New Azacycles by One-Pot Three-Component Hantzsch-Like Synthesis of Tetra(hexa)azacyclopenta[a]anthracenes, Tetraazaindeno[5,4-b]fluorenes, and Oxatetraazacyclopenta[m]tetraphenes

Multicomponent reactions (MCRs) are envisaged as an entry point for the synthesis of heterocyclic compounds with interesting biological activities. An efficient approach to annelated tetra(hexa)azacyclopenta[a]anthracenes, tetraazaindeno[5,4-b]fluorenes, and oxatetraazacyclopenta[m]tetraphene was accomplished using a three-component reaction involving 7-amino-2-methyl-3-phenylpyrazolo[1,5-a]pyrimidin-5-one with aromatic aldehydes and the corresponding active 1,3-dicarbonyl compounds (namely, dimedone, 1,3-dimethylbarbituric acid, 1,3-indanedione, and 4-hydroxycoumarine). The reactions were conducted in glacial acetic acid at reflux for 5 h to give the desired products in good yields (62–83 %). The chemical constitutions of all new products were confirmed spectroscopically

Hantzsch-like three-component synthesis of <i>bis</i>(1,4-dihydropyridines) and <i>bis</i>(fused-1,4-dihydropyridines) linked to piperazine core <i>via</i> 2-phenoxyethanone linkage: Novel hybrid molecules

The molecular hybridization of various compounds with known pharmacological activity is a particularly popular approach for the development of potential drugs with improved pharmacokinetic profiles. In this respect, a novel series of bis(1,4-dihydropyridine-3,5-dicarbonitrile), bis(decahydroacridine), bis(tetrahydrodipyrazolo[3,4-b:4′,3′-e]pyridin), and bis(tetrahydropyrimido[4,5-b]quinoline-2,4,6-trione) derivatives linked to piperazine core via phenoxyethanone linkages were prepared via Hantzsch like reaction of the ((piperazine-1,4-diylbis(2-oxoethane-2,1-diyl))bis(oxy))dibenzaldehydes, with the appropriate active methylene containing reagents. Attempted synthesis of the target products via bis-alkylation of the appropriate phenol with 1,1′-(piperazine-1,4-diyl)bis(2-chloroethan-1-one) in different basic conditions were unsuccessful. </p

Expression of Reactive Oxygen Species–Related Transcripts in Egyptian Children With Autism

The molecular basis of the pathophysiological role of oxidative stress in autism is understudied. Herein, we used polymerase chain reaction (PCR) array to analyze transcriptional pattern of 84 oxidative stress genes in peripheral blood mononuclear cell pools isolated from 32 autistic patients (16 mild/moderate and 16 severe) and 16 healthy subjects (each sample is a pool from 4 autistic patients or 4 controls). The PCR array data were further validated by quantitative real-time PCR in 80 autistic children (55 mild/moderate and 25 severe) and 60 healthy subjects. Our data revealed downregulation in GCLM, SOD2, NCF2, PRNP , and PTGS2 transcripts (1.5, 3.8, 1.2, 1.7, and 2.2, respectively; P < .05 for all) in autistic group compared with controls. In addition, TXN and FTH1 exhibited 1.4- and 1.7-fold downregulation, respectively, in severe autistic patients when compared with mild/moderate group ( P = .005 and .0008, respectively). This study helps in a better understanding of the underlying biology and related genetic factors of autism, and most importantly, it presents suggested candidate biomarkers for diagnosis and prognosis purposes as well as targets for therapeutic intervention