One pot synthesis of substituted 1H-benzo[f]chromen-3-yl-2H-chromen-2-one derivatives

The title compounds, substituted 1H-benzo[f]chromen-3-yl-2H-chromen-2-ones were obtained by reacting 3-aryl-1-(3-coumarinyl)propen-1-ones with 2-napthol catalyzed by DBU (1,8-diazabicyclo[5,4,0]undec-7-ene) and concentrated H2SO4 in ample yields. Their structures were characterized by IR, 1H NMR, 13C NMR, mass spectral and elemental analysis. All the synthesized compounds have been evaluated for their in-vitro antibacterial activity against Escherichia coli, Staphylococcus aureus, and Pseudomonas aeruginosa and antifungal activity against Aspergillus Niger and Candida albicans by using serial broth dilution method. Among those compounds 3 band 3c exhibits prominent results

The chemical reactivity of naphthols and their derivatives toward α-cyanocinnamonitriles and ethyl α-cyanocinnamates: A review of synthesis, reactions and applications of naphthopyrano

This review deals with synthesis and reactions of some naphthopyrano derivatives and their applications. The main purpose of this review is to present a survey of literatures on the reactivity of naphthols and their derivatives toward α-cyanocinnamonitrile or ethyl α-cyanocinnamate derivatives and the reactions of β-enaminonitriles and β-enaminoesters with different electrophiles followed by nucleophilic reagents. Some of these reactions have been applied successfully to the synthesis of biologically important compounds

Ship Shore Power Connection Sollutions in Riga Freeport

There are analyzed technical sollutions of ship on shore power supply in the Baltic ports. The result is proposals for Riga Freeport OPS implementation

Diversely substituted quinolines via rhodium-catalyzed alkyne hydroacylation

The Rh-catalyzed hydroacylative union of aldehydes and o-alkynyl anilines leads to 2-aminophenyl enones, and onwards to substituted quinolines. The mild reaction conditions employed in this chemistry result in a process that displays broad functional group tolerance allowing the preparation of diversely substituted quinolines in high yields. Extension to the use of o-alkynyl nitro arenes as substrates, leads to 2-nitrochalcones, from which both quinolines and quinoline N-oxides can be accessed.&gt

Investigating the Behavior of Published PAINS Alerts Using a Pharmaceutical Company Data Set

Biochemical assay interference is becoming increasingly recognized as a significant waste of resource in drug discovery, both in industry and academia. A seminal publication from Baell and Holloway raised the awareness of this issue, and they published a set of alerts to identify what they described as PAINS (pan-assay interference compounds). These alerts have been taken up by drug discovery groups, even though the original paper had a somewhat limited data set. Here, we have taken Lilly’s far larger internal data set to assess the PAINS alerts on four criteria: promiscuity (over six assay formats including AlphaScreen), compound stability, cytotoxicity, and presence of a high Hill slope as a surrogate for non-1:1 protein–ligand binding. It was found that only three of the alerts show pan-assay promiscuity, and the alerts appear to encode primarily AlphaScreen promiscuous molecules. Although not enriching for pan-assay promiscuity, many of the alerts do encode molecules that are unstable, show cytotoxicity, and increase the prevalence of high Hill slopes