Synthesis and antimicrobial evaluation of novel 1,3-thiazoles and unsymmetrical azines

El‐Kady, M. Y.; Abbas, Eman M. H.; Salem, Marwa S.; Kassem, Asmaa F.; El‐Moez, Sherein I. Abd

doi:10.1007/s11164-015-2214-z

Cited by 12 publications

(4 citation statements)

References 26 publications

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“…Treatment of 1,3,4-oxadiazolyl with ethyl chloroacetate and α-haloketones affords thiazole derivatives [ 26 ]. Synthesis of 1,3-thiazoles via reaction of thiosemicarbazide derivatives with various halogens, such as ethyl bromoacetate and ethyl-2-bromopropionate, is also known [ 27 ]. Moreover, synthesis of bisthiazoles by treating dihydrazonoyl dichloride with hydrazone has also been documented [ 28 , 29 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles

2018

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Small heterocyclic compounds containing nitrogen and sulfur atoms, such as thiazole derivatives, represent a significant class of organic azoles that exhibit promising bioactivities and have a great potential in medicinal and agricultural fields. A convenient and high-yielding synthetic approach for a range of organic molecules is presented. The nuclease-like activities of compounds were studied with the aid of E. coli AB1157 DNA and agarose gel electrophoresis. The antioxidant evaluation of the compounds was carried out with different antioxidant techniques, such as ABTS and NO scavenging efficiency. The antibacterial behavior was evaluated against various bacterial strains, both Gram-positive and -negative, and the minimum inhibitory concentration (MIC) values of these compounds were determined. The antiproliferative activities and IC50 values of the synthesized organic molecules compounds against HEPG-2, MCF-7, and HCT-116 cell lines were evaluated.

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Section: Introductionmentioning

confidence: 99%

Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles

2018

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“…In continuation of our previous work, the present work aims at utilization of the reactivity of 2‐thioxo‐1,2‐dihydrobenzo[d][1,3]thiazin‐4‐one ( 1 ) toward different electrophilic and nucleophilic reagents to design and construct new fused and nonfused heterocyclic systems and evaluate them for antitumor activity.…”

Section: Resultsmentioning

confidence: 99%

Synthesis and cytotoxic activity against human tumor cells of heterocyclic systems derived from 2‐thioxo‐1,2‐dihydro‐4H‐3,1‐benzothazin‐4‐one

Khlosy

Salem

Ali

et al. 2019

Journal of Heterocyclic Chem

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The title compound was prepared and converted to 2-hydrazinyl-1,2-dihydro-4H-benzo[d] [1,3]thiazin-4-one which was utilized to synthesize fused heterocyclic systems, namely benzotriazolothiazinone derivatives, as well as, nonfused heterocyclic systems such as pyrazolyl-benzothiazinones, benzothiazinylpyridazine and imidazolylbenzothiazinone derivatives via reaction with formamide, acetic acid, ethyl cyanoacetate, maleic anhydride and benzaldehyde followed by treatment with glycine, respectively. All compounds have been structurally characterized by means of IR, MS, and 1 H-NMR spectra. The synthesized compounds were evaluated in vitro for their antiproliferative activity against HePG-2 and MCF-7 cell lines. 2H-Benzo[d][1,3]thiazine-2,4 (1H)-dithione and 2-thioxo-1,2-dihydro-4H-benzo[d] [1,3]thiazin-4-one were the most potent against the two cancer cells compared to that of the reference compound doxorubicin. Most of the synthesized compounds also exhibited good cytotoxic activity.

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“…In continuation of our previous works , the present work aimed at utilization of the reactivity of 4‐(4‐methoxyphenyl)‐2‐oxo‐1,2,3,4,5,6,7,8‐octahydroquinoline‐3‐carbonitrile 1 towards different electrophilic and nucleophilic reagents to obtain new fused and nonfused heterocyclic systems and evaluate them for antileishmanial, antitumor, and antimicrobial activities.…”

Section: Resultsmentioning

confidence: 99%

Design, Synthesis, and In Vitro Antileishmanial and Antitumor Activities of New Tetrahydroquinolines

Madkour

El‐Hashash

Salem

et al. 2017

Journal of Heterocyclic Chem

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A novel series of tetrahydroquinolines containing acetohydrazide, oxopyrazole, oxothioxodihydropyrazole, and thioxotriazole have been synthesized. Antileishmanial, antitumor, and cytotoxicity activities of synthesized compounds were evaluated in vitro. Antileishmanial activity of the most synthesized compounds showed tremendous activity towards Leishmania major. Most of the test compounds exhibited significant level of tumor inhibition. The tetrahydropyrano[2,3‐b]quinolin‐2‐one 6 and 4‐oxo‐4H‐pyrazol‐3‐yloxytetrahydroquinoline‐3‐carbonitrile derivatives 18 showed 100% tumor inhibition comparable with standard drug vincristine (100% tumor inhibition). Tetrahydroquinolines under investigation showed cytotoxicity with LD50 values in the range 0.56–3.01 μg/mL compared with standard drug MS‐222 with LD50 value of 4.30 μg/mL. The presence of a pyrazole ring markedly improved the activity profiles of tetrahydroquinoline. All newly synthesized compounds were characterized by IR, 1H NMR, and MS.

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Synthesis and antimicrobial evaluation of novel 1,3-thiazoles and unsymmetrical azines

Cited by 12 publications

References 26 publications

Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles

Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles

Synthesis and cytotoxic activity against human tumor cells of heterocyclic systems derived from 2‐thioxo‐1,2‐dihydro‐4H‐3,1‐benzothazin‐4‐one

Design, Synthesis, and In Vitro Antileishmanial and Antitumor Activities of New Tetrahydroquinolines

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