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      • SCOPUSKCI등재

        Synthesis of New Heterocycles Derived from 3-(3-Methyl-1H-indol-2-yl)-3-oxopropanenitrile as Potent Antifungal Agents

        Gomha, Sobhi M.,Abdel-Aziz, Hatem A. Korean Chemical Society 2012 Bulletin of the Korean Chemical Society Vol.33 No.9

        New thiazoline derivatives 7a-c, and thiophenes 9a-c linked to indole moiety were easily prepared via the reaction of the acrylamide derivative 3 with phenacyl bromides 4a-c, depending on the reaction conditions. In addition, the reaction of compound 3 with hydrazonoyl chlorides 11a-f afforded a series of 1,3,4-thiadiazole derivatives 13a-f. Moreover, coupling of 3-(3-methyl-1H-indol-2-yl)-3-oxopropanenitrile (2) with the diazonium salts of 3-phenyl-5-aminopyrazole 16 or 3-amino-1,2,4-triazole 17 gave the corresponding hydrazones 18 and 19, respectively. Cyclization of the latter hydrazones yielded the corresponding pyrazolo[5,1-c]-1,2,4-triazine and 1,2,4-triazolo[5,1-c]-1,2,4-triazine derivatives 20 and 21, respectively. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, $^1H$ NMR and mass spectral data. All the synthesized compounds were tested for in vitro activities against certain strains of fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds showed marked inhibition of fungal growth nearly equal to the standards.

      • KCI등재

        Synthesis of New Heterocycles Derived from 3-(3-Methyl-1H-indol-2-yl)-3-oxopropanenitrile as Potent Antifungal Agents

        Sobhi M. Gomha,Hatem A. Abdel-Aziz 대한화학회 2012 Bulletin of the Korean Chemical Society Vol.33 No.9

        New thiazoline derivatives 7a-c, and thiophenes 9a-c linked to indole moiety were easily prepared via the reaction of the acrylamide derivative 3 with phenacyl bromides 4a-c, depending on the reaction conditions. In addition, the reaction of compound 3 with hydrazonoyl chlorides 11a-f afforded a series of 1,3,4-thiadiazole derivatives 13a-f. Moreover, coupling of 3-(3-methyl-1H-indol-2-yl)-3-oxopropanenitrile (2) with the diazonium salts of 3-phenyl-5-aminopyrazole 16 or 3-amino-1,2,4-triazole 17 gave the corresponding hydrazones 18 and 19, respectively. Cyclization of the latter hydrazones yielded the corresponding pyrazolo[5,1-c]-1,2,4- triazine and 1,2,4-triazolo[5,1-c]-1,2,4-triazine derivatives 20 and 21, respectively. The structures of the synthesized compounds were assigned on the basis of elemental analysis, IR, 1H NMR and mass spectral data. All the synthesized compounds were tested for in vitro activities against certain strains of fungi such as Aspergillus niger, Aspergillus nodulans, Alternaria alternate. Compounds showed marked inhibition of fungal growth nearly equal to the standards.

      • KCI등재

        The novel polythiadiazole polymer and its composite with a-Al(OH)3 as inhibitors for steel alloy corrosion in molar H2SO4: Experimental and computational evaluations

        Hany M Abd El-lateef,K. Shalabi,Abdelwahed R. Sayed,Sobhi M. Gomha,Esam M. Bakir 한국공업화학회 2022 Journal of Industrial and Engineering Chemistry Vol.105 No.-

        Polymer/composite materials have been commonly used as corrosion inhibitors in different fields such asmarine, oil field, and engineering industry due to their self-healing and thermal stability features. Herein,novel polythiadiazole, namely poly[(2,6-dicarbonylpyridine)(2,5-dihydrazinyl-1,3,4-thiadiazole)] (AMTP)via the interaction of 2,5-dihydrazinyl-1,3,4-thiadiazole with pyridine-2,6-dicarbonyl dichloride and itscomposite with a-Al(OH)3-gel were designed in a good yield. The structures of the fabricated materialsare characterized by FT-IR, NMR, SEM, and UV–Vis analyses. The protective action of AMTP and a-Al(OH)3@AMTP on the C1018-steel corrosion in molar-sulphuric acid was evaluated by potentiodynamicpolarization(PDP) and electrochemical impedance spectroscopic (EIS) methods. PDP findings presentedthat the AMTP polymer and a-Al(OH)3@AMTP composite performed as mixed-type inhibitors. The protectioncapacities of 90.3 and 97.6% were obtained in the presence of optimum dose 100 mg/L ofAMTP polymer and a-Al(OH)3@AMTP composite, respectively. The compound’s adsorption on C1018-steel follows the Langmuir isotherm model. The SEM/EDX outcomes reveal that the C1018-steel interfaceis inhibited by AMTP polymer and a-Al(OH)3@AMTP composite. DFT calculations exhibited that the efficiencyof the prepared materials correlates well with their electron contributing capability, whereas simulationsof Monte Carlo exposed that the favorability and extent of adsorption of additive moleculesmetal interface establish their corrosion protection routines.

      • KCI등재

        Novel Polyazaheterocyclic Systems: Synthesis, Antitumor, and Antimicrobial Activities

        Sayed M. Riyadh,Sobhi M. Gomha,Thoraya A. Farghaly 대한약학회 2010 Archives of Pharmacal Research Vol.33 No.11

        A series of new polyazaheterocyclic ring systems was synthesized via the reaction of enaminone 5 with active methylene compounds, hydrazine hydrate, hydroxylamine, and heterocyclic amines. The structures of the newly synthesized compounds were substantiated on the basis of spectral data and elemental analyses. The antitumor activity of the enaminone 5 against the human breast cell line MCF-7, the liver carcinoma cell line HEPG2-1, and HELA cells was determined. In addition, the antimicrobial activity of some selected products was evaluated.

      • KCI등재

        Synthesis of a new series of angiotensin II receptor antagonists and antibacterial agents

        Thoraya A. Farghaly,Sobhi M. Gomha,Mohamed M. Abdalla 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.3

        2-(Arylmethylenehydrazono)-4,4-diphenyl-1Himidazol-5(4H)-one 3 underwent regioselective cyclizationupon treatment with bromine in acetic acid containingsodium acetate to give the respective 3-substituted-6,6-diphenyl-6,7-dihydro-imidazo[2,1-c][1,2,4]triazole-5-one 4in overall good yields and not the isomeric structure 5. Inaddition, compound 4 was synthesized by alternativemethod via reaction of compound 1 with different acids inacetic acid. The synthesized hydrazone derivatives werescreened for their angiotensin II receptor antagonistsactivity and the results showed promising activity. Also,imidazo[2,1-c][1,2,4]triazole-5-ones 4 were screened forthe antibacterial activity and the result revealed that twoderivatives have excellent activity.

      • SCIESCOPUSKCI등재

        Synthesis of a new series of angiotensin II receptor antagonists and antibacterial agents

        Farghaly, Thoraya A.,Gomha, Sobhi M.,Abdalla, Mohamed M. 대한약학회 2014 Archives of Pharmacal Research Vol.37 No.3

        2-(Arylmethylenehydrazono)-4,4-diphenyl-1H-imidazol-5(4H)-one 3 underwent regioselective cyclization upon treatment with bromine in acetic acid containing sodium acetate to give the respective 3-substituted-6,6-diphenyl-6,7-dihydro-imidazo[2,1-c][1,2,4]triazole-5-one 4 in overall good yields and not the isomeric structure 5. In addition, compound 4 was synthesized by alternative method via reaction of compound 1 with different acids in acetic acid. The synthesized hydrazone derivatives were screened for their angiotensin II receptor antagonists activity and the results showed promising activity. Also, imidazo[2,1-c][1,2,4]triazole-5-ones 4 were screened for the antibacterial activity and the result revealed that two derivatives have excellent activity.

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