1848-60-8Relevant academic research and scientific papers
Synthesis of thiazol, thiazinan, thiadiazin, thiazolidin, triazine, thioxo-pyrimidin and thioxo-imidazolidine by inter-intra molecular cyclization
Zade, Mangesh N.,Katiya, Manish M.,Deotale, Vinod D.,Sontakke, Madhuri M.,Dhonde, Madhukar G.,Berad, Baliram N.
, p. 1493 - 1500 (2019/05/21)
Syntheses of five and six membered heterocyclic derivatives by the reaction of disubstituted thiocarbamides with interintramolecular cyclizations in catalyst free condition have been reported. The simple product isolation without column, good yields under mild condition, and applicable green matrix are the advantages of present protocol.
COMPOUNDS WHICH POTENTIATE AMPA RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 67-68, (2008/06/13)
Compounds of formula (I), and salts and solvates thereof for use as a medicament are provided: (I) wherein R1, R2, R4, R10, X and Z are defined in the specification. Processes for preparation, pharmaceutical com
Synthesis of N-benzyl- and N-phenyl-2-amino-4,5-dihydrothiazoles and thioureas and evaluation as modulators of the isoforms of nitric oxide synthase
Goodyer, Claire L. M.,Chinje, Edwin C.,Jaffar, Mohammed,Stratford, Ian J.,Threadgill, Michael D.
, p. 4189 - 4206 (2007/10/03)
Inhibition of the isoforms of nitric oxide synthase (NOS) has important applications in therapy of several diseases, including cancer. Using 1400W [N-(3-aminomethylbenzyl)acetamidine], thiocitrulline and N δ-(4,5-dihydrothiazol-2-yl)ornithine as lead compounds, series of N-benzyl- and N-phenyl-2-amino-4,5-dihydrothiazoles and thioureas were designed as inhibitors of NOS. Ring-substituted benzyl and phenyl isothiocyanates were synthesised by condensation of the corresponding amines with thiophosgene and addition of ammonia gave the corresponding thioureas in high yields. The substituted 2-amino-4,5-dihydrothiazoles were approached by two routes. Treatment of simple benzylamines with 2-methylthio-4,5-dihydrothiazole at 180 °C afforded the corresponding 2-benzylamino-4,5-dihydrothiazoles. For less nucleophilic amines and those carrying more thermally labile substituents, the 4,5-dihydrothiazoles were approached by acid-catalysed cyclisation of N-(2-hydroxyethyl)thioureas. This cyclisation was shown to proceed by an SN2-like process. Modest inhibitory activity was shown by most of the thioureas and 4,5-dihydrothiazoles, with N-(3-aminomethylphenyl)thiourea (IC50=13 μM vs rat neuronal NOS and IC50=23 μM vs rat inducible NOS) and 2-(3-aminomethylphenylamino)-4,5-dihydrothiazole (IC50=13 μM vs rat neuronal NOS and IC50=19 μM vs human inducible NOS) being the most potent. Several thioureas and 4,5-dihydrothiazoles were found to stimulate the activity of human inducible NOS in a time-dependent manner.
