Synthesis and evaluation of some novel thiazoles and 1,3-thiazines as potent agents against the rabies virus

Abdalla, Mohamed A. Y.; Gomha, Sobhi M.; El-Aziz, Mohamad Abd; Serag, Nany S. Eldin

doi:10.3906/kim-1506-13

Cited by 56 publications

(29 citation statements)

References 6 publications

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“…As a part of our research interest towards developing new routes for the synthesis of a variety of heterocyclic systems with promising biological and pharmacological activities [14][15][16][17][18][19][20][21][22][23][24][25][26], we report in the present work the synthesis of a new series of 1,3,4-thidiazoles as anti-inflammatory, analgesic and anti-ulcer agents ( Figure 2).…”

Section: Figure1 Structures Of Literature Lead Compoundsmentioning

confidence: 99%

Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles

Gomha

Muhammad

Edrees

et al. 2019

Proceedings of the 23rd International Electronic Conference on Synthetic Organic Chemistry

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A novel series of fused imidazole were prepared from reaction of 2-bromoacetyl-3phenyl-1,3,4-thiadiazole with various heterocyclic amines under microwave irradiation. The structures of all the novel products were elucidated based on elemental analysis and spectral data. In addition, the biological activity of the newly synthesized compounds was evaluated and the results obtained indicate their potency as anti-inflammatory, analgesic and anti-ulcer agents. The binding mechanism of the most active compounds was studied using MOE to analyze the molecular interactions.

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Section: Figure1 Structures Of Literature Lead Compoundsmentioning

confidence: 99%

Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles

Gomha

Muhammad

Edrees

et al. 2019

Proceedings of the 23rd International Electronic Conference on Synthetic Organic Chemistry

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“…11,12 Thiazole heterocycles, derivatives of thiosemicarbazone, are scaffolds of many natural, synthetic and semi-synthetic drugs which exhibit numerous remarkable pharmacological activities including antiparasitic, antiinflammatory and antineoplastic activities. [13][14][15][16][17] Thiazole derivatives are also known to have potential anticancer activity with a mechanism of action related to inhibition of matrix metallo-proteinases, kinases and anti-apoptotic BCL2 family proteins. [18][19][20][21] Multicomponent reactions (MCR) are one-pot processes which always occupy great importance in the repertoire of sustainable synthetic tools because of their high efficiency and atom economy.…”

Section: Introductionmentioning

confidence: 99%

<p>One-Pot Synthesis of Novel Thiazoles as Potential Anti-Cancer Agents</p>

Sayed¹,

Gomha²,

Taher³

et al. 2020

DDDT

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Background: Thiazole and thiosemicarbazone derivatives are known to have potential anticancer activity with a mechanism of action related to inhibition of matrix metalloproteinases, kinases and anti-apoptotic BCL2 family proteins. Materials and Methods: A novel three series of 5-(1-(2-(thiazol-2-yl)hydrazono)ethyl) thiazole derivatives were prepared in a one-pot three-component reaction using 2-(2-benzylidene hydrazinyl)-4-methylthiazole as a starting precursor. MS, IR, 1 H-NMR and 13 C-NMR were used to elucidate the structures of the synthesized compounds. Most of the synthesized products were evaluated for their in vitro anticancer screening against HCT-116, HT-29 and HepG2 using the MTT colorimetric assay. Results: The results indicated that compounds 4c, 4d and 8c showed growth inhibition activity against HCT-116 with IC 50 values of 3.80 ± 0.80, 3.65 ± 0.90 and 3.16 ± 0.90 μM, respectively, compared to harmine (IC 50 = 2.40 ± 0.12 μM) and cisplatin (IC 50 = 5.18 ± 0.94 μM) reference drugs. Also, compounds 8c, 4d and 4c showed promising IC 50 values of 3.47 ± 0.79, 4.13 ± 0.51 and 7.24 ± 0.62 μM, respectively, against the more resistant human colorectal cancer (HT-29) cell line compared with harmine (IC 50 = 4.59 ± 0.67 μM) and cisplatin (IC 50 = 11.68 ± 1.54 μM). On the other hand, compounds 4d, 4c, 8c and 11c were the most active (IC 50 values of 2.31± 0.43, 2.94 ± 0.62, 4.57 ± 0.85 and 9.86 ± 0.78 μM, respectively) against the hepatocellular carcinoma (HepG2) cell line compared with harmine (IC 50 = 2.54 ± 0.82 μM) and cisplatin (IC 50 = 41 ± 0.63 μM). The study also suggested that the mechanism of the anticancer action exerted by the most active compounds (4c, 4d and 8c) inside HCT-116 cells was apoptosis through the Bcl-2 family. Conclusion: Thiazole scaffolds 4c, 4d and 8c showed anticancer activities in the micromolar range and are appropriate as a candidate for cancer treatment.

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“…In this current work, we geared our research toward the synthesis of some new bis‐thiazoles with highly expected bioactive potential …”

Section: Introductionmentioning

confidence: 99%

Synthesis and characterization of some novel bis‐thiazoles

Mahmoud

Kassab

Gomha

2019

Journal of Heterocyclic Chem

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The bis‐thiosemicarbazone derivative 3 was prepared and reacted with N‐aryl‐2‐oxopropane hydrazonoyl chloride 4a‐g and ethyl (N‐arylhydrazono)chloroacetate 7a‐e in absolute ethanol in the presence of triethylamine at reflux afforded a new series of thiazoles 6a‐g and 9a‐e, respectively. Also, thiosemicarbazone derivative 3 was reacted with N′‐phenylbenzohydrazonoyl chloride 10 to give the respective bis‐thiadiazole derivative 12. Moreover, the reaction of 3 with a number of haloketones and haloesters furnished the respective bis‐thiazole derivatives 14, 16, 18, and 20. The mechanisms that account for formation of products 6, 9, and 12 were discussed. Also, the molecular structure of the synthesized compounds was illustrated by spectroscopic and elemental analysis.

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Synthesis and evaluation of some novel thiazoles and 1,3-thiazines as potent agents against the rabies virus

Cited by 56 publications

References 6 publications

Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles

Synthesis Under Microwave Irradiation and Molecular Docking of Some Novel Bioactive Thiadiazoles

<p>One-Pot Synthesis of Novel Thiazoles as Potential Anti-Cancer Agents</p>

Synthesis and characterization of some novel bis‐thiazoles

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