960061-69-2

Upstream product

• 1160960-61-1 C₅₁H₄₈N₁₂O₁₁S₆ 
• 960062-64-0 C₄₈H₄₄N₁₂O₉S₆ 

Downstream Products

• 960061-70-5 C₅₂H₅₃N₁₃O₉S₆ 
• 960062-15-1 C₅₃H₅₃N₁₃O₁₁S₆ 
• 960062-70-8 C₅₇H₅₉N₁₃O₁₁S₆ 
• 1277183-93-3 C₄₅H₄₄N₁₂O₈S₅ 
• 960061-72-7 C₄₉H₄₇N₁₃O₈S₆ 
• 960061-79-4 C₅₀H₄₉N₁₃O₁₀S₇ 
• 960061-78-3 C₄₈H₄₇N₁₃O₉S₇ 
• 960061-68-1 C₄₇H₄₅N₁₃O₇S₆ 
• 1160961-02-3 C₅₅H₅₆N₁₄O₁₀S₆ 
• 1160960-65-5 C₅₆H₅₇N₁₃O₁₁S₆ 
• 1160959-70-5 C₆₀H₆₃N₁₃O₁₄S₆ 
• 1160960-62-2 C₅₈H₆₁N₁₃O₁₃S₆ 
• 1160959-63-6 C₆₀H₅₈N₁₄O₁₃S₆ 
• 1160959-76-1 C₅₈H₅₉N₁₃O₁₃S₆ 

Relevant academic research and scientific papers

Discovery of LFF571: An investigational agent for Clostridium difficile infection

Clostridium difficile (C. difficile) is a Gram positive, anaerobic bacterium that infects the lumen of the large intestine and produces toxins. This results in a range of syndromes from mild diarrhea to severe toxic megacolon and death. Alarmingly, the prevalence and severity of C. difficile infection are increasing; thus, associated morbidity and mortality rates are rising. 4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for the treatment of C. difficile infection. The medicinal chemistry effort focused on enhancing aqueous solubility relative to that of the natural product and previous development candidates (2, 3) and improving antibacterial activity. Structure-activity relationships, cocrystallographic interactions, pharmacokinetics, and efficacy in animal models of infection were characterized. These studies identified a series of dicarboxylic acid derivatives, which enhanced solubility/efficacy profile by several orders of magnitude compared to previously studied compounds and led to the selection of LFF571 (4) as an investigational new drug for treating C. difficile infection.

4-Aminothiazolyl analogues of GE2270 A: Antibacterial lead finding

4-Aminothiazolyl analogues of the antibacterial natural product GE2270 A (1) were designed, synthesized, and evaluated for Gram positive bacteria growth inhibition. The aminothiazole-based chemical template was evaluated for chemical stability, and its de

Antibacterial optimization of 4-aminothiazolyl analogues of the natural product GE2270 A: Identification of the cycloalkylcarboxylic acids

4-Aminothiazolyl analogues of the antibiotic natural product GE2270 A (1) were designed, synthesized, and optimized for their activity against Gram positive bacterial infections. Optimization efforts focused on improving the physicochemical properties (e.g., aqueous solubility and chemical stability) of the 4-aminothiazolyl natural product template while improving the in vitro and in vivo antibacterial activity. Structure-activity relationships were defined, and the solubility and efficacy profiles were improved over those of previous analogues and 1. These studies identified novel, potent, soluble, and efficacious elongation factor-Tu inhibitors, which bear cycloalkylcarboxylic acid side chains, and culminated in the selection of development candidates amide 48 and urethane 58.

Aminothiazoles and their Uses

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases particularly bacterial infections.

EFTU INHIBITORS OR AMINOTHIAZOLES AND THEIR USES

The present application describes organic compounds that are useful for the treatment, prevention and/or amelioration of diseases.