Synthesis and Characterization of New Dibenzo[b, e]Thiepine Derivatives. I

Ilie, Corina; Stecoza, Camelia Elena; Cãproiu, Miron Teodor; Hau, Ramona; Guta, Rodica; Nanau-Andreescu, Doina; Vuia, Traian

doi:10.37358/rc.08.12.2059

Cited by 3 publications

(2 citation statements)

References 1 publication

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“…The method was adapted based on previously described procedures [43,44] and the reaction is presented in Scheme 1. The aromatic carboxylic acids 1f,g were prepared starting from thiophenol and phtalide, according to previously reported procedures [45][46][47]. The 1,3,4-thiadiazol-2-amide derivatives 3a-c were synthesized from 5-phenyl-1,3,4thiadiazol-2-amine (2a).…”

Section: Synthesis Proceduresmentioning

confidence: 99%

Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation

Stecoza,

Nitulescu,

Draghici

et al. 2023

IJMS

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Thiadiazole derivatives have garnered significant attention in the field of medicinal chemistry due to their diverse pharmacological activities, including anticancer properties. This article presents the synthesis of a series of thiadiazole derivatives and investigates their chemical characterization and potential anticancer effects on various cell lines. The results of the nuclear magnetic resonance (NMR) analyses confirmed the successful formation of the target compounds. The anticancer potential was evaluated through in silico and in vitro cell-based assays using LoVo and MCF-7 cancer lines. The assays included cell viability, proliferation, apoptosis, and cell cycle analysis to assess the compounds’ effects on cancer cell growth and survival. Daphnia magna was used as an invertebrate model for the toxicity evaluation of the compounds. The results revealed promising anticancer activity for several of the synthesized derivatives, suggesting their potential as lead compounds for further drug development. The novel compound 2g, 5-[2-(benzenesulfonylmethyl)phenyl]-1,3,4-thiadiazol-2-amine, demonstrated good anti-proliferative effects, exhibiting an IC50 value of 2.44 µM against LoVo and 23.29 µM against MCF-7 after a 48-h incubation and little toxic effects in the Daphnia test.

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Section: Synthesis Proceduresmentioning

confidence: 99%

Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation

Stecoza,

Nitulescu,

Draghici

et al. 2023

IJMS

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“…The qualitative assay of the antimicrobial activity was performed on the MuellereHinton Agar medium by an adapted disc-diffusion method as previously reported [32]. The quantitative assay of the antimicrobial activity was performed by the liquid medium microdilution method in 96-multiwell plates to establish the MIC.…”

Section: Antimicrobial Activity Assaysmentioning

confidence: 99%

Antimicrobial performance of nanostructured silica–titania sieves loaded with izohidrafural against microbial strains isolated from urinary tract infections

Tameemi

Stan

Prisacari

et al. 2016

Comptes Rendus. Chimie

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This study aimed to examine the efficiency of novel bioactive nanostructures represented by silicaetitania sieves used as carriers for a new antibacterial agent izohidrafural against bacterial strains isolated from nosocomial urinary tract infections, by using biological quantitative assays. Several release trials have been established and compared with MCM-41 in parallel experiments to achieve the optimum release profile. The obtained systems showed that silicaetitania sieves loaded with izohidrafural proved to be the most active material against Klebsiella pneumoniae (average minimal inhibitory concentration [MIC] 40.62 mg/mL), desaminase-positive strains (average MIC 2.925 mg/mL), and Proteus mirabilis (average MIC 9.37 mg/mL), the last being reported with the highest growth rate in the urinary tract catheters. In contrast, the nonloaded silicaetitanium sieves exhibited the highest antimicrobial activity against the Gram-positive cocci. Izohidrafural exhibited the highest antimicrobial efficiency, superior to the common drug nitrofurantoin against most Escherichia coli strains, with average MIC of 4.68 mg/mL.

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Synthesis and Evaluation of the Antimicrobial and Antibiofilm Activity of Novel Dibenzothiepines

Stecoza¹

2020

FARMACIA

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Synthesis and Characterization of New Dibenzo[b, e]Thiepine Derivatives. I

Cited by 3 publications

References 1 publication

Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation

Synthesis of 1,3,4-Thiadiazole Derivatives and Their Anticancer Evaluation

Antimicrobial performance of nanostructured silica–titania sieves loaded with izohidrafural against microbial strains isolated from urinary tract infections

Synthesis and Evaluation of the Antimicrobial and Antibiofilm Activity of Novel Dibenzothiepines

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