2015-20-5

Usage

InChI:InChI=1/C8H8N2O3/c11-7(12)5-10-8(13)6-1-3-9-4-2-6/h1-4H,5H2,(H,10,13)(H,11,12)

Upstream product

• 574715-93-8 ethyl (isonicotinamid-4-yl)acetate 
• 4013-73-4 isonicotinoyl azide 
• 56-40-6 glycine 
• 14254-57-0 4-(chlorocarbonyl)pyridine 
• 55-22-1 pyridine-4-carboxylic acid 
• 459-73-4 GlyOEt*HCl 
• 90557-95-2 4-pyridylcarbonylamino acetic acid methyl ester 

Downstream Products

• 1160366-88-0 (S)-N-[[3-[3-fluoro-4-[4-[2-isonicotinamidoacetyl]piperazin-1-yl]phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide 

Relevant academic research and scientific papers

Fluoroquinolone amino derivatives and use thereof in prevention and control of citrus diseases

Citrus canker and brown spot are common diseases of citrus. At present, few drugs are available to prevent and control the two diseases and have certain defects. Amino groups at the 7th positions of fluoroquinolone drugs are linked with an active fragment by means of a connecting structure so as to obtain compounds shown in a formula I or a formula II. Experiments prove that the compounds providedby the invention have effects of preventing and controlling the citrus canker and the brown spot and have very good application prospect.

Fluoroquinolone such amino derivative and use thereof (by machine translation)

The invention belongs to the field of pharmaceutical chemistry, and in particular relates to a fluoroquinolone derivatives and use thereof. The invention through structural modification of the fluoroquinolone drugs such as shown in formula I, the compounds of the invention not only can the Mycobacterium tuberculosis and the normal bacterial caused by the treatment of infection, bacteria also holds keeps the fungus, citrus pathogens, nicotinamide N - methyltransferase (NNMT) and interleukin IL - 17 PPI has inhibitory activity. The compounds of the invention preparation process operation is convenient, mild condition, to obtain the antibacterial activity is enhanced, water-soluble improve, many compounds toxic side effects, it is expected to reduce the amount of medicine used, shorten the treatment cycle, improve patient's compliance, for tuberculosis drug and other disease research provide new molecular type with the study. (by machine translation)

Design, synthesis, and biological evaluation of 17-cyclopropylmethyl-3, 14β-dihydroxy-4,5α-epoxy-6β-[(4′-pyridyl)carboxamido] morphinan derivatives as peripheral selective μ opioid receptor agents

Peripheral selective μ opioid receptor (MOR) antagonists could alleviate the symptoms of opioid-induced constipation (OIC) without compromising the analgesic effect of opioids. However, a variety of adverse effects were associated with them, partially due to their relatively low MOR selectivity. NAP, a 6β-N-4′-pyridyl substituted naltrexamine derivative, was identified previously as a potent and highly selective MOR antagonist mainly acting within the peripheral nervous system. The noticeable diarrhea associated with it prompted the design and synthesis of its analogues in order to study its structure-activity relationship. Among them, compound 8 showed improved pharmacological profiles compared to the original lead, acting mainly at peripheral while increasing the intestinal motility in morphine-pelleted mice (ED50 = 0.03 mg/kg). The slight decrease of the ED50 compared to the original lead was well compensated by the unobserved adverse effect. Hence, this compound seems to be a more promising lead to develop novel therapeutic agents toward OIC.

NON-PEPTIDYL, POTENT, AND SELECTIVE MU OPIOID RECEPTOR ANTAGONISTS

Selective, non-peptide antagonists of the ma opioid receptor { MOR) and methods of their use are provided. The antagonists may be used, for example, to identify MOR agonists in competitive binding assays, and to treat conditions related to addiction in which MOR is involved, e.g. heroin, prescription drug and alcohol addiction.