864437-46-7

Upstream product

• 122-78-1 phenylacetaldehyde 
• 864437-28-5 methyl 2-amino-5-benzylthiazole-4-carboxylate 
• 864437-38-7 methyl 5-benzylthiazole-4-carboxylate 

Relevant academic research and scientific papers

Imidazole-2-carboxylic acid metal beta-lactamase inhibitor as well as preparation method and application thereof

The invention provides an imidazole-2-carboxylic acid metal beta-lactamase inhibitor as well as a preparation method and application thereof, and belongs to the field of medicinal chemistry. The structure of the metal beta-lactamase inhibitor is shown as a formula I. The compound provided by the invention has a good inhibition effect on metal beta-lactamase. Particularly, compared with the compound 1, the compound 3, the compound 5, the compound 13, the compound 18, the compound 17-a-19-a, the compound 22-a, the compound 24-a-26-a, the compound 29-a, the compound 30-a, the compound 34-a, the compound 36-a and the compound 37-a have the advantage that the inhibition effect on MBL enzyme VIM-2 is obviously improved. In addition, the compound disclosed by the invention can reverse the drug resistance of drug-resistant bacteria to meropenem, and the antibacterial effect of meropenem is remarkably improved. The compound provided by the invention can be used for preparing a metal beta-lactamase inhibitor and an antibacterial combined drug, and has a wide application prospect.

Identification of potent type I MetAP inhibitors by simple bioisosteric replacement. Part 1: Synthesis and preliminary SAR studies of thiazole-4-carboxylic acid thiazol-2-ylamide derivatives

A series of thiazole-4-carboxylic acid thiazol-2-ylamide (TCAT, 4) derivatives were designed and synthesized according to simple bioisosteric replacement from previously reported pyridine-2-carboxylic acid thiazol-2-ylamide (PCAT) MetAP inhibitors. The preliminary SAR studies demonstrated that these TCAT series of compounds showed different activity and selectivity compared with those of the corresponding PCAT compounds. These findings provide useful information for the design and discovery of more potent inhibitors of type I MetAPs.