Novel N3 substituted derivatives of 4-iminothiazolidine-2-one were synthesised under the reactions of [2+3]cyclocondensation, thionation and aminolysis. The functionalisation of 3-phenyl-4-imino-thiazolydine-2-one was carried out in its C5 position under condensation Knoevenagel and nitrosation reactions. The antioxidant activity of the synthesised compounds was evaluated in vitro by the method of their scavenging effect on 2,2-diphenyl-1-picrylhydrazyl (DPPH) radicals. When compared with existing antioxidants, some of our compounds were found to be more potent.
The synthesis and determination of the antioxidant activity of some novel (5,7-dimethyl-2-oxo-thiazolo[4,5-b]pyridine-3-yl)-acetic acid hydrazide derivatives are described in this article. The transformation of the base heterocycle was carried out via the reactions of acylation, [2+3]cyclocondensation, Knoevenagel condencation and alkylation for the purpose to obtain substances with a satisfactory pharmacological profile. Antioxidant activity of the synthesized compounds was evaluated in vitro by means of the scavenging metod effect on 2,2 diphenyl-1-picrylhydrazyl (DPPH) radicals.
1,3,4-Oxadiazole scaffold is one of the most important heterocyclic fragments, which is considered as a perspective building block for drug discovery. Substituted 1,3,4-oxadiazoles had been reported to display a diverse range of pharmacological activities including anticancer, anti-inflammatory, antitubercular, antibacterial, antiviral, antifungal, insecticidal, antioxidant, and analgesic activities. Moreover, the 1,3,4-oxadiazole core is a structural component of approved antiretroviral (Raltegravir), anticancer (Zibotentan), and antihypertensive (Tiodazosin and Nesapidil) drugs. In the present review, we summarized the literature data about the main approaches for obtaining possible directions of structural modification and pharmacological activity of noncondensed heterocyclic systems based on the 1,3,4-oxadiazole ring as promising objects for modern bioorganic and medicinal chemistry.
The pathology of the hepatobiliary system significantly affects the state of the organs of the oral cavity. A clinical and index study of the state of periodontal tissues in 122 patients was conducted, which showed the prevalence of periodontal disease in patients with chronic acalculous cholecystitis. The examined patients were divided into groups depending on the treatment method, and the result was evaluated before treatment, directly after treatment and 6 months following treatment. Antidysbiotic hepatoprotector and 2% thiotriazolin ointment were included in the combination therapy. Studies have shown that patients with hepatobiliary pathology have increased likelihood of periodontal diseases, and after treatment, periodontal indicators and the hygiene index are significantly reduced, especially in the group where the proposed scheme was used, and the long-term results were stable for 6 months.
The synthesis and antitumor activity screening of 1,2,4-triazino [5,6-b]indoles based conjugates were performed. Reaction between 3-mercapto-1,2,4-triazino [5,6-b]indoles and several N -arylchloroacetamides yielded 3S-substituted 1,2,4-triazino [5,6-b]indoles. Based on 3-hydrazine-1,2,4-triazino [5,6-b]indoles the new 4-thiazolidinones have been synthesized. Seven synthesized compounds were tested for their anticancer activity in NCI60 cell lines.
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