Novel Strategy for Non-Aqueous Bioconjugation of Substituted Phenyl-1,2,4-triazole-3,5-dione Analogues.

A novel 4-[4-(pentafluoro-λ⁶-sulfanyl)phenyl]-1,2,4-triazole-3,5-dione () was synthesised as a potential [F]radio-prosthetic group for radiolabelling peptides and proteins via selective bioconjugation with the phenolic side chains of tyrosine residues. Preliminary conjugation tests revealed the rapid hydrolysis of under semi-aqueous conditions; these results led to further investigation into the electronic substituent effects of PTAD derivatives and corresponding hydrolytic stabilities. Five derivatives of with substituents of varying electron donating and withdrawing effects were synthesised for the investigation.

Synthesis and biological evaluation of tetrahydroisoquinoline-derived antibacterial compounds.

Antibiotic resistance is one of the greatest threats to modern medicine. Drugs that were once routinely used to treat infections are being rendered ineffective, increasing the demand for novel antibiotics with low potential for resistance. Here we report the synthesis of 18 novel cationic tetrahydroisoquinoline-triazole compounds.

Formation of an unexpected 3,3-diphenyl-3-indazole through a facile intramolecular [2 + 3] cycloaddition of the diazo intermediate.

The one-pot reaction of 2,6-bis(diphenylmethyl)-4-methoxyaniline with -butylnitrite, BTEAC and DABSO in the presence of CuCl provided an unexpected 3-indazole product . The structure of the compound was determined by HRMS, IR, NMR and further confirmed by single crystal X-ray crystallography. The compound crystallises in the triclinic -1 space group, with unit cell parameters = 9.