Salicylanilide

Salicylanilides are a group of compounds with a wide range of biological activities including antiviral potency, antibacterial (including antimycobacterial) and antifungal activities.

Synthesis of p-O-Alkyl Salicylanilide Derivatives as Novel EGFR Inhibitors.[Pubmed:26763193]

Drug Dev Res. 2016 Feb;77(1):37-42.

Preclinical Research Epidermal growth factor receptor (EGFR), a validated target for anticancer drugs, plays a critical role in tumorigenesis and tumor development. A series of p-O-alkyl Salicylanilide derivatives were designed and synthesized as novel EGFR inhibitors using a salicylic acid scaffold. A simulated six-membered ring strategy formed through intramolecular hydrogen bonds was employed to mimic the planar quinazoline of the EGFR antagonist, gefitinib. The derived compounds with hydroxyl at the ortho position were more potent than ones with methoxyl group. In particular, compounds 5d and 5b displayed significant EGFR inhibitory (IC50 values = 0.30 and 0.45 muM, respectively) activity as well as potent antiproliferative activity in A431 and HCT-116 tumor cells. These Salicylanilides could be considered as promising lead compounds for developing novel EGFR inhibitors.

Salicylanilide N-monosubstituted carbamates: Synthesis and in vitro antimicrobial activity.[Pubmed:26879856]

Bioorg Med Chem. 2016 Mar 15;24(6):1322-30.

The research of innovative antimicrobial agents represents a cutting edge topic. Hence, we synthesized and characterised novel Salicylanilide N-monosubstituted carbamates. Twenty compounds were evaluated in vitro against eight bacterial strains and eight fungal species. The lowest minimum inhibitory concentrations (MICs) were found to be 0.49 muM. Genus Staphylococcus, including methicillin-resistant Staphylococcus aureus, and fungus Trichophyton mentagrophytes showed uniformly the highest rate of susceptibility, whilst Gram-negative bacteria and most of the fungi were less susceptible. A wide range of carbamates provided comparable or superior in vitro antimicrobial activity in comparison to established drugs. Interestingly, extended-spectrum beta-lactamase producing strain of Klebsiella pneumoniae was inhibited with MICs starting from 31.25 muM. With respect to Staphylococci, 2-[(4-bromophenyl)carbamoyl]-4-chlorophenyl phenylcarbamate exhibited the lowest MIC values (0.98 muM). 2-[(4-Bromophenyl)carbamoyl]-4-chlorophenyl benzylcarbamate showed the widest spectrum of antifungal action. The results indicate that some Salicylanilide carbamates can be considered to be promising candidates for future investigation.

Salicylanilide demonstrates a wide range of biological activities including antiviral potency which can inhibit HIV virus by targeting HIV-1 integrase or reverse transcriptase.

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