DFT (B3PW91/6-311þþG**), ab initio (HF/6-311þþG**), and single point CCSD(T)/6-311þþG**//B3PW91/6311þþG** calculations were performed to investigate the stability and tautomerism of the C5-substituted 1,2,3-triazoles. Three different tautomers are possible for the substituted 1,2,3-triazoles: N1–H, N2–H, and N3–H. For all the substituents applied, the most stable is the N2–H tautomer. Out of th...

A series of 1,4-disubstituted 1,2,3-triazoles have been prepared in high yields while respecting the stringent Click criteria. In these reactions, highly stable pre-formed complexes bearing diimine ligands were used.

The synthesis and kinetic resolution of quaternary oxindoles through copper catalysed azide-alkyne cycloadditions is presented. Selectivity factors (s) up to 22.1 ± 0.5 are reported. Enantioenriched alkynes and triazoles were obtained in ≥80% enantiomeric excess (e.e.).

Rhodium-catalyzed transannulation of 1,2,3-triazoles and ring-opening reactions of epoxides is described. A number of 3,4-dihydro-2H-1,4-oxazines are obtained in moderate yields probably involving generation of α-imino rhodium(II) carbene species.

Emerging fungi resistant to triazoles are a concern because of the increased use of medical triazoles and exposure to agricultural triazoles. However, little is known about the levels of triazole susceptibility in outdoor airborne fungi making it difficult to assess the risks of inhalation exposure to airborne, antifungal-resistant fungi. This study examined triazole susceptibilities of the air...

OBJECTIVE(S) Inhibitors of p38 MAP kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. The development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 MAP kinase is described. These are analogues of 4- pyridinyl imidazole p38 MAP kinase inhibitor reported by Merck Research Laborator...

Cycloadditions of azides with alkynes to form triazoles under thermal conditions (Huisgen cycloaddition) or in the presence of copper [click reaction, copper-catalyzed azide– alkyne cycloaddition (CuAAC)] are reactions of fundamental importance in organic chemistry. Triazoles can also be obtained by means of ruthenium, silver, and iridium catalysis, as well as by a zinc-mediated process. In sha...

The present study describes an efficient and ecofriendly, ultrasound, one-pot click cycloaddition approach for the construction of a novel series of 1,4-disubstituted-1,2,3-triazoles tethered with fluorinated 1,2,4-triazole-benzothiazole molecular conjugates. It involved three-component condensation of the appropriate bromoacetamide benzothiazole, sodium azide and 4-alkyl/aryl-5-(2-fluorophenyl...

Fluconazole, voriconazole, and itraconazole may potentiate the hypercalcemic effect of other medications, although to date, triazoles alone have not been linked to hypercalcemia. We describe a case of new-onset hypercalcemia in the setting of high-dose fluconazole that resolved after changing the antifungal regimen. We reviewed our institutional database to assess the frequency of moderate or s...

objective(s) inhibitors of p38 map kinase are considered as suitable target in the treatment of inflammatory diseases such as rheumatoid arthritis and bowel inflammatory diseases. the development of 5-alkylthio-1-aryl-2-(4-pyridinyl) triazoles as inhibitors of p38 map kinase is described. these are analogues of 4- pyridinyl imidazole p38 map kinase inhibitor reported by merck research laborator...