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The present review supply an overview of the chemistry of (aryl/hetaryl)thiopyran-4-one derivatives via a systematic and comprehensive survey of thesynthetic methods, the chemical reactivity and biological importance.These aryl/hetarylthiopyran-4-one derivatives that have been reported mainly from 2000 to 2019. The biological, therapeutic, and medicinal properties of (aryl/hetaryl)thiopyran-4-one derivatives and its analogues have prompted enormous research aimed at developing synthetic routes to these heterocyles. [ABSTRACT FROM AUTHOR]

In the light of using of 5‐imidazolinones in agriculture as safe and stable herbicides, the pesticide activities of some new synthesized derivatives 3‐18 of this ring system against "cotton leaf worm (Spodoptera littoralis)" have been investigated. The interpretation of the elemental and spectral analyses proved the correct structural formulae of the new synthesized compounds. The compounds 1, 5, 6a,b, 8a,c, 9, 11, 12, 15, 16, 17, and 18 showed higher potency than chlorpyrifos (dursban) recommended insecticide. While the derivatives 2, 3, 4, 7, 8b, 10, 13, and 14 showed toxicity values less than chlorpyrifos insecticide. The 5‐imidazolinones 9 and 12 may be potentially used as insecticides for treatment of cotton leaf worm. [ABSTRACT FROM AUTHOR]

Series of novel pyrazolo[3,4‐d]pyrimidines as potential telomerase inhibitors were synthesized. Results of the antitumor assay indicated that compounds 4b, 5a–b, 13b,c, and 14a,b exhibited the most potent activity (IC50 from 39 to 43 μM) against Ehrlich ascites carcinoma cells (EAC). Also, the newly synthesized compounds were examined for telomerase inhibition by the known a TRAP assay. The results showed that compound 13c has remarkable inhibition activity with IC50 value of 30 μM. On the other hand, computational studies were performed to the titled compounds to get insight in their degree of recognition with the conserved amino acids of the telomerase enzyme active site (code: 3DU6) as promising lead in the cancer cure era. [ABSTRACT FROM AUTHOR]

An improved efficient synthesis for 2,4-azepandiones ( 3, 8, and 14) could be achieved by a careful control of the reaction conditions to cyclize ethyl 4-( N-acetylarylamino) butanoate ( 1, 7, and 13), respectively. The ethyl 4-arylamino butanoate ( 9 or 12) was prepared by stirring the ethyl 4-bromobutanoate and substituted anilines at room temperature. Then, they were acetylated with and triethylamine under the conditions that avoid the formation of 2-pyrrolidinone derivatives 10. Due to the rapid decomposition of the acetylated product ( 7 or 13) to its starting material ( 9 or 12), the reaction mixture is directly transferred without workup to the next step. The azepandione synthesis is favored by using a weak base at low temperature, where it is in a competition with the other modes of ring closure. The structures of the new compounds were supported by correct analytical and spectral data. [ABSTRACT FROM AUTHOR]

Supercritical carbon dioxide (scCO 2 ) has been suggested as a good substitution to environmentally harmful water-based tincturing. The present study describes the successful synthesis of some biologically active dispersion tinctures for supercritical carbon dioxide tincturing of polyester fabric. The coupling of 1-cyanoacetylpiperidine (1) with the diazonium salt of aryl amine derivatives (2a-d) produced 1-((aryldiazenyl) cyanoacetyl piperidines (3a-d). To create the derivatives of 4-(phenyldiazenyl)-5-(piperidin-1-yl)-1H-pyrazol-3-amine (5a), the propane nitriles (3a-d) were condensed with hydrazine hydrate. However, the unexpected 3-aminopyrazol-5-ol yellow-red dispersion dyes (4a-d) were identified as the reaction results. The MS, IR, and NMR spectra were used to describe the novel dyes, and the results exactly matched the suggested structures. The antibacterial test, which was conducted using the AATCC method, revealed that some of the compounds (3a-d) and (4a-d) had impressive antibacterial capabilities against the researched +ve and gram -ve bacteria. For eight dyestuffs, the dyeability, color strength, and color fastness of the tincturing process were evaluated. The evaluation focused on determining color uptake using a gauge for color strength (K/S). All dyes displayed excellent rubbing, washing, and light fastness (color change and staining grade of 4-5)., (© 2023. The Author(s).)