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Guida Pratica al riconoscimento delle sostanze iscritte nella X edizione della Farmacopea ufficiale della Repubblica Italiana
No full textGuida pratica al riconoscimento delle sostanze iscritte nella V edizione della Farmacopea Europea
No full textPreparation of 4-spiroheterocyclic 2,2-dimethylchromanes as activators of ATP-sensitive potassium (KATP) channels
No full textINHIBITORS OF ZINC PROTEASES THIOARYL SUBSTITUTED AND THEIR USE
No full textTitle 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
Is the conformation of the thiazolidine ring of penicillins of any importance for their antibacterial activity?
No full textCrystal and molecular structure of p-methoxybenzyl 2alpha-methyl-2beta-[(R)-acetoxy(methoxy)methyl]-6beta -phenoxyacetamidopenam-3alpha-carboxylate
No full textArylsulfonamide derivatives as metalloproteases inhibitors and their preparation, pharmaceutical compositions and use in the treatment of degenerative disorders
No full textThe invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R 1 , R 2 , R 3 , R 4 , R 5 , n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders
Crystal and molecular structure of (3R)-3-(3-methyl-7-phenoxyacetamido-3-cephem-4-yl)-3-hydroxybutanoic acid
No full textCompounds having aryl-sulphonamidic structure useful as metalloproteases inhibitors
No full textThe invention relates to arylsulfonamide derivs. of formula I, which endowed with inhibitory activity against
metalloproteases (MMP). The invention also refers to the process for their prepn., to pharmaceutical compns.
comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders. Compds.
of formula I wherein R is -Ar-X-Ar1; Ar is (un)substituted arylene and (un)substituted aryl; Ar1 is H, (un)substituted
arylene and (un)substituted aryl; X is a single bond, (un)branched C1-4 alkylene, O, S, SO2, CO, NH and derivs., NHCO
and derivs. and CONH and derivs.; R1 is OH and derivs.; R2 and R3 are independently H and (un)substituted
(un)branched C1-4 alkyl; R4 is H, CORc, COORc, SO2Rc, CONHRc and SO2NHRc; Rc is C3-6 cycloalkyl, (un)branched
alkyl, aryl, arylalkyl, alkylaryl, 5- to 6-membered heterocyclyl, etc.; R5 is H; R4R5 may taken together with nitrogen atom
attached to form (un)substituted benzo(un)condensed 4- to 6-membered heterocyclyl; n is 1-2; A is (CH2)m; m is 1-6;
provided that R is biphenyl-4-yl, R1 is iso-Pr, one of R2 and R3 is CONHOH and the other one of R2 and R3 is H, R5 is
H, m and n are both 2, then R4 is not H and benzyloxycarbonyl; and their pharmaceutically acceptable salts thereof, are
claimed. Example compd. II was prepd. by a multi-step procedure (procedure given). All the invention compds. were
evaluated for their metalloproteases inhibitory activity. From the assay, it was detd. that II exhibited IC50 value of
0.13±0.03 nM against MMP-2
Crystal and molecular structure of 4-acetyl-3-methyl-7beta-phenoxyacetamido-delta3-cephem
No full text- …
