77047-42-8

Upstream product

• 10445-91-7 4-(Chloromethyl)pyridine 
• 762-04-9 Diethyl phosphonate 
• 762-04-9 phosphonic acid diethyl ester 
• 54751-01-8 4-(bromomethyl)pyridine 
• 122-52-1 triethyl phosphite 
• 1822-51-1 4-picolylchloride hydrochloride 
• 2870-30-6 sodium diethyl phosphate 
• 872-85-5 pyridine-4-carbaldehyde 
• 2459-09-8 4-pyridinecarboxylic acid, methyl ester 
• 586-95-8 pyridine-4-methanol 

Downstream Products

• 1415818-83-5 diethyl 3-(N-benzyloxyamino)-1-(pyridin-4-yl)propylphosphonate 
• 1548368-52-0 4-iodo-N,N-bis(4-((E)-2-(pyridin-4-yl)vinyl)phenyl)aniline 
• 1548367-63-0 4-bromo-N,N-bis(4-((E)-2-(pyridin-4-yl)vinyl)phenyl)aniline 
• 1239713-20-2 C₃₉H₃₀N₄ 
• 117999-80-1 <(1-benzylpyridino)-4-methyl>phosphonic acid 
• 113229-61-1 cis-4-(phosphonomethyl)piperidine-2-carboxylic acid 
• 80241-43-6 (4-Pyridylmethyl)phosphonic acid 

Relevant academic research and scientific papers

Orotic acid as a useful supramolecular synthon for the fabrication of an OPV based hydrogel: Stoichiometry dependent injectable behavior

A facile hydrogelation of a p-pyridylenevinylene derivative (PV) bearing oxyethylene chains in the presence of orotic acid (OA) occurs via various non-covalent interactions. Depending on the PV:OA molar ratio, the hydrogel shows vesicle to either cluster-

Peptidomimetic Vinyl Heterocyclic Inhibitors of Cruzain Effect Antitrypanosomal Activity

Cruzain, an essential cysteine protease of the parasitic protozoan, Trypanosoma cruzi, is an important drug target for Chagas disease. We describe here a new series of reversible but time-dependent inhibitors of cruzain, composed of a dipeptide scaffold appended to vinyl heterocycles meant to provide replacements for the irreversible reactive "warheads" of vinyl sulfone inactivators of cruzain. Peptidomimetic vinyl heterocyclic inhibitors (PVHIs) containing Cbz-Phe-Phe/homoPhe scaffolds with vinyl-2-pyrimidine, vinyl-2-pyridine, and vinyl-2-(N-methyl)-pyridine groups conferred reversible, time-dependent inhibition of cruzain (Ki? = 0.1-0.4 μM). These cruzain inhibitors exhibited moderate to excellent selectivity versus human cathepsins B, L, and S and showed no apparent toxicity to human cells but were effective in cell cultures of Trypanosoma brucei brucei (EC50 = 1-15 μM) and eliminated T. cruzi in infected murine cardiomyoblasts (EC50 = 5-8 μM). PVHIs represent a new class of cruzain inhibitors that could progress to viable candidate compounds to treat Chagas disease and human sleeping sickness.

Antimalarial and structural studies of pyridine-containing inhibitors of 1-deoxyxylulose-5-phosphate reductoisomerase

1-Deoxy-d-xylulose-5-phosphate reductoisomerase (DXR) in the nonmevalonate isoprene biosynthesis pathway is a target for developing antimalarial drugs. Fosmidomycin, a potent DXR inhibitor, showed safety as well as efficacy against Plasmodium falciparum malaria in clinical trials. On the basis of our previous quantitative structure-activity relationship (QSAR) and crystallographic studies, several novel pyridine-containing fosmidomycin derivatives were designed, synthesized, and found to be highly potent inhibitors of P. falciparum DXR (PfDXR) having Ki values of 1.9-13 nM, with the best one being ～11× more active than fosmidomycin. These compounds also potently block the proliferation of multidrug resistant P. falciparum with EC 50 values as low as 170 nM. A 2.3 A? crystal structure of PfDXR in complex with one of the inhibitors is reported, showing that the flexible loop of the protein undergoes conformational changes upon ligand binding and a hydrogen bond and favorable hydrophobic interactions between the pyridine group and the PfDXR account for the enhanced activity.

INDAZOLYL, BENZIMIDAZOLYL, BENZOTRIAZOLYL SUBSTITUTED INDOLMONE DERIVATIVES AS KINASE INHIBITORS USEFUL IN THE TREATMENT OF CANCER

The present invention is directed to a compound is represented by Structural Formula (A):or a pharmaceutically acceptable salt therof. The present invention is also directed to a pharmaceutical composition comprising a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier or diluent. Also disclosed is a method of treating a subject having cancer, wherein the method comprises administering a therapeutically effective amount of a compound represented by Structural Formula (A) described above or a pharmaceutically acceptable salt thereof.

Substituted 4-aza-5α-androstan-ones as 5α-reductase inhibitors

Described are new 16-substituted and 7,16-disubstituted 4-aza-5α-androstan-3-ones and related compounds as 5α-reductase inhibitors.

Delta-17 and delta-20 olefinic and saturated 17 beta-substituted 4-aza-5 alpha-androstan-ones as 5 alpha reductase inhibitors useful in the prevention and treatment of hyperandrogenic disorders

Described are delta 17 and delta 20 olefinic and saturated 17 Beta-substituted 4-aza-5 alpha-androstan-3-ones and related compounds having 5 alpha reductase inhibitors for treatment of benign prostatic hyperplasia and other hyperandrogenic related disorders.

SYNTHESIS AND CHARACTERIZATION OF OXIMINO PYRIDOYL PHOSPHONATES

Oximino pyridoyl phosphonates were synthesised as well as the methiodide of oximino-2-pyridoyl phosphonate.All these compounds along with their intermediates have been characterized by spectroscopic methods and by elemental analysis.Key words: Phosphite, Michaelis-Becker reaction, Oximino pyridoyl phosphonates.

PHOTODEPHOSPHORYLATION OF PHOSPHONIC ACIDS

Photolysis of phosphonic acids in an alkaline aqeous solution gave 1-benzyl-methylpyridinium phosphates by the photocleavage of the C-P bond.

Photolysis of Pyridylmethyl- and Pyridiniomethylphosphonic Acids

Upon UV-irradiation, the C-P bond of (4-pyridylmethyl)phosphonic acid cleaved only near the isoelectronic point to give 4-methylpyridinium phophate, while (1-benzyl-4-pyridiniomethyl)phosphonic acid underwent C-P bond cleavage above pH 4 to give 1-benzyl-4-methylpyridinium phosphate.On the other hand, the C-P bond of (2-pyridylmethyl)phosphonic acid cleaved under pH region of about 1 to 2, while (1-benzyl-2-pyridiniomethyl)phosphonic acid underwent C-P bond cleavage above pH4.

Synthesis and Pharmacology of a Series of 3- and 4-(Phosphonoalkyl)pyridine- and piperidine-2-carboxylic Acids. Potent N-Methyl-D-aspartate Receptor Antagonists

We recently prepred a series of 3- and 4-(phosphonoalkyl)pyridine- and piperidine-2-carboxylic acids as antagonists of neurotransmission at N-methyl-D-aspartate (NMDA) preferring receptors.NMDA antagonists may prove to be useful therapeutic agents, for instance, as anticonvulsants, in the treatment of neurodegenerative disorders such as Alzheimer's disease and in the prevention of neuronal damage that occurs during cerebral ischemia.The compounds prepared were evaluated for their ability to displace CPP binding (an assay shown to be selective for compounds that bind at the NMDA receptor) and for their ability to block NMDA-induced lethality in mice (an assay that is also specific for competitive and noncompetitive NMDA antagonists).Two of the compounds, cis-4-(phosphonomethyl)piperidine-2-carboxylic acid (11a) and cis-4-(3-phosphonoprop-1-yl)piperidine-2-carboxylic acid (11c) proved to be potent NMDA antagonists. 11a and 11c displaced CPP binding with IC 50's of 95 and 120 nM, respectively, and both protected mice from NMDA-induced lethality, with MEDs (minimum effective dose, the dose at which three of the five animals tested survived) of 10 and 40 mg/kg ip, respectively.The rest of the compounds prepared were weakly active or inactive in these assays.The pattern of activity observed for this series parallels that observed for the acyclic series of ω-phosphono-α-amino acids, where AP5 and AP7 possessed NMDA antagonist activity while AP6 and AP8 were inactive.Reduction of conformational mobility by incorporation of the piperidine ring led to enhanced potency relative to the acyclic analogues.