54872-79-6

Usage

Uses

Used in Biochemical and Pharmacological Research:
3-Fluoro-N-hydroxy-benzamidine is utilized as a research tool for studying the functions of serine proteases and their role as potential drug targets. Its inhibitory properties allow scientists to investigate the mechanisms and pathways involving these enzymes, contributing to a deeper understanding of their biological significance.
Used in Drug Discovery and Development:
In the pharmaceutical industry, 3-Fluoro-N-hydroxy-benzamidine serves as a key component in the design and optimization of new drugs. Its application extends to the treatment of various diseases and conditions, including cancer, inflammation, and coagulation disorders. By targeting serine proteases, 3-FLUORO-N-HYDROXY-BENZAMIDINE aids in the development of therapeutic agents that can modulate the activity of these enzymes, potentially leading to effective treatments.
Used as a Building Block in Synthesis:
3-Fluoro-N-hydroxy-benzamidine is also employed as a versatile building block in the synthesis of other chemical compounds and pharmaceuticals. Its reactivity and functional groups make it an attractive candidate for the creation of novel molecules with potential applications in various fields, further expanding the utility of 3-FLUORO-N-HYDROXY-BENZAMIDINE in the chemical and pharmaceutical industries.

Upstream product

• 72505-20-5 3-fluorobenzene-1-carbothioamide 
• 403-54-3 m-Fluorobenzonitrile 
• 1073-06-9 3-fluorobromobenzene 
• 24964-64-5 3-Cyanobenzaldehyde 
• 501-00-8 3-fluorophenylacetonitrile 

Downstream Products

• 75907-90-3 O-(4,4-Dinitropentanoyl)-3-fluorobenzamidoxime 
• 1196463-28-1 C₁₂H₁₃FN₂O₄ 
• 1083401-80-2 2-(3-fluorophenyl)-1H-imidazole-4-carboxylic acid 
• 1422682-35-6 ethyl 2-(3-fluorophenyl)-1H-imidazole-4-carboxylate 
• 1630015-65-4 3-(3-fluorophenyl)-5-(7-indazolyl)-1,2,4-oxadiazole 
• 1154180-95-6 3-(3-fluoro-phenyl)-5-(2-amino-3-methylphenyl)-1,2,4-oxadiazole 
• 1338667-43-8 3-(3-fluorophenyl)-5-(3-indazolyl)-1,2,4-oxadiazole 
• 1630015-53-0 3-(3-fluorophenyl)-5-(4-indazolyl)-1,2,4-oxadiazole 
• 1630015-57-4 3-(3-fluorophenyl)-5-(5-indazolyl)-1,2,4-oxadiazole 
• 1630015-61-0 3-(3-fluorophenyl)-5-(6-indazolyl)-1,2,4-oxadiazole 
• 1630015-69-8 3-(3-fluoro-phenyl)-5-(2-nitro-3-methylphenyl)-1,2,4-oxadiazole 
• 601484-33-7 5-(chloromethyl)-3-(3-fluorophenyl)-1,2,4-oxadiazole 
• 844498-76-6 C₉H₈ClFN₂O₂ 
• 75908-00-8 5-(3,3-Dinitrobutyl)-3-(3-fluorophenyl)-1,2,4-oxadiazole 

Relevant academic research and scientific papers

Novel O-acylated amidoximes and substituted 1,2,4-oxadiazoles synthesised from (+)-ketopinic acid possessing potent virus-inhibiting activity against phylogenetically distinct influenza A viruses

This article describes the synthesis and antiviral activity evaluation of new substituted 1,2,4-oxadiazoles containing a bicyclic substituent at position 5 of the heterocycle and O-acylated amidoximes as precursors for their synthesis. New compounds were

Design, synthesis, and biological evaluation of 1,2,4-oxadiazole-containing pyrazolo[3,4-b]pyridinones as a new series of AMPKɑ1β1γ1 activators

Adenosine monophosphate-activated protein kinase (AMPK) plays a key role in maintaining whole-body homeostasis and has been regarded as a therapeutic target for the treatment of diabetic nephropathy (DN). Herein, a series of 1,2,4-oxadiazole-containing py

KCNT1 INHIBITORS AND METHODS OF USE

The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.

KCNT1 INHIBITORS AND METHODS OF USE

The present invention is directed to, in part, compounds and compositions useful for preventing and/or treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene (e.g., KCNT1). Methods of treating a neurological disease or disorder, a disease or condition relating to excessive neuronal excitability, and/or a gain-of-function mutation in a gene such as KCNT1 are also provided herein.

Design, synthesis and biological activities of piperidine-spirooxadiazole derivatives as α7 nicotinic receptor antagonists

α: 7 nicotinic acetylcholine receptors (nAChRs) expressed in the nervous and immune systems have been suggested to play important roles in the control of inflammation. However, the lack of antagonist tools specifically inhibiting α7 nAChR impedes the validation of the channel as therapeutic target. To discover a selective α7 antagonist, we started a pharmacophore-based virtual screening and identified a piperidine-spirooxadiazole derivative T761–0184 that acts as a α7 antagonist. A series of novel piperidine-spirooxadiazole derivatives were subsequently synthesized and evaluated using two-electrode voltage clamp (TEVC) assay in Xenopus oocytes. Lead compounds from two series inhibited α7 with their IC50 values ranging from 3.3 μM to 13.7 μM. Compound B10 exhibited α7 selectivity over other α4β2 and α3β4 nAChR subtypes. The analysis of structure-activity relationship (SAR) provides valuable insights for further development of selective α7 nAChR antagonists.

Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation

α7 nicotinic acetylcholine receptors (nAChRs) are relevant therapeutic targets for a variety of disorders including neurodegeneration, cognitive impairment, and inflammation. Although traditionally identified as an ionotropic receptor, the α7 subtype showed metabotropic-like functions, mainly linked to the modulation of immune responses. In the present work, we investigated the structure-activity relationships in a set of novel α7 ligands incorporating the 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazole scaffold, i.e. derivatives 21a-34a and 21b-34b, aiming to identify the structural requirements able to preferentially trigger one of the two activation modes of this receptor subtype. The new compounds were characterized as partial and silent α7 nAChR agonists in electrophysiological assays, which allowed to assess the contribution of the different groups towards the final pharmacological profile. Overall, modifications of the selected structural backbone mainly afforded partial agonists, among them tertiary bases 27a-33a, whereas additional hydrogen-bond acceptor groups in permanently charged ligands, such as 29b and 31b, favored a silent desensitizing profile at the α7 nAChR.

COMPOUNDS AND USES THEREOF

The present invention features compounds useful in the treatment of neurological disorders. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing neurological disorders.

Cobalt(III)-Catalyzed Oxadiazole-Directed C-H Activation for the Synthesis of 1-Aminoisoquinolines

Aromatic heterocycles have been identified as effective directing groups (DGs) in C-H functionalization but can be retained as undesired bulky substituents in the final products. Herein, we report a Co(III)-catalyzed 1-aminoisoquinoline synthesis strategy based on oxadiazole-directed aromatic C-H coupling with alkynes and a subsequent redox-neutral C-N cyclization reaction. This labile N-O bond-based protocol has allowed the toleration of a broad range of functional groups.

One-pot synthesis of amidoxime via Pd-catalyzed cyanation and amidoximation

A novel "one-pot" reaction was developed for the synthesis of aryl or heteroaryl-substituted amidoxime compounds containing various functional groups. Fluorescence titration experiments coupled with theoretical analysis revealed that the steric hindrance and electronic effects of substituents influence the binding ability of the amidoxime compounds to uranyl ions. This journal is

Design and discovery of 5-hydroxy-6-oxo-1,6-dihydropyrimidine-4-carboxamide inhibitors of HIV-1 integrase

Raltegravir (RAL) is a first clinically approved integrase (IN) inhibitor for the treatment of HIV but rapid mutation of the virus has led to chemo-resistant strains. Therefore, there is a medical need to develop new IN inhibitors to overcome drug resista