59702-09-9

Usage

InChI:InChI=1/C8H16N2O/c1-2-3-5-10-6-4-9-7-8(10)11/h9H,2-7H2,1H3

Upstream product

• 5619-34-1 2-amino-N-butyl-acetamide 
• 150714-97-9 tert-butyl (2-(butylamino)-2-oxoethyl)carbamate 
• 488846-76-0 4-butyl-3-oxo-piperazine-l-carboxylic acid tert-butyl ester 
• 107-06-2 1,2-dichloro-ethane 
• 76-05-1 trifluoroacetic acid 

Relevant academic research and scientific papers

Identification of a new series of benzothiazinone derivatives with excellent antitubercular activity and improved pharmacokinetic profiles

Nitrobenzothiazinone (BTZ) is a promising scaffold with potent activity against M. tuberculosis by inhibiting decaprenylphosphoryl-beta-d-ribose 2′-oxidase (DprE1). But unfavorable durability poses a challenge to further development of this class of agents. Herein, a series of BTZs bearing a variety of different substituents at the C-2 position were designed and synthesized. Compounds were screened for their antimycobacterial activity against Mycobacterium tuberculosis H37Ra and were profiled for metabolic stability, plasma protein-binding capacity and pharmacokinetics in vivo. In general, these new BTZs containing N-piperazine, N-piperidine or N-piperidone moiety have excellent antitubercular activity and low cytotoxicity. Several of the compounds showed improved microsomal stability and lower plasma protein-binding, opening a new direction for further lead optimization. And we obtained compound 3o, which maintained good anti-tuberculosis activity (MIC = 8 nM) and presented better in vitro ADME/T and in vivo pharmacokinetic profiles than reported BTZ compound PBTZ169, which may serve as a candidate for the treatment of tuberculosis.

N-(3-amino-2-hydroxy-propyl) substd. alkylamidoalkanol compd.

Disclosed are compounds of the formula (I): useful in treating Alzheimer's disease and other similar diseases. These compounds include inhibitors of the beta-secretase enzyme that are useful in the treatment of Alzheimer's disease and other diseases characterized by deposition of A beta peptide in a mammal. The compounds of the invention are useful in pharmaceutical compositions and methods of treatment to reduce A beta peptide formation.