-(4-methoxybenzoyl)benzenesulfonyl chloride with ammonia afforded the sulfonamide II which showed IC50 of 1.92 μM and of 2.49 μM against MMP2 and MMP13, resp. The present invention also provides a pharmaceutical compns. comprising compd. I, alone or in combination with other therapeutic agent. [on SciFinder(R)]