- Novel (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones as potent antimicrobial agents
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New (E)-1-(4-methyl-2-(alkylamino)thiazol-5-yl)-3-arylprop-2-en-1-ones, unsubstituted or carrying fluoro, bromo, methoxy, nitro, methyl and chloro groups on the benzene ring, were synthesized and assayed in vitro for their antimicrobial activity against Gram positive and Gram negative bacteria and fungi. The compounds were very potent towards all tested microorganisms and in most cases their activity was better than that of reference drugs.
- Liaras,Geronikaki,Glamo?lija,?iri?,Sokovi?
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experimental part
p. 7349 - 7356
(2012/01/03)
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- Synthesis and antithyroid activity of 1,4,5-trialkyl 2-thioimidazole derivatives
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A series of compounds based on the structure of MTI (1-methyl-2-thioimidazole) were synthesized by condensation of α-hydroxyketones and alkylthioureas. The α-hydroxyketones were obtained by a radical reaction in the presence of sodium and the alkyl ester, while the alkylthioureas were prepared by nucleophilic addition of ammonia on an alkylisothiocyanate. The antithyroid activity of the 13 compounds prepared was evaluated in vitro by determination of the concentrations which led to a 50% inhibition (IC50) of the activity of thyroid peroxidase, and in vivo by assay of thyroid hormones levels and histological examination of the thyroid gland in rats treated chronically with the compounds. 1-methyl-4,5-dipropyl 2-thioimidazole (compound 10) was found to have the highest antithyroid activity of the 13 compounds synthesized.
- Fatimi,Lagorce,Chabernaud,Comby,Buxeraud,Raby
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p. 253 - 257
(2007/10/02)
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- Synthesis and inhibitory effects of 1,4,5-trialkyl-2-thioimidazole derivatives on platelet aggregation
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New 1,4,5-trialkyl-2-thioimidazole have been synthesized by the condensation of α-hydroxyketones and alkylthioureas. The in vitro platelet aggregation inhibiting effect of prepared compounds on human platelets was studied in the presence of ADP and collagen as inducers. The formation of thromboxane B2 (TXB2) was inhibited. 1-isopropyl-4,5-dimethyl-2-thioimidazole has the greatest aggregation inhibiting effect, about 4 times that of aspirin. It highly inhibits the production of TXB2 (68,5% for a final concentration of 0,04 M).
- Fatimi,Lagorce,Chabernaud,Buxeraud,Raby
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p. 151 - 155
(2007/10/02)
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- Acyl amidine and acyl, guanidine substituted biphenyl derivatives
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Novel compounds are disclosed having the formula STR1 and wherein R1, R2 and R3 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
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- Reduction of 1,2,4-thiadiazol-3-yl-thioureas: Formation of 1,3,5-triazine-2-thiones, 2,4-dithiones and amidinothioureas
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Reduction of thiadiazol-3-yl-thioureas (I) in alcoholic ammoniacal hydrogen sulphide furnish 1,3,5-triazine-2-thiones (III), 2,4-dithiones (VI) and/or amidinothioureas (VII) depending upon the substituents in I.
- Joshua, C. P.,Sujatha, T. S.
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p. 330 - 334
(2007/10/02)
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- A Mild and Efficient Method for the Preparation of Guanidines
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A mild and efficient method for the preparation of guanidines by reaction of an acylated thiourea with an amine followed by removal of the acyl groups(s) from the intermediate acylguanidine is reported.Key Words: acylguanidine, acylthiourea, guanidine, water soluble carbodiimide
- Poss, Michael A.,Iwanowicz, Edwin,Reid, Joyce A.,Lin, James,Gu, Zhengxiang
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p. 5933 - 5936
(2007/10/02)
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