27737-56-0

Upstream product

• 27737-55-9 4-benzyloxy-1H-indole-2-carboxylic acid ethyl ester 
• 90-02-8 salicylaldehyde 
• 5896-17-3 2-(phenylmethoxy)benzaldehyde 
• 95264-30-5 (Z)-ethyl 2-azido-3-(2-(benzyloxy)phenyl)acrylate 

Downstream Products

• 863251-51-8 4-(2-nitro-phenoxy)-1H-indole-2-carboxylic acid ethyl ester 
• 863249-51-8 4-(3,5-difluoro-2-nitro-phenoxy)-1H-indole-2-carboxylic acid ethyl ester 
• 863251-75-6 4-(4-fluoro-2-nitro-phenoxy)-1H-indole-2-carboxylic acid ethyl ester 
• 863251-56-3 4-(5-methyl-2-nitro-phenoxy)-1H-indole-2-carboxylic acid ethyl ester 
• 863251-63-2 C₁₈H₁₆N₂O₅ 
• 27737-55-9 4-benzyloxy-1H-indole-2-carboxylic acid ethyl ester 

Relevant academic research and scientific papers

Synthesis of five libraries of 6,5-fused heterocycles to establish the importance of the heterocyclic core for antiplasmodial activity

Research has indicated that N-myristoyl transferase, an enzyme that catalyzes the addition of a myristate group to the N-terminal glycine residues of proteins, is involved in the myristoylation of more than 100 proteins. Genetic knockdown of the enzyme proved detrimental for the viability of the parasite P. knowlesi. A crystal structure of P. vivax N-myristoyl transferase (pvNMT), containing a 3-methyl benzofuran ligand has made it possible to assess key amino acid residue-ligand interactions. We synthesized five libraries of 6,5-fused heterocycles to establish the importance of the heterocycles as core scaffolds, as well as introduced various aromatic amides and esters to determine which carbonylic group affects the potency of each heterocyclic antiplasmodial agent.

Design, synthesis and antifungal activity of isosteric analogues of benzoheterocyclic N-myristoyltransferase inhibitors

N-myristoyltransferase (NMT) has been a promising new target for the design of novel antifungal agents with new mode of action. A series of benzoxazole and indole derivatives were designed and synthesized as isosteric analogues of benzoheterocyclic NMT Inhibitors. In vitro antifungal assay indicated that the benzoxazole derivatives were far more potent than the indoles. Molecular docking studies revealed that the hydrogen bonding interaction between the benzoheterocyclic core and NMT might be essential in the orientation of the inhibitor to a proper position. The antifungal activity of benzoxazole derivative 8f was comparable or superior to that of fluconazole, which can serve as a good starting point for further studies of structural diversity of the benzoheterocyclic NMT inhibitors. A series of benzoxazole and indole derivatives were designed and synthesized as isosteric analogues of benzoheterocyclic NMT Inhibitors. The binding mode was investigated by molecular docking.

CHEMOKINE RECEPTOR ANTAGONISTS

A compound of formula (I) or a pharmaceutically acceptable salt or prodrug ester thereof, wherein the variants R, R9, Z, X, Q and Y are defined in the specification.