Synthesis of -phenyl- and -thiazolyl-1-indazoles by copper-catalyzed intramolecular -arylation of -chlorinated arylhydrazones.

The broad application of 1-indazoles has prompted the development of several approaches for the synthesis of such compounds, including metal-free, palladium-, or copper-promoted intramolecular -arylation of in situ-generated or isolated -haloarylhydrazones. Such methods mainly start from -bromo derivatives due to the better yield observed when compared to those obtained from -chloroarylhydrazones. However, the -chloroarylaldehydes and -chloroarylketones used to prepare the arylhydrazones are more commercially available and less expensive than brominated analogs.

Synthesis, structural characterization, and prospects for new cobalt (II) complexes with thiocarbamoyl-pyrazoline ligands as promising antifungal agents.

Candida spp. cause invasive fungal infections. One species, Candida glabrata, may present intrinsic resistance to conventional antifungal agents, thereby increasing mortality rates in hospitalized patients.

Recent advances on the green synthesis and antioxidant activities of pyrazoles.

Pyrazoles have a representative history in medicinal chemistry. These nucleuses, molecules of synthetic origin, constitute a group of nitrogen heterocyclic compounds. Available literature particularly shows a variety of pyrazoles with antioxidant effect.

(5E)-1-Benzyl-5-(3,3,3-tri-chloro-2-oxo-propyl-idene)pyrrolidin-2-one.

In the crystal structure of the title compound, C14H12Cl3NO2, no classical hydrogen-bonding inter-actions are observed. The methyl-ene fragments of the benzyl groups participate in non-classic hydrogen-bond inter-actions with the carbonyl O atoms of neighboring mol-ecules, generating co-operative centrosymmetric dimers with R 5 (5)(10) ring motifs. The overall mol-ecular arrangement in the unit cell seems to be highly influenced by secondary non-covalent weak C-Cl⋯π [Cl⋯Cg(phenyl ring) = 3.

Anti-Candida, anti-enzyme activity and cytotoxicity of 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides.

Because of the need for more effective and less harmful antifungal therapies, and interest in the synthesis of new carboximidamides, the goal of this study was to determine the antifungal and anti-enzyme activities of some new pyrazole carboximidamides and their cytotoxicity. For this purpose, tests were performed to evaluate: minimum inhibitory concentration (MIC) and minimum fungicidal concentration (MFC); production of proteinases and phospholipase, and cytotoxicity of the extracts. Data were analyzed by ANOVA and Tukey Tests (α = 5%).

(S,Z)-3-Phenyl-2-[(1,1,1-tri-chloro-7-meth-oxy-2,7-dioxohept-3-en-4-yl)amino]-propanoic acid monohydrate.

In the title compound, C17H18Cl3NO5·H2O, intra-molecular N-H⋯O and C-H⋯Cl hydrogen bonds form S(6) and S(5) ring motifs, respectively. The chiral organic mol-ecule is connected to the solvent water mol-ecule by a short O-H⋯O hydrogen bond. In the crystal, a weak C-H⋯Cl inter-action connects the organic mol-ecules along [100] while the water mol-ecules act as bridges between the organic mol-ecules in both the [100] and [010] directions, generating layers parallel to the ab plane.

Antioxidant capacity and environmentally friendly synthesis of dihydropyrimidin-(2H)-ones promoted by naturally occurring organic acids.

The Biginelli reaction is a multicomponent reaction involving the condensation between an aldehyde, a β-ketoester, and urea or thiourea, in the presence of an acid catalyst, producing dihydropyrimidinones (DHPMs). Owing to their important pharmacological properties, the DHPMs have been studied by many authors. However, most of the methodologies used for the synthesis of these compounds require drastic reaction conditions.

Ultrasound promoted the synthesis of N-propargylic β-enaminones.

The synthesis of 14 novel N-propargylic β-enaminones from the reaction of β-alkoxy vinyltrihalomethyl[carboxyethyl] ketones [R(3)C(O)CHC(R(1))OMe, where R(3)=CF(3), CCl(3), CO(2)Et and R(1)=Me, Et, Pr, Bu, i-Pent, CH(2)CH(2)CO(2)Me] with propargyl amines [R(2)NHCH(2)CCH, where R(2)=Pr, PhCH(2)] is reported. Yields, solvents and reaction times needed for reaction completion, by microwave irradiation (MW), conventional thermal heating (TH) and under ultrasound irradiation (US) are compared. The best results were obtained under US irradiation in good to excellent yields (70-93%).

Ultrasound promoted greener synthesis of 2-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenylthiazoles.

A rapid and cleaner procedure for the synthesis of a series of 2-(3,5-diaryl-4,5-dihydro-1H-pyrazol-1-yl)-4-phenylthiazoles under ultrasonic irradiation in ethanol is described.

Efficient sonochemical synthesis of novel 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides.

An ultrasound-assisted preparation of a series of novel 3,5-diaryl-4,5-dihydro-1H-pyrazole-1-carboximidamides that proceeds via the efficient reaction of chalcones with aminoguanidine hydrochloride under clean conditions is described.

Environmentally friendly sonocatalysis promoted preparation of 1-thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles.

An efficient and green synthesis of thiocarbamoyl-3,5-diaryl-4,5-dihydro-1H-pyrazoles via the condensation of chalcones with thiosemicarbazide in ethanol and KOH under ultrasound irradiation is reported. The products were isolated in good yields after short reaction times.