556801-47-9

Upstream product

• 104-92-7 1-bromo-4-methoxy-benzene 
• 154590-33-7 1-(2-fluoro-4-nitrophenyl)piperazine 
• 38212-30-5 4-(4-methoxyphenyl)piperazine 
• 369-34-6 3,4-difluoronitrobenzene 

Downstream Products

• 1427177-61-4 4-(3-fluoro-4-(4-(4-methoxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one 
• 1427177-62-5 1-(sec-butyl)-4-(3-fluoro-4-(4-(4-methoxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one 
• 1427177-63-6 1-(sec-butyl)-4-(3-fluoro-4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one 
• 1427177-50-1 4-(4-(4-(4-(((2S,4R)-2-((1H-1,2,4-triazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methoxy)phenyl)piperazin-1-yl)-3-fluorophenyl)-2-(sec-butyl)-2,4-dihydro-3H-1,2,4-triazol-3-one 
• 1427177-60-3 N-(3-fluoro-4-(4-(4-methoxyphenyl)piperazin-1-yl)phenyl)hydrazinecarboxamide 
• 1427177-59-0 phenyl (3-fluoro-4-(4-(4-methoxyphenyl)piperazin-1-yl)phenyl)carbamate 
• 556801-49-1 {3-fluoro-4-[4-(4-methoxy-phenyl)-piperazin-1-yl]-phenyl}-carbamic acid benzyl ester 
• 465520-05-2 (R)-3-{3-Fluoro-4-[4-(4-methoxy-phenyl)-piperazin-1-yl]-phenyl}-5-hydroxymethyl-oxazolidin-2-one 
• 556801-48-0 3-fluoro-4-(4-(4-methoxyphenyl)piperazin-1-yl)aniline 

Relevant academic research and scientific papers

Benzofuroxan Derivatives as Potent Agents against Multidrug-Resistant Mycobacterium tuberculosis

Tuberculosis (TB) is currently the leading cause of death related to infectious diseases worldwide, as reported by the World Health Organization. Moreover, the increasing number of multidrug-resistant tuberculosis (MDR-TB) cases has alarmed health agencies, warranting extensive efforts to discover novel drugs that are effective and also safe. In this study, 23 new compounds were synthesized and evaluated in vitro against the drug-resistant strains of M. tuberculosis. The compound 6-((3-fluoro-4-thiomorpholinophenyl)carbamoyl)benzo[c][1,2,5]oxadiazole 1-N-oxide (5 b) was particularly remarkable in this regard as it demonstrated MIC90 values below 0.28 μM against all the MDR strains evaluated, thus suggesting that this compound might have a different mechanism of action. Benzofuroxans are an attractive new class of anti-TB agents, exemplified by compound 5 b, with excellent potency against the replicating and drug-resistant strains of M. tuberculosis.

Design and Synthesis of Tetrazole- And Pyridine-Containing Itraconazole Analogs as Potent Angiogenesis Inhibitors

Itraconazole, a widely used antifungal drug, was found to possess antiangiogenic activity and is currently undergoing multiple clinical trials for the treatment of different types of cancer. However, it suffers from extremely low solubility and strong interactions with many drugs through inhibition of CYP3A4, limiting its potential as a new antiangiogenic and anticancer drug. To address these issues, a series of analogs in which the phenyl group is replaced with pyridine or fluorine-substituted benzene was synthesized. Among them the pyridine- and tetrazole-containing compound 24 has significantly improved solubility and reduced CYP3A4 inhibition compared to itraconazole. Similar to itraconazole, compound 24 inhibited the AMPK/mTOR signaling axis and the glycosylation of VEGFR2. It also induced cholesterol accumulation in the endolysosome and demonstrated binding to the sterol-sensing domain of NPC1 in a simulation study. These results suggested that compound 24 may serve as an attractive candidate for the development of a new generation of antiangiogenic drug.

ITRACONAZOLE ANALOGS AND USE THEREOF

Provided herein are Itraconazole analogs. Also provided herein are methods of inhibition of Hedgehog pathway, vascular endothelial growth factor receptor 2 (VEGFR2) glycosylation, angiogenesis and treatment of disease with Itraconazole analogs.

Synthesis and antibacterial activity of linezolid analogues

Several new compounds of oxazolidinone class were designed and synthesized referring to the structure-activity relationship studies and the synthesis of Linezolid, and their antibacterial activity was studied.