(2S,3R)-3-Hydroxy-2-(hydroxymethyl)-3,6-dihydro-2H-pyridine 8, an important precursor for the synthesis of polyhydroxylated piperidine azasugars, has been prepared from L-serine. Highly stereoselective nucleophilic addition to amino aldehyde 5 gave the corresponding allylic alcohol 6 which proceeded to give dihydro-2H-piridine 7a via a Grubbs II catalyzed RCM. Stereoselective H-bond directed ep...

4-[5-(Pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile (FYX-051) is a potent inhibitor of bovine milk xanthine oxidoreductase (XOR). Steady-state kinetics study showed that it initially behaved as a competitive-type inhibitor with a K(i) value of 5.7 × 10(-9) M, then after a few minutes it formed a tight complex with XOR via a Mo-oxygen-carbon atom covalent linkage, as reported previ...

The heterocyclic amines (HCAs) found in cooked meat are procarcinogens that are metabolically activated by N-hydroxylation followed by O-acetylation by the N-acetyltransferases NAT1 and NAT2. Despite the importance of metabolic activation in HCA carcinogenicity and the finding that several HCAs are rodent mammary gland carcinogens, nothing was known about O-acetylation activity in the human mam...

In the title compound, [Co(C(7)H(5)O(3))(C(14)H(12)N(2))(H(2)O)(2)]NO(3)·2H(2)O, the Co(II) ion is six-coordinated by two N atoms of a 2,9-dimethyl-1,10-phenanthroline (dmphen) ligand, two carboxyl-ate O atoms of one 4-hydroxy-benzoate anion and two O atoms of two water mol-ecules, in a distorted octa-hedral environment; the two water mol-ecules occupy the apical positions. In the crystal struc...

The reaction of mercury(II) chloride dihydrate, propane-1,3-diamine and 4-hydroxy-pyridine-2,6-dicarboxylic acid in a 1:1:1 molar ratio in aqueous solution, resulted in the formation of the title compound, (C(3)H(12)N(2))[Hg(C(7)H(3)NO(5))Cl(H(2)O)](2)·4H(2)O or (pnH(2))[Hg(hypydc)Cl(H(2)O)](2)·4H(2)O (where pn is propane-1,3-diamine and hypydcH(2) is 4-hydroxy-pyridine-2,6-dicarboxylic acid). ...

Nicotine is a natural alkaloid that is very toxic to humans. To eliminate the harmful effects of nicotine in the environment, biological methods employing microbes to degrade nicotine are required (Brandsch, 2006; Liu et al., 2015). Shinella sp. HZN7 can degrade nicotine efficiently via the variant of a pyridine and pyrrolidine pathways (VPP; Ma et al., 2013; Qiu et al., 2014, 2015). The main i...

10-Nornaltrexones (3-(cyclopropylmethyl)-4a,9-dihydroxy-2,3,4,4a,5,6-hexahydro-1H-benzofuro[3,2-e]isoquinolin-7(7aH)-one, 1) have been underexploited in the search for better opioid ligands, and their enantiomers have been unexplored. The synthesis of trans-isoquinolinone 2 (4-aH, 9-O-trans-9-methoxy-3-methyl-2,3,4,4a,5,6-hexahydro-1H-benzofuro[3,2-e]isoquinolin-7(7aH)-one) was achieved through...

The reaction of iron(II) sulfate hepta-hydrate with the proton-transfer compound (pydaH)(hypydcH) (pyda = pyridine-2,6-diamine; hypydcH(2) = 4-hydroxy-pyridine-2,6-dicarboxylic acid) in an aqueous solution led to the formation of the title compound, (C(5)H(8)N(3))[Fe(C(7)H(3)NO(5))(2)]·2H(2)O. The anion is a six-coordinated complex with a distorted octa-hedral geometry around the Fe(III) atom. ...

8-Hydroxy-6-methyl-5,6,7,8-tetrahydroimidazo[1,2-a]pyridine was formed selectively in high yields from N-(beta-methallyl)imidazole by a tandem hydroformylation-cyclization sequence, representing a novel one-pot catalytic synthesis of bicyclic imidazole derivatives.

A simple and efficient protocol for the construction of substituted piperazines, piperidines, thiomorpholines, decahydroquinolines, perhydrocyclopenta[b]pyridine, and pyrrolidines bearing N-hydroxy substituents through intramolecular reductive cyclization of diketoximes using sodium cyanoborohydride is described.