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doi:10.15254/h.j.d.med.9.2017.165

Cited by 10 publications

(3 citation statements)

References 58 publications

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“…The application possibilities of hydrazides were confirmed after isonicotinic acid hydrazide (INH) was obtained. The unusual clinical value of INH has substituted the synthesis of other heterocyclic hydrazides [30]. Also, a series of 7-azaindolyl hydrazones are characterized as antiproliferative against MCF-7 breast carcinoma cell line [25].…”

Section: Discussionmentioning

confidence: 99%

The N’-Substituted Derivatives of 5-Chloro-3-Methylisothiazole-4-Carboxylic Acid Hydrazide with Antiproliferative Activity

et al. 2019

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Thanks to the progress in oncology, pharmacological treatment of cancer is gaining in importance and in the near future anti-cancer chemotherapeutics are expected to be the main method of treatment for cancer diseases. What is more, the search for new anti-cancer compounds with the desired application properties is constantly underway. As a result of designed syntheses, we obtained some new N’-substituted 5-chloro-3-methylisothiazole-4-carboxylic acid hydrazide derivatives with anticancer activity. The structure of new compounds was determined by mass spectrometry (MS), elemental analysis, proton nuclear magnetic resonance spectroscopy (1H-NMR), carbon nuclear magnetic resonance spectroscopy (13C-NMR), 1H-13C NMR correlations and infrared spectroscopy (IR). Moreover, the structures of the compounds were confirmed by crystallographic examination. The antiproliferative MTT tests for 11 prepared compounds was conducted towards human biphenotypic B cell myelomonocytic leukemia MV4-11. SRB test was used to examine their potential anticancer activity towards human colon adenocarcinoma cell lines sensitive LoVo, resistant to doxorubicin LoVo/DX, breast adenocarcinoma MCF-7 and normal non-tumorigenic epithelial cell line derived from mammary gland MCF-10A. The most active compound was 5-chloro-3-methyl-N′-[(1E,2E)-(3-phenyloprop-2-en-1-ylidene]isothiazole-4-carbohydrazide, which showed the highest antiproliferative activity against all tested cell lines.

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Section: Discussionmentioning

confidence: 99%

The N’-Substituted Derivatives of 5-Chloro-3-Methylisothiazole-4-Carboxylic Acid Hydrazide with Antiproliferative Activity

et al. 2019

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“…The availability of proton in hydrazides constitutes them as an important class of compound for new drug discovery. Therefore, researchers have shown great interest in developing these compounds as target structures for evaluating new biological activities [31].…”

Section: Mechanism Of the Pechmann Condensationmentioning

confidence: 99%

Coumarin Derivatives with Antimicrobial and Antioxidant Activities

Tătărîngă¹,

Zbancioc²

2020

Phytochemicals in Human Health

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Coumarin derivatives are structurally interesting compounds for synthesizing antimicrobial and antioxidant agents. Starting from 4-methyl-7-hydroxycoumarin, several derivatives with these properties have been obtained through different reaction steps. Their molecular structures were established by Fourier-transform infrared spectroscopy and nuclear magnetic resonance spectroscopy. The synthesized coumarin derivatives exerted meaningful activities against Gram-positive and Gram-negative bacteria as well as strains of Candida spp. All compounds also exhibited high and moderate antioxidant activity in assays for DPPH inhibition, total reducing power, and nitric oxide (NO) inhibition when compared to ascorbic acid.

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“…In addition, imine-containing azoles are highlighted to develop new potential drug candidates with diverse therapeutic efficacy such as anticancer, antibacterial, antifungal, antioxidant, antimicrobial, and antiproliferative activities [13][14][15][16]. Moreover, Schiff's bases have gained prominence role for antimicrobial, antituberculosis [17], anticonvulsant, antidepressant, analgesic, anti-inflammatory, antitumoral, vasodilator, and antiviral [18] activities. The synergism of thiazole with imine moiety in a hybridized molecule may result in increasing the biological potency, mainly because of the variation of substituents in the imine derivatives.…”

Section: Introductionmentioning

confidence: 99%

Potential COVID-19 Drug Candidates Based on Diazinyl-Thiazol-Imine Moieties: Synthesis and Greener Pastures Biological Study

et al. 2022

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A novel series of 1-aryl-N-[4-phenyl-5-(arylazo)thiazol-2-yl)methanimines has been synthesized via the condensation of 2-amino-4-phenyl-5-arylazothiazole with various aromatic aldehydes. The synthesized imines were characterized by spectroscopic techniques, namely 1H and 13C NMR, FTIR, MS, and Elemental Analysis. A molecular comparative docking study for 3a–f was calculated, with reference to two approved drugs, Molnupiravir and Remdesivir, using 7BQY (Mpro; PDB code 7BQY; resolution: 1.7 A°) under identical conditions. The binding scores against 7BQY were in the range of −7.7 to −8.7 kcal/mol for 3a–f. The high scores of the compounds indicated an enhanced binding affinity of the molecules to the receptor. This is due to the hydrophobic interactions and multi-hydrogen bonds between 3a–f ligands and the receptor’s active amino acid residues. The main aim of using in silco molecular docking was to rank 3a–f with respect to the approved drugs, Molnupiravir and Remdesivir, using free energy methods as greener pastures. A further interesting comparison presented the laydown of the ligands before and after molecular docking. These results and other supporting statistical analyses suggested that ligands 3a–f deserve further investigation in the context of potential therapeutic agents for COVID-19. Free-cost, PASS, SwissADME, and Way2drug were used in this research paper to determine the possible biological activities and cytotoxicity of 3a–f.

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Cited by 10 publications

References 58 publications

The N’-Substituted Derivatives of 5-Chloro-3-Methylisothiazole-4-Carboxylic Acid Hydrazide with Antiproliferative Activity

The N’-Substituted Derivatives of 5-Chloro-3-Methylisothiazole-4-Carboxylic Acid Hydrazide with Antiproliferative Activity

Coumarin Derivatives with Antimicrobial and Antioxidant Activities

Potential COVID-19 Drug Candidates Based on Diazinyl-Thiazol-Imine Moieties: Synthesis and Greener Pastures Biological Study

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