Herein we describe the synthesis and in vitro biological evaluation of thirteen new, racemic, diversely functionalized imidazo pyranotacrines as non-hepatotoxic, multipotent tacrine analogues. Among these compounds, 1-(5-amino-2-methyl-4-(1-methyl-1H-imidazol-2-yl)-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinolin-3-yl)ethan-1-one (4) is non-hepatotoxic (cell viability assay on HepG2 cells), a select...

The asymmetric unit of title compound, C(7)H(6)N(4)·C(6)H(6)O(2), contains one 5-(1H-imidazol-1-yl)pyrimidine mol-ecule and two half benzene-1,4-diol mol-ecules; the benzene-1,4-diol mol-ecules are located on individual inversion centers. In the pyrimidine mol-ecule, the imidazole ring is twisted with respect to the pyrimidine ring at a dihedral angle of 25.73 (7)°. In the crystal, O-H⋯N hydrog...

In the title compound, [Cu(C(11)H(9)N(6))(2)(H(2)O)(2)](n), the Cu(II) atom lies on an inversion center and is coordinated by four N atoms from four 5-[4-(1H-imidazol-1-ylmethyl)phen-yl]tetra-zolate ligands and two water mol-ecules in a distorted octa-hedral geometry. The ligands bridge the Cu(II) atoms, leading to the formation of a two-dimensional network parallel to (100). The structure is f...

The phenol of 1-(3-(1H-imidazol-1-yl)propyl)-3-(4-hydroxy-3-methoxyphenyl)thiourea was selectively carbon-11 labelled to generate [11C]PBD150 in 7.3% yield from [11C]methyl triflate (non-decay corrected; radiochemical purity ≥95%, specific activity = 5.7 Ci/µmol, n=5). Evaluation of [11C]PBD150 by small animal PET imaging (mouse and rat) determined it does not permeate the blood brain barrier, ...

In the title complex, [Fe(C(10)H(6)N(3)O(4))(2)(H(2)O)(2)], the Fe(II) atom is located on a twofold rotation axis and is coordinated by two trans-positioned N,O-bidentate and zwitterionic 5-carboxy-2-(pyridinium-4-yl)-1H-imidazol-1-ide-4-carboxylate H(2)PIDC(-) ligands and two water mol-ecules in a distorted environment. In the crystal packing, a three-dimensional network is constructed via hyd...

High-throughput screening of 201,368 compounds revealed that 1-(3-(5-ethyl-5H-[1,2,4]triazino[5,6-b]indol-3-ylthio)propyl)-1H-benzo[d]imidazol-2(3H)-one (SID 7975595) inhibited RmlC a TB cell wall biosynthetic enzyme. SID 7975595 acts as a competitive inhibitor of the enzyme's substrate and inhibits RmlC as a fast-on rate, fully reversible inhibitor. An analog of SID 7975595 had a K(i) of 62nM....

The asymmetric unit of the title compound, C(14)H(16)N(4) (2+)·2C(7)H(4)NO(4) (-)·2C(7)H(5)NO(4), comprises one-half of the 3,3'-(p-phenyl-enedimethyl-ene)di-1H-imidazol-1-ium dication, which lies on an inversion centre, one 4-nitro-benzoate anion and one 4-nitro-benzoic acid mol-ecule. In the crystal, the components are linked into a two-dimensional network parallel to (110) by O-H⋯O, N-H⋯O an...