120321-65-5Relevant articles and documents
Synthesis and biological evaluation of novel dabigatran derivatives as thrombin inhibitors
Li, Chun Lei,Ren, Yu Jie
, p. 735 - 752 (2016)
A novel series of 3-[{2-[(4-carbamimidoylphenylamino)methyl]-1-substituted-1H-benzoimidazole-5-carbonyl}(3-chloro-4-fluorophenyl)amino]propionic derivatives of dabigatran was synthesized. The structures of the compounds were characterized by 1H NMR, 13C NMR, HRMS, and elemental analysis. The compounds were screened for in vitro thrombin inhibitory activity. The results indicated that the compounds had low to moderate inhibitory activity. The compounds with N-methyl and N-ethyl side chains had much greater inhibitory activity against thrombin than those with other side chains.
DERIVATIVES OF TETRACAINE
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Paragraph 0113, (2014/02/16)
Disclosed herein are derivatives of tetracaine that, among other things, block cyclic nucleotide gated (CNG) channels and are useful in the treatment of diseases characterized by overactive CNG channels such as retinal degeneration diseases.
Halogen substituents on the aromatic moiety of the tetracaine scaffold improve potency of cyclic nucleotide-gated channel block
Kirk, Sarah R.,Jackson, Evan P.,Cuellar, Elysia,Andrade, Adriana L.,Melich, Kenneth,Karpen, Jeffrey W.
supporting information; experimental part, p. 6417 - 6419 (2011/12/02)
A series of new tetracaine derivatives with substituents on the aromatic ring was prepared and evaluated for block of retinal rod cyclic nucleotide-gated (CNG) channels. Aromatic substitutions had little effect starting with the basic tetracaine scaffold,
3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b
Skinner, Philip J.,Cherrier, Martin C.,Webb, Peter J.,Sage, Carleton R.,Dang, Huong T.,Pride, Cameron C.,Chen, Ruoping,Tamura, Susan Y.,Richman, Jeremy G.,Connolly, Daniel T.,Semple, Graeme
, p. 6619 - 6622 (2008/04/02)
A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series.
(1H-azol-1-ylmethyl) substituted benzotriazole derivatives and pharmaceutical compositions containing them
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, (2008/06/13)
(1_H-azol-1-ylmethyl)substituted benzotriazole derivatives, compositions containing the same, and methods of treating estrogen dependent disorders.