1194056-93-3

Upstream product

• 1844898-16-3 (2S,3S)-3-hydroxy-pyrrolidine-2-carboxylic acid methyl ester hydrochloride 
• 1194059-15-8 1-benzyl 2-methyl (2S,3R)-3-azido-pyrrolidine-1,2-dicarboxylate 
• 1194059-14-7 1-benzyl 2-methyl (2S,3S)-3-((3-nitrophenyl)sulfonyloxy)pyrrolidine-1,2-dicarboxylate 
• 496841-04-4 methyl (2S,3S)-3-hydroxypyrrolidine-2-carboxylate 
• 4298-08-2 trans-3-hydroxy-L-proline 

Downstream Products

• 1194059-19-2 benzyl (2R,3R)-3-((benzyloxy)carbonylamino)-2-azidomethyl-pyrrolidine-1-carboxylate 
• 1194059-20-5 benzyl (2R,3R)-3-((benzyloxy)carbonylamino)-2-((tert-butoxycarbonylamino)methyl)-pyrrolidine-1-carboxylate 
• 1194059-18-1 benzyl (2S,3R)-3-((benzyloxy)carbonylamino)-2-(((4-methylphenyl)sulfonyl)oxymethyl)-pyrrolidine-1-carboxylate 

Relevant academic research and scientific papers

Synthesis and Microbiological Evaluation of Novel Tetracyclic Fluoroquinolones

Conformationally constrained tetracyclic fluoroquinolones (FQs) were synthesized and profiled for their microbiological spectrum. The installation of a seven-membered ring between the pyrrolidine substituents and the C8 position on the FQ core scaffold resulted in a remarkable enhancement of microbiological potency toward both Gram-positive and Gram-negative bacteria. Focused optimization of seven-membered ring composition, stereochemistry, and amine placement led to the discovery of the two lead compounds that were selected for further progression.

ANTIBACTERIAL FLUOROQUINOLONE ANALOGS

Compounds having antibacterial activity are disclosed. The compunds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein A, B, D, E, G, R1, R2, R3, R4, R5, R6 and R7 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.