13578-57-9Relevant 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.
Synthesis and Biological Activity of 2-Aminothiazolines and 2-Mercaptothiazolines as Octopaminergic Agonists
Hirashima, Akinori,Yoshii, Yutuka,Eto, Morifusa
, p. 2537 - 2546 (2007/10/02)
2-Aminothiazoline derivatives were synthesized by both hydrochloric acid-catalyzed cyclization of thiourea and cyclization of β-aminoalkyl hydrogen sulfate with isothiocyanate in the presence of sodium hydroxide.Substituted 2-mercaptothiazoline derivatives were prepared by alkylation or acylation of the sodium salt of 2-mercaptothiazoline, which was obtained from β-aminoalkyl hydrogen sulfate with carbon disulfide. 2-(4-Chloro-o-toluidino)-2-thiazoline (III-16) was 33percent as effective as octopamine at 100 μM in stimulating adenylate cyclase of Periplaneta americana ventral-nerve-cord homogenates.Its activity was nonadditive to the activity of octopamine.Stimulation of nerve-cord adenylate cyclase activity by III-16 was inhibited by several antagonists, including mianserin, cyproheptadine, chlorpromazine and gramine.The rank-order ability of these antagonists to block the activation by III-16 was identical to the rank-order ability of the same antagonists to block enzyme activation of octopamine.The β-adrenergic antagonist propanolol was less potent.These data suggest that III-16 is a potent and selctive agonist of octopamine-activated adenylate cyclase.Aminothiazolines which activated adenylate cyclase by 10-87percent relative to octopamine also had acaricidal activity at 300 ppm, indicating a correlation between the in vitro octopaminergic-agonist activity and in vivo acaricidal activity of aminothiazolines.
Aminothiazines et aminothiazoles analogues ouverts du levamisole: synthese et approche du mode d'action nematicide
Caujolle, Raymond,Amarouch, Hamid,Payard, Marc,Loiseau, Philippe R.,Bories, Christian,et al.
, p. 287 - 292 (2007/10/02)
New compounds with thiazoline or dihydrothiazine rings substituted by alkylamino or arylamino groups were synthesized and screened in vitro against three Nematodes.Inhibition of fumarate-reductase activity was also evaluated.For all in vitro anti-parasitic tests, dihydrothiazines were more potent than corresponding thiazolines derivatives, however, thiazolines showed a greater inhibition of fumarate-reductase.
Synthesis of new 'benzyl'-thiourea derivatives and their cyclic analogues with diuretic and saluretic activity
Reiter,Toldy,Schafer,et al.
, p. 41 - 53 (2007/10/02)
A series of new 'benzyl'-thiourea derivatives 2 and their cyclic analogues 3 were synthesized and tested for diuretic activity. The structure-activity relationships - being also computed - are discussed. Some selected compounds were studied in detail for
