89781-55-5Relevant articles and documents
N-Imidazolyl derivatives of the naphthalene and chroman rings as thromboxane A2 synthase inhibitors
Cozzi, P,Branzoli, U,Carganico, G,Ferti, C,Pillan, A,et al.
, p. 423 - 433 (2007/10/02)
A series of N-imidazol-1-yl derivatives of 1,2-dihydronaphthalene, 1,2,3,4-tetrahydronaphthalene, 2H-1-benzopyran and some related compounds were synthesized and tested as inhibitors of thromboxane A2 synthase in ex vivo experiments with orally treated rats.Some compounds showed good activity which was confirmed in experiments in vitro in rabbit whole blood.Some structural requirements for significant TxA2 synthase inhibitory activity are discussed.The selected 5,6-dihydro-7-(1H-imidazol-1-yl)-2-naphthalene-carboxylic acid (compound 7) was conformationally analysed using the Sybyl molecular model system in comparison with dazoxiben.Compound 7 was further pharmacologically investigated and on the basis of its interesting activities in vitro, ex vivo and in vivo and its low toxicity was selected for clinical investigation.
N-imidazolyl derivatives of bicyclic compounds and pharmaceutical compositions containing the same
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, (2008/06/13)
A pharmaceutical compositon having activity against nephropathies comprising, as an active agent, a therapeutically effective amount of a compound of formula (I) STR1 wherein (a) STR2 wherein Y completes a single bond or is oxygen or a --CH2 -- group and the symbol STR3 represents a single bond or (b) STR4 STR5 and the symbol STR6 represents a double bond; one of R1, R2, R3 and R4 is --CH2 OH, C2 -C4 acyl, STR7 in which each of R1, R8 and R9 is independently hydrogen or C1 -C4 alkyl and the others are independently chosen from hydrogen, hydroxy, halogen, C1 -C4 alkyl, C1 -C4 alkoxy and --COOR, wherein R7 is as defined above, and one of R5 and R6 is hydrogen and the other is hydrogen, C1 -C6 alkyl or phenyl; or a pharmaceutically acceptable salt thereof; and a pharmaceutically acceptable carrier and/or diluent.
N-Imidazolyl derivatives containing naphthalene or indene nucleus
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, (2008/06/13)
Compounds of the formula (I) STR1 wherein the symbol represents a single or a double bond; Z completes a single bond or is a --CH2 -- group; each of R1, R2, R3 and R4, which may be the same or different is (a) hydrogen; hydroxy; halogen; cyano; C1 -C6 alkyl; C1 -C6 alkoxy; a C2 -C4 acyl or C2 -C4 acylamino group; --SR', --N(R') (R"), --CH2 OR', --COR or --CH2 COR, wherein R is OR' or --N(R') (R") and each of R' and R", being the same or different, is hydrogen or C1 -C6 alkyl; or (b) one of R1, R2, R3 and R4 is 5- tetrazolyl or a group selected from --COCH2 OR', --CH=C(R')-COR and --X-C(R') (R")-COR, wherein R, R' and R" are as defined above, and X is --O--, --S--, or --NH--, and the others are as defined above under (a); one of R5 and R6 is hydrogen and the other is hydrogen, C1 -C6 alkyl, C3 -C6 cycloalkyl, or a phenyl or pyridyl ring, wherein the phenyl or pyridyl ring is unsubstituted or substituted by one to three substituents chosen from hydroxy and C1 -C4 alkoxy; or pharmaceutically acceptable salts thereof exhibit pharmaceutical activity as vasodilators or blood platelet aggregation inhibitors. Additionally, these compounds and their pharmaceutically acceptable salts are useful in the treatment of migraine, diabetic microangeopathy, rheumatoid arthritis, hypertension, peptic ulcers, osteoporosis, angina pectoris, atherosclerosis and dislipidaemies.
