218131-31-8Relevant articles and documents
Synthesis and evaluation of isoleucine derived angiotensin II AT 2 receptor ligands
Veron, Jean-Baptiste,Joshi, Advait,Wallinder, Charlotta,Larhed, Mats,Odell, Luke R.
, p. 476 - 479 (2014/01/23)
Sixteen new C-terminally modified analogues of 2, a previously described potent and selective AT2R ligand, were designed, synthesized and evaluated for their affinity to the AT2R receptor. The introduction of large, hydrophobic substituents was shown to be beneficial and the most active compound (17, Ki = 8.5 μM) was over 12-times more potent than the lead compound 2.
Iron-porphyrin NO complexes with covalently attached N-donor ligands: Formation of a stable six-coordinate species in solution
Berto, Timothy C.,Praneeth,Goodrich, Lauren E.,Lehnert, Nicolai
experimental part, p. 17116 - 17126 (2010/03/25)
A series of substituted tetraphenylporphyrin type macrocycles (TMP or To-F2PP) with covalently attached N-donor ligands (pyridine or imidazole linker) have been synthesized. Linkers with varying chain lengths and designs have been applied to systematically investigate the effect of chain length and rigidity on the binding affinity of the linker to the corresponding Fe(II)-NO heme complexes. The binding of the linker is monitored in solution using a variety of spectroscopic methods including UV-vis absorption, EPR, and IR spectroscopy. Both the N-O stretching frequency and the imidazole 14N hyperfine coupling constants show a good correlation with the Fe-(N-donor) bond strength in these systems. The complexes with covalently attached pyridyl and alkyl imidazole ligands only exhibit weak interactions of the linker with iron(II). However, the stable six-coordinate complex [Fe(To-F2PP-BzIM)(NO)] (4) is obtained when a rigid benzyl linker is applied. This complex exhibits typical properties of six-coordinate ferrous heme-nitrosyls in which an N-donor ligand is bound trans to NO, including the Soret band at 427 nm and the typical nine line 14N hyperfine splitting in the EPR spectrum. A crystal structure has been obtained for the corresponding zinc complex. Here, we report the first systematic study on the requirements for the formation of stable six-coordinate ferrous heme nitrosyl complexes in solution at room temperature in the absence of excess axial N-donor ligand.
A structure-Permeability study of small drug-like molecules
Fichert, Thomas,Yazdanian, Mehran,Proudfoot, John R.
, p. 719 - 722 (2007/10/03)
A systematic structure-permeability relationship study on a set of small drug-like molecules with log D values in the range -2.5 to 3 and carrying a diverse array of functionality reveals that the compounds with log D>0 and 3 are highly permeable. Surprisingly, several tetrazole derivatives were found to be substrates for efflux pump(s).
