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EnglishTitle compds. I [X1 = S(O)q; R1 and R2 independently = H, (un)substituted alkyl, aryl, etc., or R1 and R2 are linked to form carbocyclic or heterocyclic ring; X = O or S, or divalent group selected from disulfide, disulfoxide, sulfone, amino, etc.; E = alkyl, alkenyl, alkynyl or (un)substituted carbocyclic or heterocyclic ring, optionally benzocondensed; Z = chelating moiety; m = 0 or 1; n = 0 or 1; q = 0-2], and their pharmaceutically acceptable salts thereof, are prepd. and disclosed as inhibitors of zinc metalloproteinases. Thus, e.g., II was prepd. by substitution of o-iodobenzoic acid with 4- methoxythiophenol. Data for inhibition activity of representative compds. towards select proteases were provided, e.g., 2-(2-biphenyl-4-ylthio)phenylacetic acid possessed IC50 values of 334±5.7, 0.33±0.026, and 6.7±0.3 (mM) toward MMP- 1, MMP-2, and MMP-9, resp.
| Titolo: | INHIBITORS OF ZINC PROTEASES THIOARYL SUBSTITUTED AND THEIR USE | |
| Autori interni: | ||
| Anno di deposito: | 2008 | |
| Abstract: | Title compds. I [X1 = S(O)q; R1 and R2 independently = H, (un)substituted alkyl, aryl, etc., or R1 and R2 are linked to form carbocyclic or heterocyclic ring; X = O or S, or divalent group selected from disulfide, disulfoxide, sulfone, amino, etc.; E = alkyl, alkenyl, alkynyl or (un)substituted carbocyclic or heterocyclic ring, optionally benzocondensed; Z = chelating moiety; m = 0 or 1; n = 0 or 1; q = 0-2], and their pharmaceutically acceptable salts thereof, are prepd. and disclosed as inhibitors of zinc metalloproteinases. Thus, e.g., II was prepd. by substitution of o-iodobenzoic acid with 4- methoxythiophenol. Data for inhibition activity of representative compds. towards select proteases were provided, e.g., 2-(2-biphenyl-4-ylthio)phenylacetic acid possessed IC50 values of 334±5.7, 0.33±0.026, and 6.7±0.3 (mM) toward MMP- 1, MMP-2, and MMP-9, resp. | |
| Handle: | http://hdl.handle.net/11568/116517 | |
| Appare nelle tipologie: | 6.1 Brevetto |
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