The asymmetric unit of the title compound, C15H16N2·C4H8O, contains two amidine mol-ecules (A and B) with slightly different conformations and two tetra-hydro-furan (THF) solvent mol-ecules. In the amidine mol-ecules, the di-methyl-phenyl ring and the NH2 group lie to the same side of the N=C bond and the dihedral angles between the aromatic rings are 54.25 (7) (mol-ecule A) and 58.88 (6) ° (mo...

Stress testing or forced degradation studies of denagliptin (1) tosylate in solution and solid-state, its blends with excipients, and capsules were conducted in order to elucidate degradation pathways, aid formulation development, and generate data to support regulatory filings. In solution, denagliptin was stressed in acid, water, and base using organic cosolvents. In the solid-state, denaglip...

Cryptosporidicidal effects of two polyether ionophores (maduramicin and alborixin), a fluorinated 4-quinolone (enrofloxacin), and three analogs of pentamidine were evaluated in a suckling mouse bioassay. Treatment with all compounds except enrofloxacin and one of the pentamidine analogs [1,3-di(4-imidazolinophenoxy)propane] resulted in significant (P less than 0.05) reductions in oocyst excretion.

Amidine-type peptide bond isosteres were designed based on the substitution of the peptide bond carbonyl (C=O) group with an imino (C=NH) group. The positively-charged property of the isosteric part resembles a reduced amide-type peptidomimetic. The peptidyl amidine units were synthesized by the reduction of a key amidoxime (N-hydroxyamidine) precursor, which was prepared from nitrile oxide com...

This communication demonstrates the preparation, isolation, and full characterization of superelectrophilic salts based on amidine dications in organic solvent, as their triflate salts. These dications are highly activated toward regiospecific reaction with hydrogen gas under mild conditions in the presence of a metal catalyst (Pd/C), mimicking the behavior of the natural substrate, N(5),N(10)-...