A congeneric set of carbamimidolyl-aryl-vinyl-carboxamidines from the National Cancer Institute (NCI) open chemical repository were identified as potent inhibitors of anthrax lethal factor (LF), a zinc-dependent metalloprotease that plays a critical role in potentiating Bacillus anthracis infection. Surprisingly, these compounds exhibited no differential change in activity with concentration. D...

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Titanium(IV)-mediated reactions between primary amines and secondary carboxamides exhibit different outcomes, amidine formation versus transamidation, depending on the identity of the TiIV complex used and the reaction conditions employed. The present study probes the origin of this divergent behavior. We find that stoichiometric TiIV, either Cp*TiIV complexes or Ti(NMe2)4, promotes formation o...

Protein Arginine Deiminases (PADs) catalyze the post-translational conversion of peptidyl-Arginine to peptidyl-Citrulline in a calcium-dependent, irreversible reaction. Evidence is emerging that PADs play a role in carcinogenesis. To determine the cancer-associated functional implications of PADs, we designed a small molecule PAD inhibitor (called Chor-amidine or Cl-amidine), and tested the imp...

In the title compound, C(10)H(11)N(3), the amidine unit, including the two methyl substituents, is virtually planar [maximum deviation = 0.016 (5) Å]. The plane of the benzene ring forms a dihedral angle of 46.5 (3)° with the amidine group.

four amidine nr2b-selective nmda receptor antagonists, n-( 2-methoxy benzyl) -3-phenyl-acrylamidine, n-[diduterio(2-methoxyphenyl) methyl]-3-phenyl-acrylamidine, n-benzyl-3-phenyl-acryl amidine and n-[diduterio(phenyl)methyl]-3-phenyl-acrylamidine, all fourlabeled with carbon-14 in the 1-position, have been synthesized as part of 5-step sequence fromba14co3.

The title compound, C(13)H(11)BrN(2)O, a hydroxy-amidine derivative (an amidoxime), was obtained by addition of the corresponding imidoyl chloride to hydroxy-lamine. The benzene and phenyl rings are twisted from the mean plane of the hydroxy-amidine group by 34.4 (1) and 59.2 (1)°, respectively. In the crystal structure, inter-molecular O-H⋯N hydrogen bonds link pairs of mol-ecules, forming cen...