24310-36-9Relevant articles and documents
Photoactive NO hybrids with pseudo-zero-order release kinetics for antimicrobial applications
Guo, Yuda,Han, Guifang,Hou, Jingli,Liao, Yongfang,Liu, Yangping,Qian, Meng,Song, Yuguang,Wang, Xing,Ye, Zizhen
supporting information, p. 5473 - 5480 (2020/08/03)
Bacterial infection is a major threat to the health and life of humans due to the development of drug resistance, which is related to biofilm formation. Nitric oxide (NO) has emerged as an important factor in regulating biofilm formation. In order to harness the potential benefits of NO and develop effective antibacterial agents, we designed and synthesized a new class of NO hybrids in which the active scaffold benzothienoazepine was tagged with a nitroso group and further conjugated with quaternary ammoniums or phosphoniums. The temporal release of NO from these hybrids can be achieved by photoactivation. Interestingly, the NO release follows a pseudo-zero-order kinetics, which is easily determined by measuring the fluorescent benzothienoazepine or NO. Compared to the positive control ciprofloxacin, the NO hybrid with triphenyl phosphonium (TPP) exhibited more effective activity against S. aureus biofilm in darkness. Irradiation of the NO hybrid led to higher inhibition against S. aureus biofilm compared to the parental NO hybrid in darkness or the corresponding NO-released product, indicating the combined effect of NO and the NO-released product. Therefore, this new class of NO hybrids includes very promising antimicrobial agents and this work provides a new way for the design of highly effective antimicrobial agents. This journal is
NOVEL BENZO [...] DERIVATIVES AND THEIR MEDICAL USE
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Page/Page column 33; 34, (2019/04/26)
One objective of the present invention is to provide a compound having V2 receptor agonist effect. The pharmaceutical composition of this invention uses a compound expressed by the following general formula (I) or its pharmacologically acceptable salt as an active ingredient, wherein, R1 represents the following formula: wherein, A represents a lower alkylene group or the like which may be substituted with a lower alkyl group; R6 represents a hydrogen atom or the like; R7 represents a hydroxyl group, an aromatic heterocyclic group which may be substituted with a lower alkyl group, amine methyl acyl or the like; R2 represents a hydrogen atom or a lower alkyl group; R3 represents a lower alkyl group which may be substituted with 1 to 3 fluorine atoms or a halogen atom; R4 represents 5-membered aromatic monocyclic heterocyclic group, or 5-membered non-aromatic monocyclic heterocyclic group or the like, wherein the heterocyclic group contains at least one nitrogen atom, and may be substituted with a lower alkyl group; R 5 represents a lower alkyl group or a halogen atom or the like.