Omneya M. Khalil

Synthesis and antimicrobial activity of certain novel quinoxalines

In this study, certain 3-methyl-2-[4-(substituted amino carbonyl)anilino] quinoxalines, (2a-d) and (3a-d), were synthesized from the new key compound 2-[4-(ethoxycarbonyl)anilino]-3-methyl quinoxaline (1). In addition, a series of 2-[4-(arylidene hydrazinocarbonyl)anilino]-3-methyl quinoxalines (5a-e), as well as their cyclized oxadiazolinyl derivatives (6a-e), and a series of 2-[4-N-acylhydrazinocarbonyl anilino]-3-methyl quinoxalines (7a-d), as well as their cyclized oxadiazoiyl derivatives (8a-d) were also prepared. Some of these derivatives were evaluated for antimicrobial activityin vitro. It was found that all the selected compounds exhibit antimicrobial activity and that compound5b had a broad spectrum of activity.

Synthesis and anti-inflammatory activity of certain piperazinylthienylpyridazine derivatives.

In this study, a novel series of 2-(4-substituted piperazin-l-ylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(3a- f), 2-(4-substituted piperazin-l-yl carbonylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(4a- c) and 2-[2-(4-substituted piperazin-l-ylcarbonylethyl)]-6-(thien-2-yl)-2H-pyridazin-3-ones(5a,b) were prepared from 6-(thien-2-yl)-2H- pyridazin-3-one(1). In addition, 3-(4-substituted piperazin-l-ylcarbonyl methyl thio)-6-(thien-2-yl) pyridazines(6a- c) and 3-[2-(4-substitutedpiperazin-l-ylcarbonyl ethylthio]-6-(thien-2-yl) pyridazines(7a,b) were synthesized. Furthermore, 5-(4-substituted piperazin-l-ylmethyl)-6-(thien-2-yl)-2H-pyridazin-3-ones(12a,b) were prepared. The structures of the new compounds were confirmed by elemental analysis as well as by1H-NMR,IR andMS data. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity against carrageenan-induced paw edema at a dose of 10 mg/kg using indomethacin as the reference standard.

Synthesis and antitumor activity of novel 6-aryl and 6-alkylpyrazolo[3,4-d]pyrimidin-4-one derivatives

A series of new 6-arylpyrazolo[3,4-d]pyrimidin-4-ones and 6-alkylpyrazolo[3,4-d]pyrimidin-4-ones were synthesized. Some of the newly synthesized compounds were tested in vitro on human colon tumor cell line (HCT116). Most of the test compounds exploited potent antitumor activity, especially compound 10a which displayed the highest activity among the test compounds with IC(50) equal to 0.47 μg/mL.

Synthesis and anti-inflammatory activity of 1-acetyl/propanoyl-5-aryl-3-(4-morpholinophenyl)-4,5-dihydro-1H-pyrazole derivatives

A series of novel pyrazoline derivatives containing 4-morpholinophenyl moiety were synthesized to investigate their potential anti-inflammatory activity. The chemical structures of the compounds were elucidated by spectral data and element analyses. The test compounds in the series exhibited different levels of anti-inflammatory activities when compared with reference drug indomethacin.

Synthesis of Some Chalcones and Pyrazolines Carrying Morpholinophenyl Moiety as Potential Anti-Inflammatory Agents

Chalcones of 2a–f and their corresponding products, pyrazolines 3a–f, were synthesized and evaluated for their anti‐inflammatory activity against carrageenan edema in albino rats at a dose of 10 mg/kg. All the compounds of this series showed promising anti‐inflammatory activity. The most active compounds of this series, 2a, 2b, and 2d, were found to be most potent. They showed higher percentage of inhibition of edema than the standard drug indomethacin.

Synthesis of tricyclic systems containing a fused thieno[3,4- d ]pyrimidine nucleus

The synthesis and characterisation of novel tricyclic systems containing a fused thieno[3,4-d]pyrimidine nucleus starting from a useful synthon, ethyl-4-cyano-3-ethoxymethyleneamino-5-phenylamino-2-thiophenecarboxylate, are reported.

Synthesis of novel pyridazinyl benzimidazole, benzothiazole and benzoxazole of expected anti-inflammatory activity

In this study, a novel series of 6-oxopyridazinyl benzazoles and 3, 6-dioxopyridazinyl benzazoles were prepared from the starting compounds, 2-hydrazinobenzimidazole, 2-hydrazinobenzothiazole and 2-hydrazinobenzoxazole by reaction with butyric acid derivatives and cyclic anhydrides respectively. The structures of the new compounds were confirmed by elemental analysis as well as 1H NMR, IR and MS data. Some of the newly prepared compounds were subjected to evaluation for their anti-inflammatory activity using carrageenan induced paw edema at dose 100 mg kg−1 using indomethacin as a reference standard and were found to be bioactive.

Synthesis and antibacterial activity of novel quinoxalinone derivatives

The reaction of 3-hydrazinocarbonylmethylquinoxalin-2(1H)-one with phthalic anhydride, certain aromatic aldehydes, isocyanates and phenyl isothiocyanate furnished corresponding imide, Schiffs, semi- and thiosemicabazide derivatives. Treatment of 3-[2-(phenylcarbamoyl)hydrazinocarbonylmethyl]quinoxalin-2(1H)-one with chloroacetic acid, sulfuric acid and sodium hydroxide yielded cyclised derivatives. Moreover, 3-[2-bromobenzylidenehydrazinocarbonyl-methyl]quinoxalin-2(1H)-one was cyclised to oxadiazolinyl derivative using acetic anhydride. Furthermore, 3-[5-sulfanylidene-4,5-dihydro-1,3,4-oxadiazol-2-yl)methyl]quinoxalin-2(1H)-one was employed as a precursor in the synthesis of some novel 2(1H)-quinoxalinones. Some of the newly prepared compounds were evaluated for in vitro antibacterial activity using ofloxacin as the reference standard.