128073-02-9

Upstream product

• 57266-69-0 3-chloropyridine-2-carboxylic acid 

Downstream Products

• 1617540-26-7 ethyl 4-oxo-1-((4'-(trifluoromethyl)biphenyl-2-yl)methyl)-1,4-dihydro-1,5-naphthyridine-3-carboxylate 
• 1617540-25-6 ethyl 1-(2-bromobenzyl)-4-oxo-1,4-dihydro-1,5-naphthyridine-3-carboxylate 
• 1617540-23-4 1-oxo-1-((4'-(trifluoromethyl)biphenyl-2-yl)methyl)-1,4-dihydro-1,5-naphthyridine-3-carboxylic acid 
• 1423036-78-5 5-(3-chloropyridin-2-yl)-1-(2,2,2-trifluoroethyl)-1H-pyrazole-4-carboxylic acid (4-chloro-2-methyl-6-methylcarbamoylmethoxycarbamoylphenyl)amide 
• 1423122-29-5 N-[4-chloro-2-((Z)-1,3-dithiolan-1-ylidenecarbamoyl)-6-methyl-phenyl]-5-(3-chloro-2-pyridyl)-1-(2,2,2-trifluoroethyl)pyrazole-4-carboxamide 
• 1616681-80-1 3-chloro-N-(2-hydroxy-5-[(trifluoromethyl)sulfinyl]phenyl)pyridine-2-carboxamide 

Relevant academic research and scientific papers

Design and Discovery of Novel Antifungal Quinoline Derivatives with Acylhydrazide as a Promising Pharmacophore

Inspired by natural 2-quinolinecarboxylic acid derivatives, a series of quinoline compounds containing acylhydrazine, acylhydrazone, sulfonylhydrazine, oxadiazole, thiadiazole, or triazole moieties were synthesized and evaluated for their fungicidal activity. Most of these compounds exhibited excellent fungicidal activity in vitro. Significantly, compound 2e displayed the superior in vitro antifungal activity against Sclerotinia sclerotiorum, Rhizoctonia solani, Botrytis cinerea, and Fusarium graminearum with the EC50 values of 0.39, 0.46, 0.19, and 0.18 μg/mL, respectively, and were more potent than those of carbendazim (EC50, 0.68, 0.14, >100, and 0.65 μg/mL, respectively). Moreover, compound 2e could inhibit spore germination of F. graminearum. Preliminary mechanistic studies showed that compound 2e could cause abnormal morphology of cell walls and vacuoles, loss of mitochondrion, increases in membrane permeability, and release of cellular contents. These results indicate that compound 2e displayed superior fungicidal activities and could be a potential fungicidal candidate against plant fungal diseases.

Substituted formyldimethomorph (ethylpiperazine compound and) application thereof

The invention relates to substituted formyl morpholinoethyl piperazine compounds and an application thereof. The compounds are shown in a general formula (I) in the description, wherein R is phenyl, pyridyl, furyl, pyrazolyl, thiazolyl, thienyl or phenazi

Identification and Optimization of a Series of 8-Hydroxy Naphthyridines with Potent in Vitro Antileishmanial Activity: Initial SAR and Assessment of in Vivo Activity

Visceral leishmaniasis (VL) is a parasitic infection that results in approximately 26 ?000-65 ?000 deaths annually. The available treatments are hampered by issues such as toxicity, variable efficacy, and unsuitable dosing options. The need for new treatments is urgent and led to a collaboration between the Drugs for Neglected Diseases initiative (DNDi), GlaxoSmithKline (GSK), and the University of Dundee. An 8-hydroxynaphthyridine was identified as a start point, and an early compound demonstrated weak efficacy in a mouse model of VL but was hampered by glucuronidation. Efforts to address this led to the development of compounds with improved in vitro profiles, but these were poorly tolerated in vivo. Investigation of the mode of action (MoA) demonstrated that activity was driven by sequestration of divalent metal cations, a mechanism which was likely to drive the poor tolerability. This highlights the importance of investigating MoA and pharmacokinetics at an early stage for phenotypically active series.

Discovery of pyrazolo[1,5-a]pyrimidine-3-carbonitrile derivatives as a new class of histone lysine demethylase 4D (KDM4D) inhibitors

Herein we report the discovery of a series of new small molecule inhibitors of histone lysine demethylase 4D (KDM4D). Molecular docking was first performed to screen for new KDM4D inhibitors from various chemical databases. Two hit compounds were retrieved. Further structural optimization and structure-activity relationship (SAR) analysis were carried out to the more selective one, compound 2, which led to the discovery of several new KDM4D inhibitors. Among them, compound 10r is the most potent one with an IC50 value of 0.41?±?0.03?μM against KDM4D. Overall, compound 10r could be taken as a good lead compound for further studies.

NAPHTHYRIDINONE DERIVATIVES AND THEIR USE IN THE TREATMENT, AMELIORATION OR PREVENTION OF A VIRAL DISEASE

The present invention relates to a compound having the general formula (V), optionally in the form of a pharmaceutically acceptable salt, solvate, polymorph, codrug, cocrystal, prodrug, tautomer, racemate, enantiomer, or diastereomer or mixture thereof, which are useful in treating, ameloriating or preventing a viral disease. Furthermore, specific combination therapies are disclosed.

N-THIO-ANTHRANILAMIDE COMPOUNDS AND THEIR USE AS PESTICIDES

The present invention relates to N-thio-anthranilamide compounds of formula (I) and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the N-thio-anthranilamide compou

CARBAMOYLMETHOXY- AND CARBAMOYLMETHYLTHIO- AND CARBAMOYLMETHYLAMINO BENZAMIDES FOR COMBATING INVERTEBRATE PESTS

The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the ca

ANTHRANILAMIDE COMPOUNDS AND THEIR USE AS PESTICIDES

The present invention relates to anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the anthranilamide compounds or of the compositions co

SUBSTITUTED PYRAZOLO [1,5-α] PYRIDINE COMPOUNDS AND THEIR METHODS OF USE

The present invention is directed to substituted pyrazolo[l,5-α]pyridines and related methods for their synthesis and use.

Antiallergic agents. III. N-(1H-tetrazol-5-yl)-2-pyridinecarboxamides

A series of N-tetrazolylpyridinecarboxamides was prepared and evaluated for antiallergic activity by the passive cutaneous anaphylaxis assay. From the structure-activity relationships of this class of compounds, it was revealed that the N-tetrazolylcarbamoyl group as an acidic functionality is required to be at the 2-position of the pyridine nucleus and that the phenyl group as a substituent is not necessarily required for activity. 6-Methyl-N-(1H-tetrazol-5-yl)-2-pyridinecarboxamide showed good oral activity and low toxicity.