Ulcerative colitis (UC) is a chronic disease, in which the lining of the colon becomes inflamed and develops ulcers leading to abdominal pain, diarrhea, and rectal bleeding. The extent of these symptoms depends on disease severity. The protein arginine deiminase (PAD) family of enzymes converts peptidyl-Arginine to peptidyl-Citrulline through citrullination. PADs are dysregulated, with abnormal...

Production of innate and adaptive immune cells from hematopoietic stem cells, and maturation of T lymphocytes are effective immune responses to fight severe microbial infection. In sepsis, this emergency myelopoiesis is damaged, leading to failure of bacterial clearance, and excessive stress-induced steroids cause immature T-lymphocyte apoptosis in thymus. We recently found that Cl-amidine, a p...

Rheumatoid arthritis is associated with the development of autoantibodies to citrullinated self-proteins. Citrullinated synovial proteins, which are generated via the actions of the protein arginine deiminases (PADs), are known to develop in the murine collagen-induced arthritis (CIA) model of inflammatory arthritis. Given these findings, we evaluated whether N-α-benzoyl-N5-(2-chloro-1-iminoeth...

DiC14-amidine (N-t-butyl-N°-tetradecylaminopropionamidine) is a cationic lipid used as transfection agent in vitro [1] and as a vector for in vivo gene therapy applications. DiC14-amidine molecules assemble in a liposomal structure (transition temperature: 23C-critical micelle concentration: 10-7 M). Compared to other cationic lipids, diC14-amidine does not require a helper lipid. This property...

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...

The conversion of peptidylarginine into peptidylcitrulline by calcium-dependent peptidylarginine deiminases (PADs) has been implicated in the pathogenesis of a number of diseases, identifying PADs as therapeutic targets for various diseases. The PAD inhibitor Cl-amidine ameliorates the disease course, severity, and clinical manifestation in multiple disease models, and it also modulates dendrit...

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.

Ulcerative colitis is a dynamic, idiopathic, chronic inflammatory condition that carries a high colon cancer risk. We previously showed that Cl-amidine, a small-molecule inhibitor of the protein arginine deiminases, suppresses colitis in mice. Because colitis is defined as inflammation of the colon associated with infiltration of white blood cells that release free radicals and citrullination i...

Three amidines, N, N’-Diphénylbenzamidine (1), N-Cyclohexyl-N’-phényl-octamidine (2), N, N’diphényldodécamidine (3), were synthesized and investigated for their antioxidant activity using 2, 2-diphenyl-1picrylhydrazyl (DPPH) radical scavenging, ferric reducing antioxidant power (FRAP) and β-carotene/linoleic acid assays. The results indicated that amidines tested possess good antioxidant activi...