457-59-0Relevant academic research and scientific papers
Synthesis and biological activity of novel symmetrical bis-2- phenyliminothiazolidine derivatives
Li, Gang-Yue,Qian, Xu-Hong,Yan, Sheng-Gang,Cui, Jing-Nan,Huang, Qing-Chun,Zhang, Rong,Liu, Feng-Yu,Cui, Da-Wei
, p. 2851 - 2861 (2007/10/03)
A series of novel symmetrical bis-2-phenyliminothiazolidine derivatives were designed and synthesized. The structures of all the title compounds were characterized by 1H NMR and, in some cases, by 13C NMR, IR, and high-resolution mas
Synthesis and fungicidal activity of fluorine-containing phenylimino-thiazolidines derivatives
Xu, Xiaoyong,Qian, Xuhong,Li, Zhong,Song, Gonghua,Chen, Weidong
, p. 297 - 300 (2007/10/03)
Nine new fluorine-containing phenylimino-thiazolidines derivatives were prepared. The structures of all compounds were confirmed by 1H NMR, mass and high resolution mass spectroscopy. The antifungicidal activities of the title compounds on Phytophthoza capsici L., Pyriculazia ozyzae C., Fusazium spp. at 100 ppm were screened.
Synthesis and fungicidal activity of fluorine-containing phenylimino-thiazolidines derivatives
Xu, Xiaoyong,Qian, Xuhong,Li, Zhong,Song, Gonghua,Chen, Weidong
, p. 1159 - 1162 (2007/10/03)
Nine new fluorine-containing phenylimino-thiazolidines derivatives were prepared. The structures of all compounds were confirmed by 1H NMR, mass and high resolution mass spectroscopy. The antifungicidal activities of the title compounds on Phytophthora capsici L., Pyricularia oryzae C, Fusarium spp. at 100 ppm were screened.
Syntheses, structures and bioactivities of fluorine-containing phenylimino-thia(oxa)zolidine derivatives as agricultural bioregulators
Qian, Xuhong,Xu, Xiaoyong,Li, Zhibin,Li, Zhong,Song, Gonghua
, p. 1609 - 1620 (2007/10/03)
From insight into the structure of trehazolin as trehalase inhibitor, six series of fluorine-containing phenylimino-thiazolidines (oxazolidines) derivatives were designed and prepared through a convenient synthesis of fluoroaryl isothiocyanate and a one-pot facile synthesis in high yield of fluorophenyl aminobenzoxazoles by cyclodesulfurization. The structures of the target compounds were confirmed with using IR, NMR, MS and elemental analysis. Their X-ray crystal analysis suggested that there were novel intermolecular (sp2CF?H3C) and intramolecular (sp 2CF?HN) hydrogen bonds between the fluorine atom on benzene ring and hydrogen atom of methyl group or amino group on five-membered heterocycle. Their fungicidal activities against Rhizoctonia solani and Pyricuraria oryzae at 100 ppm were determined. From insight into the structure of trehazolin as trehalase inhibitor, six series of fluorine-containing phenylimino-thiazolidines (oxazolidines) derivatives were designed and prepared through a convenient synthesis of fluoroaryl isothiocyanate and a one-pot facile synthesis in high yield of fluorophenyl aminobenzoxazoles by cyclodesulfurization. The structures of the target compounds were confirmed with using IR, NMR, MS and elemental analysis. Their X-ray crystal analysis suggested that there were novel intermolecular (sp2CF?H 3C) and intramolecular (sp2CF?HN) hydrogen bonds between the fluorine atom on benzene ring and hydrogen atom of methyl group or amino group on five-membered heterocycle. Their fungicidal activities against Rhizoctonia solani and Pyricuraria oryzae at 100 ppm were determined. fx1
Synthesis and QSAR studies in 2-(N-aryl-N-aroyl)amino-4,5-dihydrothiazole derivatives as potential antithrombotic agents
Saxena, Anil K.,Pandey, Suresh K.,Seth,Singh,Dikshit,Carpy
, p. 2025 - 2034 (2007/10/03)
A series of 2-(N-aryl-N-aroyl)amino-4,5-dihydrothiazole derivatives have been synthesized via cyclocondensation of N-aryl thioureas with 2-bromoethylamine hydrobromide followed by the reaction of the product thus obtained with aroyl chlorides. Title compounds were evaluated for their antithrombotic activity in vivo in mice where one of these compound 29 provided 65% protection as compared to 77% protection offered by the standard Indomethacin. Quantitative Structure-Activity Relationship (QSAR) studies were performed on these compounds using physicochemical (hydrophobic, electronic, steric) parameter as independent and antithrombic activity as dependent parameter, where antithrombotic activity correlated best (r > 0.8) with electronic parameters (F, σ or μ) having high statistical significance > 99.9% (F2,22 > 15.0; F2,22α:0.001 = 11.0) suggesting that hydrophobic, steric and resonance factors are insignificant in this set of molecules for the activity.
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.
