New N-acylhydrazones with Potential Cytotoxic Activity

Socea, Laura Ileana; Bărbuceanu, Ștefania Felicia; Iscrulescu, Lucian; Socea, Bogdan; Hrubaru, Madalina; Pahontu, Elena Mihaela; Diaconu, Camelia Cristina; Bratu, Ovidiu Gabriel; Olaru, Octavian Tudorel

doi:10.37358/rc.18.12.6745

Cited by 3 publications

(3 citation statements)

References 5 publications

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“…The last group of compounds which is worth attention are 5H-dibenzo[a,d] [7]annulene derivatives with cytotoxic [19], antioxidant [20] and antimicrobial [21] properties. Kopanski confirmed effects of long-term treatment of rats with antidepressants on adrenergic-receptor sensitivity in cerebral cortex [22].…”

Section: Computational Detailsmentioning

confidence: 99%

Theoretical Study of the Geometry of Dibenzoazepine Analogues

Szymańska

Majerz

2022

Molecules

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The geometry of dibenzoazepine analogues—typical multifunctional drugs—was investigated to find the geometrical parameters sensitive to the substitution of the central seven-membered ring. Exploration of the crystal structure database (CSD) shows that the geometrical parameter sensitive to the substitution of the carbon atom distance of the central ring not included in the aromatic rings to the plane through the carbon atoms common for the central ring and the aromatic side rings. Presence of the double bond in the central ring was reflected in its partial aromaticity expressed by the HOMED parameter. Some derivatives of 5H-dibenzo[b,f]azepine with flat conformation of the central ring are characterized by mobility of the electron density comparable to the mobility in the aromatic side rings. Influence of the surrounding on the investigated compounds was confirmed by comparison of the optimized molecules and the molecules in the crystal state where the packing forces can influence the molecular geometry.

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Section: Computational Detailsmentioning

confidence: 99%

Theoretical Study of the Geometry of Dibenzoazepine Analogues

Szymańska

Majerz

2022

Molecules

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“…The determinations were made in duplicate against áalanine (positive control) and 1% DMSO (negative control). The experiment was carried out according to the protocol previously described [27][28][29]. From each compound, six concentrations ranging from 5 to 200 µg/mL were tested.…”

Section: Cytoxicity Evaluationmentioning

confidence: 99%

Synthesis, characterization and Cytotoxicity Evaluation of New Compounds from Oxazol-5(4H)-ones and Oxazoles Class Containing 4-(4-Bromophenylsulfonyl)phenyl Moiety

Apostol¹,

Bărbuceanu²,

Olaru³

et al. 2019

Rev. Chim.

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Steiger N-acylation of a-alanine with 4-(4-bromophenylsulfonyl)benzoyl chloride led to 2-[4-(4-bromophenylsulfonyl)benzamido]propanoic acid. This compound underwent intramolecular cyclization in the presence of N-methylmorpholine and ethyl chloroformate or acetic anhydride to the corresponding saturated azlactone. Then acylaminoacylation of dry aromatic hydrocarbons with 2-[4-(4-bromophenylsulfonyl)phenyl]-4-methyloxazol-5(4H)-one or 2-[4-(4-bromophenylsulfonyl) benzamido ]propanoyl chloride in the presence of anhydrous aluminum chloride led to corresponding a-acylamino ketones. These new intermediates were heterocyclized under the action of phosphorus oxychloride or concentrated sulfuric acid in the presence of acetic anhydride to the corresponding oxazoles. The newly synthesized compounds were characterized by spectral studies (FT-IR, UV-Vis, MS, 1H- and 13C-NMR) and elemental analysis. The purity of the new compounds was evaluated by RP-HPLC. The experimental research regarding to the in vitro cytotoxic activity of the new compounds were performed using Daphnia magna bioassay.

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“…Their production, stockpiling and use are monitored by international organizations (Organization for the Prohibition of Chemical Weapons -OPCW) [9][10][11][12][13]. Neurotoxic chemical agents have the property of irreversibly inhibiting the erythrocytary acetylcholinesterase (AChE) [14][15][16][17][18]. The coupling reaction of the organophosphoric compounds at the level of the active situs of the enzyme is represented in fig.1, 2.…”

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confidence: 99%

The Synthesis and Toxicological Characterization of Neurotoxic Chemical Agents Simulants

Tudosie¹,

Secara²,

Smarandache³

et al. 2019

Rev.Chim.

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Neurotoxic warfare chemical agents (CWA/NA) induce major toxicological effects to the affected personnel. Their increased toxicity justifies the necessity of developing analytical methods for diagnosis and specific medical counter measures. CWA/NA are extremely toxic agents which are subject to international regulations (The Geneva Protocol regarding the prohibition of chemical weapons). Taking into account the ban on human experimenting due to high toxicity, simulators of neurotoxic chemical agents are being used in laboratories. These are analogue chemical compounds which possess the same relevant physical, chemical and pharmacodynamical properties of the corresponding agents, but with lower intrinsical toxicity. The synthesis and toxicological characterization of these simulators of neurotoxic chemical agents allow the laboratory research of these extremely toxic compounds and the unfolding of risk-free antidote studies. This paper proposes the synthesis and toxicological testing of chemical compounds which simulate sarin (4-nitrophenyl isopropyl methylphosphonate - NIMP) and VX (4-nitrophenyl ethyl methylphosphonate - NEMP).

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New N-acylhydrazones with Potential Cytotoxic Activity

Cited by 3 publications

References 5 publications

Theoretical Study of the Geometry of Dibenzoazepine Analogues

Theoretical Study of the Geometry of Dibenzoazepine Analogues

Synthesis, characterization and Cytotoxicity Evaluation of New Compounds from Oxazol-5(4H)-ones and Oxazoles Class Containing 4-(4-Bromophenylsulfonyl)phenyl Moiety

The Synthesis and Toxicological Characterization of Neurotoxic Chemical Agents Simulants

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