Khairy A. M. El-Bayouki

Silica Sulfuric Acid: An Efficient, Reusable, Heterogeneous Catalyst for the One-Pot, Five-Component Synthesis of Highly Functionalized Piperidine Derivatives

Abstract A series of highly functionalized piperidine derivatives was synthesized through one-pot, five-component reaction of aldehydes, amines, and β-ketoesters. Silica sulfuric acid efficiently catalyzes the reaction to afford the corresponding piperidine derivatives in good yields. As a representative example, heating of 4-methylaninle, 4-fluorobezaldehyde, and methyl-acetoacetate in methanol in the presence of silica sulfuric acid furnished the corresponding ethyl 2,6-bis(4-fluorophenyl)-1-p-tolyl-4-(p-tolylamino)-1,2,5,6-tetrahydropyridine-3-carboxylate in excellent yield (85%). Most of the synthesized compounds were screened in vitro for their antibacterial and antifungal activities. Most of compounds showed significant antibacterial activity. GRAPHICAL ABSTRACT

Utilization of isatoic anhydride in the syntheses of various types of quinazoline and quinazolinone derivatives

ABSTRACT Isatoic anhydride has attracted a great deal of attention in recent decades. A review of the methods of preparation of all known quinazoline and quinazolinone derivatives is given herein. Isatoic anhydrides react with some nitrogen nucleophiles, followed by cyclocondensation by electrophiles, to produce several quinazoline and quinazolinone derivatives. These compounds find use as medicinal and pharmacological substances. GRAPHICAL ABSTRACT

New series of 4(3H)-quinazolinone derivatives: syntheses and evaluation of antitumor and antiviral activities

New series of 3-(3-trifluoromethylphenyl)-6-iodo-4(3H)-quinazolinone derivatives bearing thiosemicarbazones, pyrazoles, azomethine moieties at C-2 were synthesized. The obtained products were screened for their expected anticancer activity against; human liver cancer cell line (HepG2), breast cancer cell line (MCF-7) and human lung adenocarcinoma epithelial cell line (A549) tumor cell lines. Cytotoxicity of the synthesized compounds showed good IC50 for some products in comparison with the standard drug, doxorubicin. On the other hand, antiviral activity of the synthesized products against H5N1 showed moderate to weak activity compared to Zanamivir reference drug.

Synthesis, Characterization, and Molluscicidal Activity of Mn, Co, Ni, and Cu Complexes of Ethyl 5-Amino-2-(Methylthio) Thiazole-4-Carboxylate

The Mn, Co, Ni, and Cu complexes of ethyl 5-amino-2-(methy lthio) thiazole-4-carboxylate were synthesized. The structure of the metal complexes was established by microanalyses, IR, and UV-vis spectra. Thermal and electron spin resonance properties of the metal complexes were studied by TGA and ESR techniques. Metal complexes analyses suggested that: the ligand coordinated to the metal ions via nitrogen of amino group and the oxygen of carbonyl group; the synthesized complexes are binuclear with four-coordinated metal centers. Moreover, octahedral structure is suggested for all complexes. Molluscicidal activity of metal complexes was tested against Biomphalaria alexandrina snails.

New Biguanides as Anti-Diabetic Agents, Part II: Synthesis and Anti-Diabetic Properties Evaluation of 1-Arylamidebiguanide Derivatives as Agents of Insulin Resistant Type II Diabetes: New Biguanides as Anti-Diabetic Agents

New 1‐arylamidebiguanide hydrochloride salts were synthesized via reaction of hydrazide derivatives with dicyandiamide in acidic medium. The structure of the obtained derivatives was characterized by spectroscopic and elemental analysis tools. The anti‐diabetic properties of the synthesized compounds were determined. Oral treatment of hyperglycemic rats with the synthesized biguanide derivatives showed a significant decrease of the elevated glucose in comparison with the anti‐diabetic standard drug, metformin. The effects of the synthesized biguanide derivatives on the diabetic properties regarding liver function enzyme activities (AST, ALT, and ALP), lipid profiles (TC, TG, and TL), lipid peroxide, and nitrous oxide as well as histopathological characteristics were investigated and discussed.