915199-15-4

Upstream product

• 7377-26-6 4-Methoxycarbonylbenzoyl chloride 
• 915199-14-3 4-(azetidin-1-carbonyl)benzoic acid methyl ester 

Downstream Products

• 915199-11-0 1-{[4-(1-azetidinylcarbonyl)phenyl]carbonyl}-4-(4-{[1-(1-methylethyl)-4-piperidinyl]oxy}phenyl)piperidine 

Relevant academic research and scientific papers

Discovery of Novel Thiophene-arylamide Derivatives as DprE1 Inhibitors with Potent Antimycobacterial Activities

In this study, we report the design and synthesis of a series of novel thiophene-arylamide compounds derived from the noncovalent decaprenylphosphoryl-β-d-ribose 2′-epimerase (DprE1) inhibitor TCA1 through a structure-based scaffold hopping strategy. Systematic optimization of the two side chains flanking the thiophene core led to new lead compounds bearing a thiophene-arylamide scaffold with potent antimycobacterial activity and low cytotoxicity. Compounds 23j, 24f, 25a, and 25b exhibited potent in vitro activity against both drug-susceptible (minimum inhibitory concentration (MIC) = 0.02-0.12 μg/mL) and drug-resistant (MIC = 0.031-0.24 μg/mL) tuberculosis strains while retaining potent DprE1 inhibition (half maximal inhibitory concentration (IC50) = 0.2-0.9 μg/mL) and good intracellular antimycobacterial activity. In addition, these compounds showed good hepatocyte stability and low inhibition of the human ether-à-go-go related gene (hERG) channel. The representative compound 25a with acceptable pharmacokinetic property demonstrated significant bactericidal activity in an acute mouse model of tuberculosis. Moreover, the molecular docking study of template compound 23j provides new insight into the discovery of novel antitubercular agents targeting DprE1.

Diaryl 2- amide-substituted thiophene imide ester compound as well as preparation method and application thereof (by machine translation)

The invention also discloses a 2 - synthesis method thereof, and an application of the compound as an antibacterial agent, in the phthisis-caused by the bacterium, in particular to the, mycobacterium-induced infectious disease (especially (Tuberculosis,TB), mycobacterium- induced mycobacterium, tuberculosis), and (I) the invention, specifically relates to a pharmaceutical composition containing the compound of the present invention or, a R pharmaceutical composition comprising the compound of the present invention. 1 , R2 , R3 , R4 , R5 As described Y in the present invention. as described in the specification, the present invention is directed, to the preparation of novel compounds, having an anti-mycobacterial activity as potential, new drug (s) for the treatment (TB) or preventative treatment of infectious diseases, consisting of M. tuberculosis, in particular phthisis- caused by tubercular mycobacteria, while being useful in overcoming the problems associated with drug resistance. (by machine translation)

4-Acyl-1-(4-aminoalkoxyphenyl)-2-ketopiperazines as a novel class of non-brain-penetrant histamine H3 receptor antagonists

A series of ketopiperazines were prepared and evaluated for their activity as histamine H3 antagonists. From investigation of the tertiary basic center in the aminopropyloxyphenyl template, the 2(R)-methylpyrrolidine was identified as the most

PIPERAZINONE DERIVATIVES USEFUL AS HISTAMINE H3 RECEPTOR ANTAGONISTS AND/OR INVERSE AGONISTS

The invention relates to compounds of formula (I) or salts and solvates thereof, processes for their preparation, to compositions containing them and to their use in the treatment of various disorders, such as allergic rhinitis, wherein R1 and

SUBSTITUTED PIPERIDINE ANTAGONIST OF HI RECEPTOR TO BE USED FOR THE TREATMENT OF RHINITIS

The present invention relates to the compound, (I) and salts thereof, processes for its preparation, to compositions containing it and to its use in the treatment of various disorders, such as allergic rhinitis.