19064-26-7

Usage

Uses

Used in Pharmaceutical Industry:
DFPCA is used as an intermediate in the synthesis of various drugs and pharmaceutical compounds, contributing to the development of new therapeutic agents with improved efficacy and safety profiles.
Used in Antifungal Applications:
DFPCA is used as an antifungal agent, exhibiting potential activity against various fungal pathogens, which can be beneficial in treating fungal infections and developing new antifungal drugs.
Used in Antibacterial Applications:
DFPCA is used as an antibacterial agent, showing potential activity against various bacterial strains, which can be advantageous in treating bacterial infections and developing new antibacterial drugs.
Used in Drug Development:
DFPCA is used as a precursor in the development of new therapeutic agents, enabling the creation of innovative drugs with enhanced efficacy and safety profiles for various medical applications.

InChI:InChI=1/C8H6ClF2NO/c9-4-7(13)12-8-5(10)2-1-3-6(8)11/h1-3H,4H2,(H,12,13)

Upstream product

• 5509-65-9 2,6-difluoroaniline 
• 79-04-9 chloroacetyl chloride 

Downstream Products

• 1017590-13-4 C₁₂H₁₂F₂N₂O₂S 
• 1236306-23-2 N-(2,6-difluorophenyl)-2-(4-(4-(pyridin-4-ylmethyl)phthalazin-1-yl)piperazin-1-yl)acetamide 
• 1236306-36-7 N-(2,6-difluorophenyl)-2-(4-(4-benzylphthalazin-1-yl)piperazin-1-yl)acetamide 

Relevant academic research and scientific papers

Synthesis and Biological Evaluation of Dithiobisacetamides as Novel Urease Inhibitors

Thirty-eight disulfides containing N-arylacetamide were designed and synthesized in an effort to develop novel urease inhibitors. Biological evaluation revealed that some of the synthetic compounds exhibited strong inhibitory potency against both cell-free urease and urease in intact cell with low cytotoxicity to mammalian cells even at concentration up to 250 μM. Of note, 2,2′-dithiobis(N-(2-fluorophenyl)acetamide) (d7), 2,2′-dithiobis(N-(3,5-difluorophenyl)acetamide) (d24), and 2,2′-dithiobis(N-(3-fluorophenyl)acetamide) (d8) were here identified as the most active inhibitors with IC50 of 0.074, 0.44, and 0.81 μM, showing 32- to 355-fold higher potency than the positive control acetohydroxamic acid. These disulfides were confirmed to bind urease without covalent modification of the cysteine residue and to inhibit urease reversibly with a mixed inhibition mechanism. They also showed very good anti-Helicobacter pylori activities with d8 showing a comparable potency to the clinical used drug amoxicillin. The impressive in vitro biological profile indicated their immense potential as therapeutic agents to tackle H. pylori caused infections.

Halogen-substituted triazolethioacetamides as a potent skeleton for the development of metallo-β-lactamase inhibitors

Metallo-β-lactamases (MβLs) are the target enzymes of β-lactam antibiotic resistance, and there are no effective inhibitors against MβLs available for clinic so far. In this study, thirteen halogen-substituted triazolethioacetamides were designed and synthesized as a potent skeleton of MβLs inhibitors. All the compounds displayed inhibitory activity against ImiS with an IC50 value range of 0.032–15.64 μM except 7. The chlorine substituted compounds (1, 2 and 3) inhibited NDM-1 with an IC50 value of less than 0.96 μM, and the fluorine substituted 12 and 13 inhibited VIM-2 with IC50 values of 38.9 and 2.8 μM, respectively. However, none of the triazolethioacetamides exhibited activity against L1 at inhibitor concentrations of up to 1 mM. Enzyme inhibition kinetics revealed that 9 and 13 are mixed inhibitors for ImiS with Ki values of 0.074 and 0.27μM using imipenem as the substrate. Docking studies showed that 1 and 9, which have the highest inhibitory activity against ImiS, fit the binding site of CphA as a replacement of ImiS via stable interactions between the triazole group bridging ASP120 and hydroxyl group bridging ASN233.

Synthesis and antitumor activities of novel 1,4-disubstituted phthalazine derivatives

In an attempt to develop potent and selective antitumor agents,a series of novel 1,4-disubstituted phthalazine derivatives was designed and synthesized. All the prepared compounds were screened for their cytotoxic activities against A549,HT-29 and MDA-MB-231 cell lines in vitro. Among them,seven compounds (7a7e,7j and 7i) displayed excellent selectivity for MDA-MB-231 cells with IC50 values in the nM range,a desirable range for pharmacological testing. The most promising compound,7a (IC50 = 3.79 μ M,2.32 μ M,0.84 nM),was 5.6-,10.8-and 6.9 × 104-times more active than PTK-787 (IC50 = 21.16 μ M,22.11 μ M,57.72 μ M),respectively.

FUSED RING COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES

The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.