Benzimidazole scaffold based hybrid molecules for various inflammatory targets: Synthesis and evaluation was written by Kaur, Gaganpreet;Silakari, Om. And the article was included in Bioorganic Chemistry in 2018.Recommanded Product: 1-(Chloromethyl)-3-methylbenzene This article mentions the following:
Designing of hybrid drugs with specific multitarget profile is a promising line of attack against inflammation. In light of this, a series of benzimidazole scaffold based hybrid mols. were designed by integrating benzimidazoles (containing pharmacophoric elements for COXs and LOXs inhibitors) with phthalimide subunit of thalidomide (pharmacophore element for TNF-α inhibitor) under one construct via mol. hybridization strategy. The designed mols. were synthesized and evaluated for their inhibitory activity against COXs (COX-1, COX-2), LOXs (5-LOX, 15-LOX) enzymes as well as TNF-α inhibitory effect. The results revealed that, compounds (3a-l) obtained showed inhibition in submicromolar range against COXs and LOXs targets whereas milder inhibitory activity was obtained against lipopolysaccharides (LPS)-induced TNF-α secretion by murine macrophage-like cells (RAW264.7). Within this class of compounds, I emerged as having alluring multiple inhibitory effects on set of COX-1/2 and 5-/15-LOX enzymes (COX-1 IC50 = 9.85 μM; COX-2 IC50 = 1.00 μM; SI = 9.85; 5-LOX IC50 = 0.32 μM; 15-LOX IC50 = 1.02 μM) in conjunction with a good anti-inflammatory and analgesic activities. Addnl., compound I showed gastrointestinal safety with reduced lipid peroxidation Docking results of compound I with COX-2 and 5-LOX were also consistent with the in vivo anti-inflammatory results. In the experiment, the researchers used many compounds, for example, 1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9Recommanded Product: 1-(Chloromethyl)-3-methylbenzene).
1-(Chloromethyl)-3-methylbenzene (cas: 620-19-9) belongs to organic chlorides. Organochlorines are organic compounds having multiple chlorine atoms. They were the first synthetic pesticides that were used in agriculture. They are resistant to most microbial and chemical degradations. Alkyl chlorides readily react with amines to give substituted amines. Alkyl chlorides are substituted by softer halides such as the iodide in the Finkelstein reaction.Recommanded Product: 1-(Chloromethyl)-3-methylbenzene
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics