124623-44-5Relevant articles and documents
Synthetic Study of the Highly Potent and Selective Anti-platelet Activating Factor Thiazolidin-4-one Agents and related Compounds
Tanabe, Yoo,Yamamoto, Hitomi,Murakami, Masanari,Yanagi, Kazunori,Kubota, Yoshino,et al.
, p. 935 - 948 (2007/10/02)
Stereoselective cyclo-condensation of α-sulfanylcarboxylic acids (or esters) 6 with N-methylarylimines 7 afforded the title compounds, 2-arylthiazolidin-4-ones, some of which exhibit highly potent anti-PAF activity.The reaction without added catalyst gave predominantly cis products, however, when titanium(IV) isopropoxide was added as catalyst trans products were predominantly formed.Allylation of 3-methyl-2-(3-pyridyl)thiazolidin-4-one 22 with allyl bromide using lithium amides gave the trans-5-allyl-2-(3-pyridyl)thiazolidin-4-one 23 with good selectivity.To study the stereostructure-activity relationship, the four optically active isomers of 3,5-dimethyl-2-(3-pyridyl)thiazolidin-4-one 4 and 5-(4-chlorophenyl)-3-methyl-2-(3-pyridyl)thiazolidin-4-one 5 were synthesized.The absolute configurations of compounds 4 and 5 were determined by X-ray analyses and 1H NMR measurements.Epimerization of the 5-position of compounds 4 and 5 was found to be effected by bases with high regioselectivity (>99percent), which was checked by a cross-over experiment using several optically active compounds.
Certain pyridyl-thiazolidin-4-one having anti-ulcer activity
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, (2008/06/13)
A 2-pyridyl-thiazolidin-4-one derivative represented by the formula: STR1 wherein R1 and R2 are each a hydrogen atom, an C1 -C20 alkyl group, an C2 -C20 alkenyl group, an C2 -C20 alkynyl group, an aryl group, a C3 -C8 cycloalkyl group or an aralkyl group which may have a substituent, R3 is a hydrogen atom, an C1 -C20 alkyl group, an C2 -C20 alkenyl group, an C2 -C20 alkynyl group, a C3 -C8 cycloalkyl group or an aralkyl group which may have a substituent, P is a pyridyl group or its N-substituted pyridinium salt which may have a substituent, said substituent being selected from the group consisting of halogen atom, cyano group, hydroxy group, amino group, lower alkyl group, lower alkoxy group, lower alkylamino group, halogenated lower alkyl group, acyl group, acyloxy group, acylthio group, acylamino group, carboxyl group, lower alkoxycarbonyl group, carbamoyl group, lower alkyl substituted carbamoyl group, heterocyclic group, and lower cycloalkyl group, and n represents an integer of 0, 1 or 2, or a pharmaceutically acceptable salts thereof and an anti-ulcer agent which contains, as an effective ingredient, said 2-pyridyl-thiazolidine-4-one derivative or a pharmaceutically acceptable salt thereof.
Novel thiazolidin-4-one derivatives and acid addition salts therof
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, (2008/06/13)
A novel 2-pyridylthiazolidin-4-one derivative represented by the general formula STR1 wherein Ar denotes an aryl group unsubstituted or substituted with a halogen atom or with a lower alkoxy group; X denotes a straight-chain or branched-chain lower alkylene group or a single bond; R denotes a hydrogen atom, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, acyloxy, di(lower alkyl) amino, hydroxyl or aryl group, or denotes an aryl group substituted with a lower alkoxy group; and Py denotes a pyridyl group, and the acid addition salt thereof, which have an excellent platelet activating factor antagonsm.
