N-(coumarin-3-yl)-N′-(2-amino-5-phenyl-1,3,4-thiadiazol-2-yl) urea was synthesized and characterized by elemental analysis, IR, 1H NMR, 13C NMR, UV–Vis and emission spectroscopy, as well as by single-crystal X-ray diffraction. X-ray crystallographic analyses have indicated that the crystal str...

Reaction of thiosemicarbazide with carboxylic acids, including N-substituted amino acids, in ionic liquids with H2SO4 as a catalyst affords 5-R-2-amino-1,3,4-thiadiazoles. On using alkanedicarboxylic acids, α,ω-bis(2-amino-1,3,4,-thiadiazol-5-yl)alkanes were obtained.

The asymmetric desymmetrization of 3-(4-fluorophenyl)glutaric anhydride 9 with lithiated chiral oxazolidin-2-one 8 has been studied. The desymmetrized product was formed with >90% de and converted into known intermediates for both (+)- and (−)-paroxetines.

6-Amidino-2-naphthyl [4-(4,5-dihydro-1H-imidazol-2-yl)amino]benzoate dimethanesulphonate has been developed for the therapy of pancreatitis. A reversed-phase high-performance liquid chromatographic assay of the levels of this drug and its metabolites in biological fluids was investigated. Fluore...

The acylation of substituted 2-aminopropanamides with (2S)-Boc-proline, (2S)-Cbz-proline and (2S)-Bn-proline was used to prepare substituted 1-protected N-(1-carbamoyl-1,1-dialkyl-methyl)-(S)-prolinamides (74–89%), whose subsequent deprotection gave N-(1-carbamoyl-1,1-dialkyl-methyl)-(S)-prolin...

A new series of five thermally and dimensionally stable aromatic poly(ether-imide)s consisting of an electron donating ortho-catenated triphenylamine (TPA) derivative bearing two trifluoromethyl groups and various electron-accepting phthalimide moieties were synthesized and thoroughly investigat...

Dichloro[4-(dimethylamino)phenyl]arsine (1) and tris[4-(dimethylamino)phenyl]arsine (2) were synthesized and characterized using single crystal X-ray diffraction studies, NMR spectroscopy, IR spectroscopy and elemental analyses techniques. The X-ray structure analysis of 1 (P1¯, triclinic, Z = ...

The synthesis of the trifluoromethyl group containing enol ethers by the palladium-catalyzed intermolecular reaction of 2,3,3-trifluoroallylic carbonates with oxygen nucleophiles was accomplished. The reaction proceeds through the intermolecular attack of oxygen nucleophiles on the C-2 carbon at...

3,5-Bis-(trifluoromethyl)phenyl isothiocyanate, was used as a convenient reagent for the derivatization of histamine, tyramine, tryptamine and 2-phenylethylamine, which eliminates the purification step. The obtained derivatives were determined by liquid chromatography-tandem mass spectrometry (L...

On account of the reported anticancer activity of pyrazoles and oxadiazoles, we have designed and synthesized a novel combinatorial library of S-substituted-1,3,4-oxadiazole bearing N-methyl-4-(trifluoromethyl)phenyl pyrazole moiety and tested for in-vitro cytotoxic activity by MTT assay. Amongs...

Fluorodecarboxylation of aryloxydifluoroacetic acid (ArOCF2CO2H) and arylmercaptodifluoroacetic acid (ArSCF2CO2H) towards ArXCF3 (X = O, S) using silver (I) salts in the presence of Selectfluor in a biphasic system with trifluoroacetic acid additive is discussed.

Determining the stereochemistry at the anomeric position of glycosides is imperative in chemical synthesis. As for 1,2-cis-β-glycosides such as β-mannosides, 13C-1H coupling constants, 1JCHs, are conventionally used when glycosides are in an ordinary chair conformation. In this work, we search...

In order to optimize the antileishmanial activity of piperazinyl-linked 5-(5-nitrofuran-2-yl)-1,3,4-thiadiazoles, we synthesized a series of 5-(5-nitrofuran-2-y1)-1,3,4-thiadiazoles with piperazinyl-linked benzamidine substituent as scaffold found in pentamidine related antiprotozoals. The struc...

Chagas disease affects around 8 million people worldwide and its treatment depends on only two nitroheterocyclic drugs, benznidazole (BZD) and nifurtimox (NFX). Both drugs have limited curative power in chronic phase of disease. Nifuroxazide (NF), a nitroheterocyclic drug, was used as lead to de...

Chagas disease, caused by the protozoan Trypanosoma cruzi, is a neglected chronic tropical infection endemic in Latin America. New and effective treatments are urgently needed because the two available drugs - benznidazole (BZD) and nifurtimox (NFX) - have limited curative power in the chronic p...

A facile synthetic approach to 5-arylamino-4-(5-nitrofuran- 2-yl)pyrimidines by the Buchwald–Hartwig cross-coupling with various anilines has been developed. All synthesized compounds demonstrated a significant level of in vitro antibacterial activity against Neisseria gonorrhoeae, Streptococcu...

We report the synthesis and biological evaluation of new 2-amino-4,5-diarylpyrimidines as selective antagonists at the adenosine A1 receptor. The scaffold they are based upon is a deaza variation of a previously reported collection of 3-amino-5,6-diaryl-1,2,4-triazines, members of which had a su...

We report herein the synthesis of some N-Mannich bases in addition to different N-4 substituents of norfloxacin. The antibacterial activities of the newly synthesized compounds were evaluated and correlated with their physicochemical properties. Results revealed that some of the tested compounds...

Synthesis and HIV-1 protease inhibitory activity of compound 5 based on the structure of a novel cyclic sulfonamide pharmacophore has been recently disclosed from our group. X-ray crystallographic structure of 5 when bound to the HIV-1 protease defined its binding mode. The importance of the geo...

In this study, a new method was developed for the oxidation of 5-hydroxymethylfurfural (HMF) into 2,5-furandicarboxylic acid (FDCA) over Merrifield resin supported Co(II)–meso-tetra(4-pyridyl)-porphyrin (abbreviated as Merrifield resin-Co-Py). Diffuse reflectance spectra showed that Co(II)–mes...