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At least 739 records · Page 41Linked to original sources
PubMed1980

Co-oxidative metabolism of 2-amino-4-(5-nitro-2-furyl)-thiazole by prostaglandin hydroperoxidase.

Co-oxidative metabolism of ANFT by either the fatty acid cyclo-oxygenase or hydroperoxidase activities of prostaglandin endoperoxide synthetase was examined by using solubilized and particulate microsomes prepared from rabbit renal inner medulla and ram seminal vesicles. The rate of metabolism was measured by the decrease in absorbance at 385 nm. In both soluble and particulate preparations, ANFT metabolism was dependent upon specific fatty acid substrates and prevented by specific inhibitors of prostaglandin endoperoxide synthetase. Other inhibitor and substrate specificity studies suggest that ANFT was not metabolized by xanthine oxidase, lipoxygenase, lipid peroxidation, or mixed-function oxidases. Under incubation conditions which demonstrated co-oxidation of ANFT, a metabolite (peak I) was observed by high-pressure liquid chromatography. In the presence of indomethacin, peak I was not present, and only authentic ANFT was observed. Co-oxidation of ANFT was also observed with cumene hydroperoxide. Cumene hydroperoxide-mediated co-oxidation was not prevented by indomethacin or SKF-525A but was blocked by the antioxidants butylated hydroxytoluene, ethoxyquin, and vitamin E. The data indicate that ANFT is metabolized by a co-oxidative process involving the prostaglandin hydroperoxidase activity of prostaglandin endoperoxide synthetase.

Animals↗
PubMedDate not supplied

[Interaction of DNA with actinocyl-bis-thiazole].

The DNA complexes with actinocyl-bis-bithiazole have been investigated by spectrophotometry, viscometry and flow birefringence. It was estimated, that at low degrees of binding (r < or = 0.07) this compound binds to DNA by bisintercalation via bithiazole groups located in positions 1 and 9 of the phenoxazone chromophore. The phenoxazone moiety plays in this case the role of a link connecting two intercalating fragments. As r increases, external groove binding becomes the second type of complex formation.

DNA↗
PubMed1997

Synthesis and antimicrobial screening of some novel thiazoles, dithiazoles and thiazolylpyridines.

Several thiazolines 2a-c, and 4-thiazolidinones 3a-c were synthesized through the reaction of the cyanoacetic acid hydrazide derivatives 1a-c with phenacyl bromides or chloroacetic acid, respectively. The dithiazoles 4a, b were obtained from 2a, b through their reaction with sulphur and phenyl isothiocyanate. The dithiazoles 6a, b were prepared from 4a through its reaction with dimethyl sulphate followed by reaction of the produced 2-methylthiothiazolium salt 5 with either malononitrile or ethyl cyanoacetate. The thiazolyl-pyridines 7a, b and 8a, b were obtained from 2a, b through their reaction with arylidene malonitrile and arylidene ethyl cyanoacetate, respectively. The prepared compounds were screened for their antibacterial and antifungal activities in vitro. Some of them showed weak effects.

Anti-Bacterial Agents↗
PubMed1979

[Pharmacological properties of dl-2-(3'-t-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl) thiazole hydrochloride (S-596), a new beta-adrenergic blocking agent (author's transl)].

We developed a new beta-adrenergic blocking, antiarrhythmic compound S-596 and compared the findings with those of propranolol or practolol. S-596 antagonized the positive chronotropic and inotropic actions of adrenaline in isolated guinea-pig atria, and blocked the relaxant response to adrenaline of isolated guinea pig tracheal strips. In anesthetized mongrel dogs, S-596 given intravenously inhibited increases in heart rate and myocardial contractile force and decreases in systemic blood pressure induced by isoproterenol. In conscious dogs, the oral administration of S-596 reduced the isoproterenol induced tachycardia and the maximal effect was attained one hour after administration. In this regard S-596 was about 5 times more potent than propranolol, and S-596 was significantly longer-acting than propranolol. Thus, S-596 has greater beta-blocking activity than propranolol. S-596 has a lesser degree of myocardial depressant action than propranolol in spontaneously contracting rat or guinea pig atria and no intrinsic sympathomimetic activity in reserpinized rats. S-596 also has a weaker local anesthetic and antiarrhythmic activity than propranolol, as determined in guinea pigs and rabbits.

Adrenergic beta-Antagonists↗
PubMed2005

Inhibitors of type I MetAPs containing pyridine-2-carboxylic acid thiazol-2-ylamide. Part 2: SAR studies on the pyridine ring 3-substituent.

Systematic SAR studies on the pyridine ring 3-substituent of PCAT, an inhibitor of EcMetAP1 and ScMetAP1, revealed that 3-substituents have different selectivity for EcMetAP1 and ScMetAP1. The selective inhibitors of type I MetAP are useful tools for investigating the detailed interactions between the enzymes and their inhibitors. In addition, these findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.

Aminopeptidases↗
PubMed1991

Synthesis and anthelmintic activity of 3'-benzoylurea derivatives of 6-phenyl-2,3,5,6-tetrahydroimidazo[2,1-b]thiazole.

Reaction of 3-amino derivatives of the nematocides tetramisole and levamisole with variously substituted benzoylisocyanates gave a series of benzoylureas I which were tested for activity against helminths and ectoparasites. Compounds bearing 2,6-difluoro and 4-trifluoromethyl substituents had potent nematocidal activity in both mice and sheep. No antiectoparasitic activity was observed.

Animals↗