Essam M. Hussein

A green synthetic approach to the synthesis of Schiff bases from 4-amino-2-thioxo-1,3-diazaspiro[5.5]undec-4-ene-5-carbonitrile as potential anti-inflammatory agents.

A green, novel, rapid, and efficient protocol is developed for the synthesis of various Schiff bases from 4-amino-2-thioxo-1,3-diazaspiro[5.5]undec-4-ene-5-carbonitrile using ammonium chloride as a very inexpensive and readily available reagent in refluxing ethanol. High yields, easy work-up, and short reaction times are advantages of this environmentally benign procedure. The prepared compounds were screened for their anti-inflammatory activity “at a dose of 10 mg/kg body weight,” which revealed promising activities relative to indomethacin used as a reference standard in this study.

Synthesis and Reactions of Some New Spiropyranthiazoline Derivatives

Pyrano[2,3-d]thiazoline-7-spiro-3′-(1′-substitutedindoline-2′-ones) 5a,b has been synthesized and reacted with some nucleophile reagents to afford new spirothiazolino[4,5:2′,3′]pyrano[6′,5′-d]pyrimidine derivatives 6a,b–13a,b, which are analogues of some reported biologically active spiroheterocyclic compounds.

Enviro-economic, Ultrasound-assisted One-pot, Three-component Synthesis of Pyrido(2,3-d)pyrimidines in Aqueous Medium

Tetra-n-butyl ammonium bromide (TBAB) was found to be an efficient phase-transfer catalyst for the synthesis of pyrido[2,3-d]pyrimidines by one-pot reaction of 6-aminouracils, aromatic aldehydes, and malononitrile or ethyl cyanoacetate in water under ultrasonic irradiation. The advantages of this method are the use of an inexpensive and readily available catalyst, short reaction time, easy work-up, improved yields, and the use of water as a solvent that is environmentally benign. Graphical Abstract Enviro-economic, Ultrasound-assisted One-pot, Three-component Synthesis of Pyrido[2,3-d]pyrimidines in Aqueous Medium

A convenient regioselective synthesis of spirooxindolinopyrrolizidines incorporating the pyrene moiety through a [3 + 2]-cycloaddition reaction

Abstract A facile one-pot synthesis of spirooxindolinopyrrolizidines incorporating the pyrene moiety was accomplished in good yields through a 1,3-dipolar cycloaddition reaction of 3-aryl-1-(pyren-1-yl)prop-2-en-1-one derivatives with in situ-generated azomethine ylides.

Synthesis of some novel 6′-(4-chlorophenyl)-3,4′-bipyridine-3′-carbonitriles: assessment of their antimicrobial and cytotoxic activity

Abstract A series of novel substituted 6′-(4-chlorophenyl)-3,4′-bipyridine-3′-carbonitriles with incorporated pyrazole and/or triazole moieties have been synthesized using 2-(6′-(4-chlorophenyl)-3′-cyano-3,4′-bipyridin-2′-yloxy)acetohydrazide (3) as starting material. Also, the key intermediate 3 reacted with aromatic aldehydes and tosyl chloride to give the corresponding Schiff bases and tosyl hydrazide derivatives, respectively. The antimicrobial of these newly synthesized compounds was evaluated against Bacillus subtilis as Gram-positive bacteria and Trichoderma viride as a fungus; some of these compounds such as 5, 6, 7, 8, 10, 12, and 14 showed excellent activities as antimicrobial agents. Moreover, the cytotoxic activity of the most active compounds was assessed in vitro against human tumor liver cancer cell line (HEPG2); compounds 8, 10, 13a, and 14 showed potent activities relative to Doxorubicin which was used as a reference standard drug in this study.