58660-74-5

Upstream product

• 58660-59-6 Diethyl cyclohexanone-2,4-dicarboxylic ester 
• 63579-89-5 triethyl pentane-1,3,5-tricarboxylate 
• 1312919-56-4 diethyl 4-(benzylamino)cyclohexane-1,3-dicarboxylate 
• 339555-27-0 diethyl 4-(hydroxyimino)cyclohexane-1,3-dicarboxylate 

Downstream Products

• 1312919-63-3 diethyl 4-(6-butoxynaphthalene-2-sulfonamido)cyclohexane-1,3-dicarboxylate 
• 1312919-81-5 4-(6-butoxynaphthalene-2-sulfonamido)cyclohexane-1,3-dicarboxylic acid 
• 1312919-72-4 diethyl 4-(6-(4-cyano-2-fluorobenzyloxy)naphthalene-2-sulfonamido)cyclohexane-1,3-dicarboxylate 
• 1312919-90-6 4-(6-(4-cyano-2-fluorobenzyloxy)naphthalene-2-sulfonamido)cyclohexane-1,3-dicarboxylic acid 

Relevant academic research and scientific papers

Second-generation sulfonamide inhibitors of d-glutamic acid-adding enzyme: Activity optimisation with conformationally rigid analogues of d-glutamic acid

d-Glutamic acid-adding enzyme (MurD) catalyses the essential addition of d-glutamic acid to the cytoplasmic peptidoglycan precursor UDP-N-acetylmuramoyl- l-alanine, and as such it represents an important antibacterial drug-discovery target enzyme. Based on a series of naphthalene-N-sulfonyl-d-Glu derivatives synthesised recently, we synthesised two series of new, optimised sulfonamide inhibitors of MurD that incorporate rigidified mimetics of d-Glu. The compounds that contained either constrained d-Glu or related rigid d-Glu mimetics showed significantly better inhibitory activities than the parent compounds, thereby confirming the advantage of molecular rigidisation in the design of MurD inhibitors. The binding modes of the best inhibitors were examined with high-resolution NMR spectroscopy and X-ray crystallography. We have solved a new crystal structure of the complex of MurD with an inhibitor bearing a 4-aminocyclohexane-1,3-dicarboxyl moiety. These data provide an additional step towards the development of sulfonamide inhibitors with potential antibacterial activities.

BENZAMIDINE DERIVATIVES SUBSTITUTED BY CYCLIC AMINO ACID AND CYCLIC HYDROXY ACID DERIVATIVES AND THEIR USE AS ANTI-COAGULANTS

This invention is directed to benzamidine derivatives substituted by cyclic amino acid and cyclic hydroxy acid derivatives which are useful as anti-coagulants. This invention is also directed to pharmaceutical compositions containing the compounds of the invention, and methods of using the compounds to treat disease-states characterized by thrombotic activity.