Design, in silico, one-pot synthesis, and biological evaluations of novel bis-urea analogs

Shoja, Sajede; Mahmoodi, Nosrat O.; Ghafouri, Hossein; Rassa, Mehdi; Sharafshah, Alireza; Kokhdan, Esmaeel Panahi

doi:10.1007/s11164-020-04134-7

Cited by 8 publications

(2 citation statements)

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“…In this study, relying on our prior projects related to the two-directional synthesis and with the aim of developing effective synthesis of new compounds and designing novel molecules with pharmacological activities [28][29][30][31][32][33][34], the synthesis of bis-hydroxychalcone derivatives (Scheme 1) is reported. Initially for synthesize of 4-methoxy/methyl 2,6-diformyl phenol 2 the 4-methoxy/methyl, phenol 1 was participated in the Duff reaction and re uxed for 20h by using HMTA (hexamethylenetetramine) and TFA (trifuoroacetic acid), after which the medium is acidifed and the temperature of the reaction mixture was reaches 110 °C for additional 30 min re ux.…”

Section: Chemistrymentioning

confidence: 99%

Synthesis, biological evaluation and molecular docking studies of a new series of bis-chalcones

2022

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A convenient and e cient reaction for the synthesis of several new bis-hydroxy derivatives of chalcones 4a-h was accomplished via the two-directional Claisen Schmidt condensation of different ketones 3a-e with premade benza-ldehyde 2 under alkaline conditions. Products were obtained with reasonable yields and with excellent purity. The in vitro antioxidant activity of bis-hydroxychalcones were assessed by DPPH radical scavenging activity in comparison to ascorbic acid and products showed good antioxidant activity. To determine the possible binding mechanism with the active site of Tubulin, docking analyses were performed. According to the docking results, ompound s 4a-b showed the best binding a nity of -9.13 and -9.11 kcal/mol for Tubulin, respectively.

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Section: Chemistrymentioning

confidence: 99%

Synthesis, biological evaluation and molecular docking studies of a new series of bis-chalcones

2022

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“…Azo compounds have attracted much attention in both academic and applied research [28,29]. The most prominent feature of these dyes is containing one or more azo groups (-N = N-) that act as bridges between the two organic dyes and at least one of these groups are aromatic [30][31][32]. Azo dyes are used in a variety of elds, such as dyeing, textile, bers, and high-tech applications such as lasers, liquid crystal displays, electro-optical devices, and inkjet printers [33][34][35].…”

Section: Introductionmentioning

confidence: 99%

Efficient Synthesis of New Azoimino-sulfathiazole and Considering Their Antibacterial, Antioxidant and Cytotoxic Activities

Amouee

Mahmoodi

Nyaki

et al. 2022

Preprint

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Sulfonamides are important compounds that have special applications in pharmacy due to their antibacterial and anti-parasitic properties and are known as sulfa-drugs. One of the most important drugs is sulfathiazole. This drug has many uses in the treatment of diseases. In this research, the hybrid reaction between sulfathiazole and various azo compounds was performed via the imine bond. Here, nine new azoiminosulfathiazoles were synthesized, while compound 5g was designed in such a way that two sulfathiazole units were linked by an azo linker. The structure of the newly synthesized hybrid molecules after separation and purification was examined and confirmed by TLC, M.P, FT-IR, 1H NMR, and 13C NMR, and their cytotoxicity was evaluated via MTT assay. Evaluation of antibacterial and antioxidant and anticancer again (PC-3) human prostate line cells using MTT assay properties also showed acceptable results. Comparing 5g with penicillin as a standard drug with the aura of non-growth of bacteria (31 mm) in the presence of Staphylococcus aureus (27 mm) and in the presence of E.coli bacteria showed that it has the best antibacterial properties. Also, evidence shows that some compounds have more effective antibacterial activity than penicillin.

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Urea-thiazole/benzothiazole hybrids with a triazole linker: synthesis, antimicrobial potential, pharmacokinetic profile and in silico mechanistic studies

et al. 2021

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Design, in silico, one-pot synthesis, and biological evaluations of novel bis-urea analogs

Cited by 8 publications

References 35 publications

Synthesis, biological evaluation and molecular docking studies of a new series of bis-chalcones

Synthesis, biological evaluation and molecular docking studies of a new series of bis-chalcones

Efficient Synthesis of New Azoimino-sulfathiazole and Considering Their Antibacterial, Antioxidant and Cytotoxic Activities

Urea-thiazole/benzothiazole hybrids with a triazole linker: synthesis, antimicrobial potential, pharmacokinetic profile and in silico mechanistic studies

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