The lithium salts of 2-, 3- and 4-pyridinecarboxylic acids undergo deprotonation at the position adjacent to the carboxylate group when treated with LTMP in THF at 0 °C, −50 °C and −25 °C, respectively. The lithiation conditions could be extended to chloronicotinic acids, and even to an activ...

This paper presents polarographic (direct current, dc, and differential pulse, DP) and voltammetric (linear-sweep cyclic voltammetry) studies on the electroreduction of 6-chloronicotinic acid (6CNA) on mercury electrodes. In order to obtain the dissociation constants of 6CNA, UV–vis spectra wer...

Studies concentrating on hydrogen bonding between the base of 2-aminoheterocyclic compounds 5,7-dimethyl-1,8-naphthyridine-2-amine, 4-phenylthiazol-2-amine, and carboxylic acid derivatives have led to an increased understanding of the role 2-aminoheterocyclic compounds have in binding with carbo...

The determination of imidacloprid and its main metabolite (6-chloronicotinic acid) in honeybees was performed by liquid chromatography with post-column photochemical derivatisation in alkaline medium and fluorescence detection. The compounds were extracted from honeybees with acetone under ultra...

Pyridine-based compounds have been playing a crucial role as agrochemicals or pesticides including fungicides, insecticides/acaricides and herbicides, etc. Since most of the agrochemicals listed in the Pesticide Manual were discovered through screening programs that relied on trial-and-error tes...

The heterogeneous decarboxylative cyclization reaction between 2-benzoylpyridines and α-amino acids was achieved in toluene at 120 °C in the presence of 15 mol% of l-proline-functionalized MCM-41-supported copper(II) complex [l-Proline-MCM-41-Cu(OTf)2] and iodine with di-tert-butyl peroxide (D...

Cyclic voltammetry and controlled-potential electrolysis have been employed to investigate the direct and cobalt(I) salen-catalyzed reduction of 2,6-bis(chloromethyl)pyridine at carbon cathodes in acetonitrile containing tetramethylammonium tetrafluoroborate. A cyclic voltammogram for direct red...

As part of our effort to develop potential topoisomerase IIα (topo IIα) targeting anticancer agents, we systematically designed a new series of hydroxy and chloro-substituted 2,4-diphenyl 5H-chromeno[4,3-b]pyridines. Total eighteen compounds were synthesized and tested for their ability to inh...

The FT-IR and FT-Raman spectra of 2,6-Bis(chloromethyl)pyridine (BCMP) have been recorded in the regions 4000–400 cm−1 and 3500–100 cm−1, respectively. The total energy calculations of BCMP were tried for the possible rotational isomers. The molecular structure, geometry optimization, vibratio...

Tartrate-resistant acid phosphatase (TRAP/ACP5/uteroferrin/purple acid phosphatase/PP5) has received considerable attention as a newly discovered proinvasion metastasis driver associated with different malignancies. This renders TRAP an interesting target for novel anti-cancer therapy approaches...

36 new compounds with the typical skeleton of 4-anilino-5-vinyl/ethynyl pyrimidine, 4-anilino-3-cyano-5-vinyl/ethynyl/phenyl pyridine, and m-amino-N-phenylbenzamide, are designed, synthesized and selectively tested on EGFR, ErbB-2 kinases, and A-549, HL60 cells growth inhibition. Results from th...

Two series of 8-aminomethylated derivatives were prepared by Mannich reaction of scutellarein (2) with appropriate aliphatic amines, alicyclic amines and formaldehyde. All the compounds were tested for their thrombin inhibition activity through the analyzation of prothrombin time (PT), activated...

In order to improve the biological activity and water solubility of scutellarin (1), some derivatives of its main metabolite (scutellarein) were designed and synthesized. All the compounds were tested for their thrombin inhibition activity through the analyzation of thrombin time (TT), activated...

Nevadensin is major constituents of Lysionotus pauciflorus Maxim. (Chinese name: Shidiaolan), which has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive. In this paper, we investigated the metabolism of ...

Human carboxylesterase 1 (hCE1) is a key enzyme responsible for the hydrolysis of a wide range of endogenous and xenobiotic esters, but the highly selective inhibitors against hCE1 are rarely reported. This study aimed to assess the inhibitory effects of natural flavonoids against hCE1 and to fi...

Sterically hindered 2,4-disubstituted 3-(5-tetrazolyl)pyridines were synthesized from corresponding nicotinonitriles using microwave technology. 2-Methylnicotinonitriles were converted into the 2-azidomethyl-3-cyanopyridines via 2-hydroxymethyl and 2-chloromethyl derivatives. Intramolecular [3+2...

The metabotropic glutamate receptor subtype 5 (mGluR5) has been implicated in numerous neuropsychiatric disorders including addiction. We have discovered that the rigid diaryl alkyne template, derived from the potent and selective noncompetitive mGluR5 antagonist 2-methyl-6-(phenylethynyl)pyridi...

A green and convenient approach to the synthesis of 2-amino-4,6-diphenylnicotinonitriles via four-component reaction of malononitrile, aromatic aldehydes, acetophenone derivatives and ammonium acetate in water under ultrasound irradiation is described. The combinatorial synthesis was achieved fo...

Benzo[h]-1,6-naphthyridines and 5-ones, selectively functionalized at C-2, C-3, C-5 and C-10, were obtained by alkyllithium-, lithium amide- or potassium hydroxide-induced anionic cyclization of 3-cyano-2-(2-fluorophenyl)pyridine, which was functionalized regioselectively at positions 4, 5, 6, a...

An alternative and environmentally caring way for the synthesis of novel 2-amino-3-cyanopyridine derivatives bearing 5-imidazopyrazole nucleus is reported by one-pot four-component cyclocondensation reaction of substituted 5-(1H-imidazol/4-methyl-1-yl)-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyd...