754235-62-6Relevant articles and documents
Development of potent nanosized isatin-isonicotinohydrazide hybrid for management of Mycobacterium tuberculosis
Eldehna, Wagdy M.,El Hassab, Mahmoud A.,Abdelshafi, Nahla A.,Al-Zahraa Sayed, Fatma,Fares, Mohamed,Al-Rashood, Sara T.,Elsayed, Zainab M.,Abdel-Aziz, Marwa M.,Elkaeed, Eslam B.,Elsabahy, Mahmoud,Eissa, Noura G.
, (2021/12/20)
Inspired by the antitubercular activity of isoniazid (INH) and 5-bromoisatin, isatin–INH hybrid (WF-208) has been synthesized as a potent agent against multidrug-resistant (MDR) and extensively drug-resistant (XDR) strains of M. tuberculosis. In silico molecular docking studies indicated that DprE1, a critical enzyme in the synthesis of M. tuberculosis cell wall, is a potential enzymatic target for WF-208. The synthesized WF-208 was incorporated into a nanoparticulate system to enhance stability of the compound and to sustain its antimicrobial effect. Nanosized spherical niosomes (hydrodynamic diameter of ca. 500–600 nm) could accommodate WF-208 at a high encapsulation efficiency of 74.2%, and could impart superior stability to the compound in simulated gastric conditions. Interestingly, WF-208 had minimal inhibitory concentrations (MICs) of 7.8 and 31.3 μg/mL against MDR and XDR M. tuberculosis, respectively, whereas INH failed to demonstrate bacterial growth inhibition at the range of the tested concentrations. WF-208-loaded niosomes exhibited a 4-fold increase in the anti-mycobacterial activity as compared to the free compound (MIC of 1.9 vs. 7.8 μg/mL) against H37Rv M. tuberculosis, after three weeks of incubation with WF-208-loaded niosomes. Incorporation of the compound into nanosized vesicles allowed for a further increase in stability, potency and sustainability of the anti-mycobacterial activity, thus, providing a promising strategy for management of tuberculosis.
CF 3 COOH/O 2 -Mediated Metal-Free Domino Construction of the Isatin Skeleton
Chen, Yongjian,Li, Jianjun,Wang, Fang,Zhang, Qiwei,Zhou, Jiadi
supporting information, p. 1799 - 1804 (2019/09/09)
Directed by the strategy of C-H activation, an efficient construction of the isatin skeleton was developed through aerobic oxidation of glycine esters. The reactions were performed under CF 3 COOH/O 2 conditions in the absence of met
SUBSTITUTED HETEROCYCLIC COMPOUNDS
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Page/Page column 35, (2011/06/11)
The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (I) as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.