Anti-inflammatory and Anti-ulcer Activities of New Fused Thiazole Derivatives Derived from 2-(2-Oxo-2H-chromen-3-yl)thiazol-4(5H)-one

Mohareb, Rafat M.; Al‐Omran, Fatima; Abdelaziz, Mahmoud A.; Ibrahim, Rehab Ali

doi:10.17344/acsi.2017.3200

Cited by 19 publications

(13 citation statements)

References 17 publications

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“…Its 1 H-NMR spectrum revealed singlet signals at 2.12, 3.01 and 3.09 ppm assignable to three CH 3 protons. Also, 13 (23). The assignment of structure 23 was supported by elemental analysis and spectral data.…”

Section: Methodsmentioning

confidence: 87%

“…[10][11][12][13][14][15][16][17][18][19][20] Consequently, thienopyrimidines have become an important class of compounds in drug discovery programs and the medicinal chemistry. [21][22][23][24][25] In continuation of our previous work on biologically active nitrogen and sulfur heterocycles, [26][27][28][29] it was of interest to synthesize some novel thieno [2,3-d:4,5-d`]dipyrimidine derivatives and evaluate these compounds for their cytotoxic activity.…”

Section: Introductionmentioning

confidence: 99%

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Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

El‐Sayed¹,

Fadda²

2018

ACSi

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Synthesis of some novel tricyclic compounds bearing thienodipyrimidine moiety by the reaction of ethyl 6-amino-1,3-dimethyl-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,2-d]pyrimidine-7-carboxylate (1) with different types of aromatic amines to give the corresponding carboxamide derivatives 2-11, which cyclized with triethyl orthoformate in acetic anhydride to afford thieno[2,3-d:4,5-d']dipyrimidine derivatives 12-15 is described. Similarly, thieno[2,3-d:4,5-d']dipyrimidine derivative 17 was also prepared via the reaction of carboxamide derivative 2 with chloroacetyl chloride in chloroform to give thieno[3,2-d]pyrimidine-7-carboxamide derivative 16, followed by a cyclization in boiling acetic anhydride. The structure of these compounds was confirmed on the basis of their spectral and analytical data such as IR, 1 H-NMR, 13 C-NMR spectroscopy and mass spectral data. The synthesized compounds were screened for their cytotoxic activity.

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Section: Methodsmentioning

confidence: 87%

Section: Introductionmentioning

confidence: 99%

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

El‐Sayed¹,

Fadda²

2018

ACSi

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“…et al, designed and synthesized some azolylchroman derivatives and investigated anticonvulsive and antiepileptogenic properties by lithiumepilocarpine induced seizure and PTZ-induced kindling models. 7-chloro-3-(1H-imidazol-1-yl chroman-4-one(10) showed delaying in the onset of a seizure and decreasing duration of seizures in a model of epilepsy21 .…”

mentioning

confidence: 93%

Untitled

2020

IJPSR

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Chromens are oxygen-containing heterocycles, abundantly found in nature in the form of flavone, is flavones, flavanones, catechins, anthocyanins and collectively known as flavonoids and isoflavonoids. Being a polar and ionizable aromatic compound, it improves the pharmacokinetic characteristics of lead molecules. Imidazole derivatives have occupied a unique place in the field of medicinal chemistry. Therefore, the incorporation of the chromen nucleus is an important synthetic strategy in drug discovery. The high therapeutic properties of the chromen related drugs have encouraged the researchers to synthesize new chemotherapeutic agents. A variety of cellular targets are interacting with the derivatives of chromen and that can be responsible for their wide-ranging epileptic activities. The substitution of chromen nucleus is a crucial step in the drug discovery process. In the present review, chromen derivatives having antiepileptic activity is described using a structural substitution pattern. The interest in chromen is ever-growing since they offer a fairly diverse chemical space for exploration of medicinal potential.

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“…15 According to our previous work a large number of heterocyclic compounds with anti-proliferative and anti-inflammatory activities were recently synthesized by our research group. 16,17 Recently, our research group was involved in the synthesis and determination of the anti-proliferative properties of a large number of heterocyclic compounds. 18,19 In addition, according to our continued interest in the design of new multicomponent reactions and the application in the synthesis of heterocyclic compounds we found some unprecedented reaction patterns in the reaction of dimedone (1) with aromatic aldehydes 2a-c, to produce the benzylidene derivatives 3a-c and with aromatic diazonium salts 10a,b to produce products which underwent heterocyclization reactions to give compounds with potential antitumor activities.…”

Section: Introductionmentioning

confidence: 99%

Synthesis of Heterocyclic Compounds Derived From Dimedone and their Anti-tumor and Tyrosine Kinase Inhibitions

Mohareb

Manhi

Abdelwahab

2020

ACSi

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The reaction of dimedone with arylaldehydes gave the benzylidene derivatives 3a-c, the latter underwent a series of heterocyclization reactions to give fused thiophene, pyrazole isoxazole and pyridazine derivatives. The synthesized compounds were evaluated against different kinds of cancer cell lines together tyrosine kinases and Pim-1 kinase inhibitions. All the synthesized compounds were assessed for the inhibitory activities against A549 (non-small cell lung cancer), H460 (human lung cancer), HT-29 (human colon cancer) and MKN-45 (human gastric cancer) cancer cell lines together with foretinib as the positive control by a MTT assay. The promising compounds were 3c, 5b, 5e, 5f, 7c, 7f, 9c, 11b, 12c, 12d, 13b, 13d, 14b, 16c and 16d among the tested compounds. On the other hand, compounds 5b, 5e, 5f, 7c, 11b, 12c, 12d, 13d, 14b, 16c and 16d were the most effective inhibitors against tyrosine kinases and compounds 5b, 11b, 12d, 13d, 14b and 16c were the most potent against Pim-1 kinase.

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Anti-inflammatory and Anti-ulcer Activities of New Fused Thiazole Derivatives Derived from 2-(2-Oxo-2H-chromen-3-yl)thiazol-4(5H)-one

Cited by 19 publications

References 17 publications

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

Synthesis and Cytotoxic Activity of Some Novel Thieno[2,3-d:4,5-d’]Dipyrimidine Derivatives

Untitled

Synthesis of Heterocyclic Compounds Derived From Dimedone and their Anti-tumor and Tyrosine Kinase Inhibitions

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