347196-12-7

Usage

Uses

Used in Pharmaceutical Industry:
CHEMBRDG-BB 4022584 is used as a potential therapeutic agent for cancer treatment due to its antineoplastic and antiangiogenic properties. It acts as a potent inhibitor of vascular endothelial growth factor receptor 2 (VEGFR-2), a key mediator of angiogenesis, thereby inhibiting the formation of new blood vessels that supply nutrients to tumors.
Used in Cancer Research:
CHEMBRDG-BB 4022584 is used in cancer research to study its potential as an anti-angiogenic drug. Further studies are needed to evaluate its efficacy in inhibiting tumor growth and proliferation, as well as its potential synergistic effects when combined with conventional chemotherapeutic drugs.
Used in Angiogenesis-Related Disease Treatment:
CHEMBRDG-BB 4022584 is used as a potential candidate for the development of drugs targeting angiogenesis-related diseases, such as age-related macular degeneration, rheumatoid arthritis, and psoriasis. Its antiangiogenic properties may help in reducing the abnormal blood vessel growth associated with these conditions.

InChI:InChI=1/C9H9ClFNO/c1-6-7(11)3-2-4-8(6)12-9(13)5-10/h2-4H,5H2,1H3,(H,12,13)

Upstream product

• 443-86-7 3-fluoro-2-methylaniline 
• 79-04-9 chloroacetyl chloride 

Downstream Products

• 952587-04-1 2-cyano-N-(3-fluoro-2-methyl-6-nitrophenyl)acetamide 
• 952587-06-3 7-fluoro-8-methyl-2(1H)-quinoxalinone 
• 952587-08-5 7-fluoro-8-methyl-2-(methyloxy)quinoxaline 
• 485832-96-0 3-fluoro-2-methyl-6-nitroaniline 
• 952587-03-0 2-chloro-N-(3-fluoro-2-methyl-6-nitrophenyl)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.

Design, synthesis, antibacterial and quorum quenching studies of 1,2,5-trisubstituted 1,2,4-triazoles

Abstract: In view of discovering novel bioactive molecules, 1-phenyl-1H-2-(1-aryl-5-methyl-1H-1,2,3-triazol-4-yl)-3-(N-aryl-carbamoylmethylthio)-1,2,4-triazoles (8a–n) were designed and synthesized in good yield. Preliminary antibacterial activity was tested against Chromobacterium violaceum and Xanthomonas campestris pv. Campestris (Xcc). Out of 14 derivatives, compound 8g selectively possessed antibacterial activity against C. violaceum. Further derivatives that possessed an electron-withdrawing group and halogen atoms in N-phenylacetamide moiety were moderately active against Xcc (plant pathogen). After observing the reduction of violacein production through plate assay, compounds 8a, 8c, 8h, 8i and 8m were subjected to quantification of quorum sensing inhibition. Compounds with the electron-withdrawing group in N-phenylacetamide moiety showed admirable activity with > 80% inhibition of violacein. Mainly compound 8c which was inactive against the growth of bacteria were identified as excellent QSI which could be a lead compound for further development. Graphic abstract: One of the best approaches to acquire anti-virulence strategies and new direction for the discovery of antibacterial drugs[Figure not available: see fulltext.]

AZATRICYCLIC COMPOUNDS AND THEIR USE

Tricyclic nitrogen containing compounds),of formula (I) or a pharmaceutically, acceptable salt, solvate and/or N-oxide thereof: and their use as antibacterials.

PYRROLO-QUINOXALINONE DERIVATIVES AS ANTIBACTERIALS

Tricyclic nitrogen containing compounds of the following Formula (I) and their use as antibacterials.

Novel piperidine and piperazine derivatives

The invention provides piperidine and piperazine derivatives of general formula (I), processes for their preparation, pharmaceutical compositions containing them, a process for preparing the pharmaceutical compositions, and their use in therapy