2015-20-5Relevant articles and documents
Fluoroquinolone amino derivatives and use thereof in prevention and control of citrus diseases
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Paragraph 0084; 0087, (2018/07/30)
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.
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
Yuan, Yunyun,Elbegdorj, Orgil,Chen, Jianyang,Akubathini, Shashidhar K.,Zhang, Feng,Stevens, David L.,Beletskaya, Irina O.,Scoggins, Krista L.,Zhang, Zhenxian,Gerk, Phillip M.,Selley, Dana E.,Akbarali, Hamid I.,Dewey, William L.,Zhang, Yan
supporting information, p. 10118 - 10129 (2013/01/16)
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.
Synthesis and antimicrobial activity of some new isonicotinoylamino acid and dipeptide derivatives
El-Naggar,Hussein,El-Nemma,Samour
, p. 662 - 670 (2007/10/02)
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