- Synthesis, characterization, and biological evaluation of some novel pyrazolo[5,1-b]thiazole derivatives as potential antimicrobial and anticancer agents
-
The pharmacological activities of thiazole and pyrazole moieties as antimicrobial and anticancer agents have been thoroughly described in many literature reviews. In this study, a convenient synthesis of novel pyrazolo[5,1-b]thiazole-based heterocycles was carried out. The synthesized compounds were characterized by IR,1H and13C NMR spectroscopy and mass spectrometry. Some selected examples were screened and evaluated for their antimicrobial and anticancer activities and showed promising results. These products could serve as leading compounds in the future design of new drug molecules.
- Al-Aizari, Faiz A.,Almarhoon, Zainab M.,Alsayari, Abdulrhman,Asiri, Yahya I.,Ghabbour, Hazem A.,Kheder, Nabila A.,Mabkhot, Yahia N.,Muhsinah, Abdullatif Bin
-
-
- An Fe3O4@SiO2/Schiff base/Cu(ii) complex as an efficient recyclable magnetic nanocatalyst for selective mono: N-arylation of primary O-alkyl thiocarbamates and primary O-alkyl carbamates with aryl halides and arylboronic acids
-
An efficient, convenient and novel method for the selective mono N-arylation of primary O-alkyl thiocarbamates and primary O-alkyl carbamates with aryl halides and arylboronic acids in the presence of a recyclable magnetic Cu(ii) nanocatalyst is described. A variety of mono N-arylated O-alkyl thiocarbamates and O-alkyl carbamates were prepared in good to excellent yields with a broad range of aryl coupling partners. The magnetic nanocatalyst can be easily recovered with an external magnetic field and reused at least five times without noticeable leaching or loss of its catalytic activity. This cost-effective and eco-friendly methodology has some other advantages, such as easy preparation of the catalyst, simple workup procedure, and easy purification, which makes this protocol interesting for the users in various fields of pharmacology and biotechnology systems.
- Sardarian, Ali Reza,Dindarloo Inaloo, Iman,Zangiabadi, Milad
-
p. 8557 - 8565
(2019/06/14)
-
- A comparative study of glycosyl thioimidates as building blocks for chemical glycosylation
-
Our results indicate that the reactivity and the activation profile of thioimidate glycosyl donors vary significantly depending on the endocyclic heteroatom (N,O,S). Reactivity diminishes in accordance with the following sequence: O > S > N; and this tren
- Ranade, Sneha C.,Hasty, Scott J.,Demchenko, Alexei V.
-
p. 360 - 379
(2013/10/08)
-
- Syntheses of N-alkyl, A,N-dialkyl, and N-(4-substituted phenyl) O-ethyl thioncarbamates: A kinetic study
-
The kinetics of the syntheses of N-alkyl, N,N-dialkyl, and N-(4-substituted phenyl) O-ethyl thioncarbamates from sodium ethyl xanthogenacetate, ten alkylamines, and eight substituted anilines were studied at 25, 30, 35, and 40 °C. The reactions were found to follow second-order kinetics. The kinetic (Arrhenius) parameters, such as the activation energy and the frequency factor, as well as the Eyring parameters, such as the standard entropy, the standard Gibbs energy, and the standard enthalpy of activation, were calculated from the second-order rate constants. The mechanism of the reaction was postulated based on the kinetic studies presented and the optimization of the reaction mechanism using the MOPAC PM6 semi-empirical method.
- Milosavljevic, Milutin M.,Marinkovic, Aleksandar D.,Veljkovic, Vlada B.,Milenkovic, Dragan D.
-
experimental part
p. 43 - 49
(2012/07/13)
-
- A one-pot conversion of di-substituted thiourea to O-organyl arylthiocarbamate using FeCl3
-
Unsymmetrical thiourea, which on demand can generate isothiocyanate in the presence of FeCl3, can serve as a latent isothiocyanate functionality and circumvent the difficulties associated with the direct use of reactive isothiocyanate functiona
- Sahoo, Santosh K.,Chakraborty, Supratim,Patel, Bhisma K.
-
experimental part
p. 143 - 153
(2012/06/01)
-
- Effect of successive increase in alcohol chains on reaction with isocyanates and isothiocyanates
-
The reaction of isocyanates and isothiocyanates with long-chain alcohols, e.g. n-hexanol, n-heptanol and n-octanol, exclusively gave N-aryl-O-alkyl carbamates, while N-aryl-O-alkyl carbamates were formed along with symmetrical 1,3-disubstituted ureas and thioureas when the same reactions were carried out with small-chain alcohols at room temperature without using any solvent.
- Perveen, Shahnaz,Yasmin, Arfa,Khan, Khalid Mohammed
-
experimental part
p. 18 - 23
(2010/04/23)
-
- Expeditious routes to 4-alkoxyquinazoline-2-carbonitriles and thiocarbamates via N-arylimino-1,2,3-dithiazoles using microwave irradiation
-
Conversion of N-arylimino-4-chloro-5H-1,2,3-dithiazole 11 into the 4- alkoxyquinazoline-2-carbonitriles 13a-i and of the aryl isothiocyanates 15 into aryl thiocarbamates 16a-j with sodium alkoxides in the corresponding alcohol, either by conventional ther
- Besson, Thierry,Dozias, Marie-Joelle,Guillard, Jerome,Jacquault, Patrick,Legoy, Marie-Dominique,Rees, Charles W.
-
p. 6475 - 6484
(2007/10/03)
-
- Kinetics and mechanism of the aminolysis of O-ethyl S-aryl dithiocarbonates in acetonitrile
-
The aminolysis reactions of O-ethyl S-(Z-phenyl) dithiocarbonates (Z = p-CH3, H, p-Cl, and p-NO2) with anilines (AN) and N,N-dimethylanilines (DMA) in acetonitrile at 30.0 °C are investigated. Relatively small values of βx (βnuc, 0.4 ca. 0.7) and βz (βlg-0.1 ca. -0.4) for both ANs and DMAs, significantly large kH/kD values (1.1 ca. 1.9) involving deuterated anilines, and large negative ρxz values for ANs (-0.56) are interpreted to indicate a concerted mechanism for both ANs and DMAs but with a hydrogen bonded four-center type transition state (TS) for ANs. The relative leaving ability, k(Z = p-NO2)/k(Z = p-CH3), is smaller for ANs than for DMAs, especially for a weaker nucleophile (1.9 and 4.7 for AN and DMA, respectively, with X = p-Cl). This suggests that the rate enhancement by the hydrogen-bond formation in the four-center type TS for AN is greater for a weaker nucleofuge (Z = p-CH3), especially when the nucleophile (X = p-Cl) is weaker.
- Oh,Lee,Yun,Park,Lee
-
p. 419 - 423
(2007/10/03)
-
- Ethanolysis of thioureas
-
In a study on the ethanolysis of thioureas it is demonstrated that N,N'-di- and trisubstituted aryl- and alkylarylthioureas when heated in ethanolic solution undergo fission to give N-arylthiocarbamic acid O-ethyl esters and amines. The reaction rates are depending on the nature of the substituents on the phenyl rings. Generally, the reactions are promoted by mineral acid.
- Derume, Anita,Egg, Helmut,Koenig, Roman
-
p. 327 - 333
(2007/10/03)
-
- 5-Substituted 2,3-dihydro-6-mercapto-1,3-diphenyl-2-thioxo-4(3H)-pyrimidinones and their 6-(acylthio) derivatives with platelet antiaggregating, antiinflammatory, antiarrhythmic, antihyperlipidemic and other activities
-
The synthesis in excellent yields of 2,3-dihydro-6-mercapto-1,3,5-triphenyl-2-thioxo-4(3H)-pyrimidinone 3 and 5-ethoxycarbonyl-2,3-dihydro-6-mercapto-1,3-diphenyl-2-thioxo-4(3H)-py rimidinone 4 by reaction of methyl phenylacetate or diethyl malonate, resp
- Ranise,Bruno,Bondavalli,Schenone,D'Amico,Falciani,Filippelli,Rossi
-
p. 551 - 558
(2007/10/02)
-
- Triorganophosphinegold(I) Carbonimidothioates
-
The title compounds, R3PAuSC(=NPh)OR', R = Et, Ph or Cy and R' = Me, Et, Pr, Pri or Cy, have been prepared and characterized by spectroscopic methods (i.r., 1H and 13C n.m.r. and f.a.b. m.s.) and, in the case of the R = Ph and R'= Me compound,
- Hall, Veronica J.,Siasios, George,Tiekink, Edward R. T.
-
p. 561 - 570
(2007/10/02)
-
- Reformatsky reaction on thiocarbonyl compounds: New C-C bond forming reaction
-
Reformatsky regants are shown to undergo facile C-C bond formation on trithiocarbonates, xanthates, thione and dithioesters, through carbophilic additional yielding products formed by elimination of either sulphur or alkylthio group.
- Chandrasekharam,Bhat, Laxminaraya,Ila, Hiriyakkanavar,Junjappa, Hiriyakkanavar
-
p. 6439 - 6442
(2007/10/02)
-
- INTERACTION BETWEEN PHENYLMETHANEPHOSPHONIC ACID DIETHYL ESTER AND ISOTHIOCYANATES
-
Diethyl esters of 1-N-substituted thioamido-phenylmethanephosphonic acids are obtained from O,O-diethyl phenylmethanephosphonate, sodium amide as a metallation agent and alkyl- or arylisothiocyanates.It is established that parallel reactions also occur, resulting in the formation of the respective 1,3-disubstituted thioureas and O-ethylthiocarbamates.These represent the main reaction products in the cases when ethanephosphonic acid diethyl ester is used as a starting reagent.
- Lachkova, Victoria,Petrov, Galin
-
p. 227 - 233
(2007/10/02)
-
- KINETIC ANALYSIS OF COMPETITIVE REACTIONS OF ISOTHIOCYANATES WITH HYDROXYL AND ALKOXIDE IONS
-
The reaction of isothiocyanates with hydroxyl and alkoxide ions has been followed spectrophotometrically in alkaline aqueous-alcoholic solutions.Both the nucleophiles are added to the carbon atom of isothiocyanate group in a competition reaction.The effec
- Augustin, Josef,Balaz, Stefan
-
p. 443 - 452
(2007/10/02)
-
- Reactions of Monoprotic Thioureas with Ethyl α-Chloroacetoacetate, Ethyl Bromomalonate, and Ethyl Bromocyanoacetate
-
N,N,-Dialkyl-N'-arylthioureas (1) with ethyl α-chloroacetoacetate, furnished dialkylamine hydrochlorides, aryl isothiocyanates, 2-arylimino-1,3-oxathioles (2), 2-arylimino-3-aryl Δ4-thiazolines (3), diarylthioureas (9), and carbonyl sulphide.With ethyl bromomalonate the products were dialkylamine hydrobromides, aryl isothiocyanates, 2-arylimino-3-arylthiazolidin-4-ones (11), and diarylthioureas (9).Ethyl bromocyanoacetate gave an ethyl cyanothio>acetate (13).Compound (13) with triethylamine gave the starting thiourea (1) and diethyl dicyanofumarate.
- Singh, Harjit,Ahuja, Amarjit S.,Malhotra, Nageshwar
-
p. 653 - 656
(2007/10/02)
-
- O-Ethyl Thiocarbamates. A Convenient Route to 2-Aryliminoimidazolidines
-
The reaction of N-aryl thionocarbamates and ethylenediamine lead to the corresponding 2-aryliminoimidazolidines, whose structure in pharmacology is well known.But, the behaviour of the N-alkyl thionocarbamates is quite different under operative conditions and these compounds afford with ethylenediamine, to 2-(2'-aminoethylamino)-Δ2-imidazoline, according to a mechanism which is discussed.
- Reynaud, Pierre,Brion, Jean-Daniel,Davrinche, Catherine,Phan-Chi-Dao
-
p. 1789 - 1792
(2007/10/02)
-