65136-87-0

Upstream product

• 121-98-2 methyl 4-methoxybenzoate 
• 107-15-3 ethylenediamine 
• 701-53-1 p-methoxybenzoyl fluoride 
• 18299-54-2 ethylenediamine hydrochloride 
• 100-07-2 4-methoxy-benzoyl chloride 
• 100-09-4 4-methoxybenzoic acid 
• 1227301-63-4 N-tert-butoxycarbonyl-N'-(4-methoxybenzoyl)ethylenediamine 
• 4231-69-0 1-(4-methoxybenzoyl)-1H-1,2,3-benzotriazole 
• 57260-73-8 N-BOC-1,2-diaminoethane 
• 1290636-90-6 C₁₄H₁₀ClNO₅ 
• 1261242-15-2 C₁₈H₂₀N₂O₄ 

Downstream Products

• 65111-65-1 1β-oxo-6β-(2-phenyl-acetylamino)-1λ⁴-penicillanic acid 2-(4-methoxy-benzoylamino)-ethylamide 
• 866109-37-7 N-[2-(4-methoxybenzoylamino)ethyl]-3,4-dimethoxy-5-nitrobenzamide 
• 1261242-30-1 N-(2-((4-(6-(4-fluorophenyl)imidazo[2,1-b]thiazol-5-yl)pyrimidin-2-yl)amino)ethyl)-4-methoxybenzamide 
• 1407190-08-2 N-(2-diethylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 1407190-09-3 N-(2-dipropylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 1407190-10-6 N-(2-dibutylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 32276-18-9 N-(2-(diethylamino)ethyl)-4-methoxy-benzamide 
• 1407190-11-7 N-(2-dipentylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 1407189-95-0 N-(2-(dipentylamino)ethyl)-4-methoxy-benzamide 
• 1407190-12-8 N-(2-dihexylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 1407189-96-1 N-(2-(dihexylamino)ethyl)-4-methoxy-benzamide 
• 1407189-97-2 N-(2-(diheptylamino)ethyl)-4-methoxy-benzamide 
• 1407190-14-0 N-(2-dioctylamino-2-methyl-ethyl)-4-methoxy-benzamide 
• 1407189-98-3 N-(2-(dioctylamino)ethyl)-4-methoxy-benzamide 

Relevant academic research and scientific papers

Toll-like receptor-7 small molecule inhibitor and preparation method thereof

The invention belongs to the field of chemical small molecules, and particularly relates to a Toll-like receptor-7 small molecule inhibitor. The invention provides the Toll-like receptor-7 small molecule inhibitor, which takes a co-inhibitor of TLR7 and TLR8 obtained by screening as a research object, realizes selective regulation and control of TLR7 and TLR8 through the research on the structureoptimization and structure-activity relationship (SAR) of a parent compound, and further develops a high-efficiency, non-toxic and specific small molecule inhibitor with certain selectivity on TLR 7.The TLR7 small molecule inhibitor has a certain effect and potential medicinal value in autoimmune diseases (systemic lupus erythematosus).

Synthesis of sp3-rich chemical libraries based upon 1,2-diazetidines

A strategy for the creation of sp3-rich, non-planar scaffolds for drug discovery is described. Stereocontrolled ring opening of homochiral 1,2-epoxides by hydrazine monohydrate followed by selective protection of both nitrogen atoms and Mitsuno

N-Acylbenzotriazole: convenient approach for protecting group-free monoacylation of symmetric diamines

Abstract: An efficient green route for monoacylation of aromatic diamines, namely o-phenylenediamine and p-phenylenediamine and aliphatic diamines ethylenediamine and piperazine using N-acylbenzotriazoles (NABs) in n-butanol was developed. The new protocol does not require prior selective protection of the diamine and comprises simple conditions, short reaction times, an easy work up as well as high isolated yields (69–94%). Moreover, the method described herein enable stepwise acylation of aliphatic diamines such as ethylenediamine and piperazine with two different N-acylbenzotriazoles affording unsymmetrical substituted diamines that can be used for construction of pharmaceutically important targets such as drugs, foldamers, and drug conjugates. Graphic abstract: [Figure not available: see fulltext.]

Imidazothiazole-based potent inhibitors of V600E-B-RAF kinase with promising anti-melanoma activity: biological and computational studies

A series of imidazothiazole derivatives possessing potential activity against melanoma cells were investigated for molecular mechanism of action. The target compounds were tested against V600E-B-RAF and RAF1 kinases. Compound 1zb is the most potent agains

Biofilm inhibition and anti-Candida activity of a cationic lipo-benzamide molecule with twin-nonyl chain

A series of cationic lipo-benzamide compounds with varying lengths of hydrocarbon chains (C2M–C18M) were evaluated for anti-Candida activity. Four compounds harbouring 8–11 hydrocarbon chains demonstrated concentration-dependent inhibition of fungal cell

TARGETING AMINOACID LIPIDS

The present invention is directed to carrier systems comprising ether-lipids conjugated to one or more bioactive ligands and exposed on the surface of the carrier system for use in targeted delivery and/or antigen display systems. Optionally one or more further bioactive agents may be encapsulated or embedded within or attached to or adsorbed onto the carrier system. The present invention is further directed to methods of their preparation and their uses in medical applications, such as targeted delivery of bioactive agents to specific tissues or cells and antigen display systems for the study, diagnosis, and treatment of traits, diseases and conditions that respond to said bioactive agents.

A systematic exploration of the effects of flexibility and basicity on sigma (σ) receptor binding in a series of substituted diamines

The sigma-1 receptor (S1R) has attracted a great deal of attention as a prospective drug target due to its involvement in numerous neurological disorders and, more recently, for its therapeutic potential in neuropathic pain. As there was no crystal structure of this membrane-bound protein reported until 2016, ligand generation was driven by pharmacophore refinements to the general model suggested by Glennon and co-workers. The generalised S1R pharmacophore comprises a central region where a basic amino group is preferred, flanked by two hydrophobic groups. Guided by this pharmacophore, S1R ligands containing piperazines, piperazinones, and ethylenediamines have been developed. In the current work, we systematically deconstructed the piperazine core of a prototypic piperazine S1R ligand (vide infra) developed in our laboratories. Although we did not improve the affinity at the S1R compared to the lead, we identified several features important for affinity and selectivity. These included at least one basic nitrogen atom, conformational flexibility and, for S1R, a secondary or tertiary amine group proximal to the anisole. Furthermore, S2R selectivity can be tailored with functional group modifications of the N-atom proximal to the anisole.

Broad-spectrum antiproliferative activity of a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives

This article described the synthesis and in vitro antiproliferative activities a series of 6-(4-fluorophenyl)-5-(2-substituted pyrimidin-4-yl)imidazo[2,1-b]thiazole derivatives. The nine target compounds were tested for in vitro antitumor effect against a

Expanding the structural diversity of Bcr-Abl inhibitors: Dibenzoylpiperazin incorporated with 1 H -indazol-3-amine

A series of N,N'-dibenzoylpiperazine derivatives incorporated with 1H-indazol-3-amine have been designed, synthesized and evaluated as novel Bcr-Abl inhibitors. Several title compounds exhibited potent inhibitory activity against Bcr-Abl wild type as well as T315I mutant. Two compounds, 11a and 12c, strongly suppressed the activity of native and mutant Bcr-Abl. In particular, 11a exhibited comparable potency with that of Imatinib. It potently inhibited both Bcr-AblWT and Bcr-AblT315I with IC50 values of 0.014 μM and 0.45 μM, respectively. Furthermore, compound 11a also inhibited the proliferation of K562 leukemia cancer cells. Therefore, it could serve as promising lead compound for further optimization of Bcr-AblWT and Bcr-AblT315I inhibitors.

ANTIMICROBIAL COMPOUNDS

The invention provides compounds for use in treating microbial infection in an animal. Example compounds include Pyridin-3-ylmethyl (4-((2-aminophenyl)- carbamoyl)benzyl)carbamate ("Entinostat"). The compounds can act via induction of the innate antimicrobial peptide defense system, and stimulation of autophagy.