1093192-05-2

Upstream product

• 1093192-03-0 (S)-3-methyl-3-nitro-2-(((S)-1-phenylethyl)amino)butanoic acid 
• 2627-86-3 (S)-1-phenyl-ethylamine 
• 1093192-04-1 (S)-methyl 3-methyl-3-nitro-2-(((S)-1-phenylethyl)amino)butanoate 

Downstream Products

• 1093192-06-3 (S)-methyl 3-((tert-butoxycarbonyl)amino)-3-methyl-2-(((S)-1-phenylethyl)amino)butanoate 
• 1093192-07-4 (S)-2-amino-3-(tert-butoxycarbonylamino)-3-methylbutanoic acid methyl ester 
• 1363368-24-4 (S)-N-(3-amino-1-(hydroxyamino)-3-methyl-1-oxobutan-2-yI)-4-(4-(2-aminophenyl)buta-1,3-diynyl)benzamide 
• 1363373-88-9 C₂₈H₃₁N₃O₅ 
• 1363373-89-0 C₂₃H₂₃N₃O₃ 

Relevant academic research and scientific papers

COMPOUND ACTING AS ANTIBIOTICS

The present invention provides a novel antibiotic compound represented by the following formula (I), a pharmaceutically acceptable salt thereof, an ester thereof, a prodrug thereof, a solvate thereof, or a deuterated analog thereof, or a stereoisomer thereof. The compound of the present invention exhibits excellent antibacterial activity, especially against Gram bacteria. wherein each group is defined as in the description.

Design, synthesis and structure-activity relationship evaluation of novel LpxC inhibitors as Gram-negative antibacterial agents

LpxC inhibitors are new-type antibacterial agents developed in the last twenty years, mainly against Gram-negative bacteria infections. To develop novel LpxC inhibitors with good antibacterial activities and biological metabolism, we summarized the basic skeleton of reported LpxC inhibitors, designed and synthesized several series of compounds and tested their antibacterial activities against Escherichial coli and Pseudomonas aeruginosa in vitro. Structure-activity relationships have been discussed in this article. The metabolism stability of YDL-2, YDL-5, YDL-8, YDL-14, YDL-20–YDL-23 have been evaluated in liver microsomes, which indicated that the 2-amino isopropyl group may be a preferred structure than the 2-hydroxy ethyl group in the design of LpxC inhibitors.

ETHYNYLBENZENE DERIVATIVES

Disclosed are compounds of formulae (I), (II), and (II)I: and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R101, L, D, Q, Y, X, and Z are defined herein. These compounds are useful for treating Gram-negative bacteria infections.

ANTIBACTERIAL AGENTS

Antibacterial compounds of formula (I) are provided, as well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of such compounds.