294199-10-3Relevant academic research and scientific papers
Synthesis of new azolyl azoles and azinyl azoles
Al-Saleh, Balkis,El-Apasery, Morsy Ahmed,Elnagdi, Mohamed Hilmy
, p. 483 - 486 (2005)
Synthesis of new azolyl azoles and azinyl azoles from the reaction of compounds 1, 4 and 7 with phenyl isothiocyanate is reported. Compound 10 reacts with benzene diazonium chloride to yield either phenylhydrazones 11 and 12 or the triazoloquinoline 13.
Lipase-Catalyzed Kinetic Resolution of Novel Antifungal N-Substituted Benzimidazole Derivatives
?ukowska-Chojnacka, Edyta,Staniszewska, Monika,Bondaryk, Ma?gorzata,Maurin, Jan K.,Bretner, Maria
, p. 347 - 354 (2016/03/19)
A series of new N-substituted benzimidazole derivatives was synthesized and their antifungal activity against Candida albicans was evaluated. The chemical step included synthesis of appropriate ketones containing benzimidazole ring, reduction of ketones to the racemic alcohols, and acetylation of alcohols to the esters. All benzimidazole derivatives were obtained with satisfactory yields and in relatively short times. All synthesized compounds exhibit significant antifungal activity against Candida albicans 900028 ATCC (% cell inhibition at 0.25 μg concentration > 98%). Additionally, racemic mixtures of alcohols were separated by lipase-catalyzed kinetic resolution. In the enzymatic step a transesterification reaction was applied and the influence of a lipase type and solvent on the enantioselectivity of the reaction was studied. The most selective enzymes were Novozyme SP 435 and lipase Amano AK from Pseudomonas fluorescens (E > 100).
Studies with functionally substituted heteroaromatics: The chemistry of N-phenylhydrazonylalkylpyridinium salts and of phenylhydrazonylalkylbenzoazoles
Abdel-Khalik, Mervat Mohammed,Elnagdi, Mohammed Hilmy,Agamy, Samia Michel
, p. 1166 - 1169 (2007/10/03)
2-Pyrid-1-yliniumacetonitrile bromide 1a and 2-pyrid-1- ylinium-1-phenylethanone bromide 1b coupled with benzenediazonium chloride to yield the corresponding phenylhydrazones 3a, b. Similarly, compounds 2a-c also coupled with aryldiazonium chloride, yielding the arylhydrazones 10a-b, which were used as precursors for the synthesis of azolypyfidazinones 11a, b. Compounds 3a, b were converted into 1,2,4,5-dihydrotetrazines 4a, b on refluxing in acetonitrile in the presence of ammonium acetate. Refluxing 3a in dimethylformamide resulted in the formation of the 3-cyanoindazole 6. Compound 3a was converted to pyrazole 8 on treatment with the enaminone 7, and to hydrazonyl bromide 9 on heating in dioxane/acetonitrile. Compound 12 was synthesized from the reaction of 10b with ethanolic aqueous sodium hydroxide.
