Design, synthesis, docking studies and bioactivity evaluation of 1,2,3-triazole eugenol derivatives.

The design, synthesis, docking studies and evaluation of the antifungal and cytotoxic properties of eugenol (EUG) containing 1,2,3-triazole derivatives are reported. Most of the derivatives have not been reported. The EUG derivatives were synthesized, molecular docked and tested for their antifungal activity.

Powerful antioxidants within Greene female cones and leaves essential oil.

The composition and antioxidant activity of the essential oil obtained from the female cones and leaves of were assessed using the DPPH assay. The total oil yields obtained through hydrodistillation from the female cones and leaves were 1.9% (v/w) and 0.

Montmorillonite K10 Clay Catalyzed Synthesis of Novel β-Aminocarbonyl Compounds and Their Biological Evaluation.

An efficient and reusable green catalyst for the synthesis of β-aminocarbonyl compounds has been developed. In this new and greener approach, β-aminocarbonyl compounds (1a-1r) were obtained by Montmorillonite K10 clay catalyzed reaction of aryl amines, aliphatic/aromatic aldehydes and β-ketoesters. Molecular docking investigations were performed for all compounds (1a-1r) with the proteins PDB ID: 1JIJ and 1KZN for S.

Natural Abenquines and Their Synthetic Analogues Exert Algicidal Activity against Bloom-Forming Cyanobacteria.

Abenquines are natural quinones, produced by some Streptomycetes, showing the ability to inhibit cyanobacterial growth in the 1 to 100 μM range. To further elucidate their biological significance, the synthesis of several analogues (4f-h, 5a-h) allowed us to identify some steric and electronic requirements for bioactivity. Replacing the acetyl by a benzoyl group in the quinone core and also changing the amino acid moiety with ethylpyrimidinyl or ethylpyrrolidinyl groups resulted in analogues 25-fold more potent than the natural abenquines.

Chemical Variability and Biological Activities of Eucalyptus spp. Essential Oils.

Many plant species produce mixtures of odorous and volatile compounds known as essential oils (EOs). These mixtures play important roles in Nature and have been utilized by mankind for different purposes, such as pharmaceuticals, agrochemicals, aromatherapy, and food flavorants. There are more than 3000 EOs reported in the literature, with approximately 300 in commercial use, including the EOs from species.

Stink bug predator kills prey with salivary non-proteinaceous compounds.

Podisus nigrispinus Dallas (Hemiptera: Pentatomidae) is a predator insect with potential applications in biological control because both nymphs and adults have been shown to prey on other insect pests by injection of toxic salivary gland contents. This study identified non-proteinaceous compounds with insecticidal activity from the saliva of P. nigrispinus in Anticarsia gemmatalis.

The fungal phytotoxin alternariol 9-methyl ether and some of its synthetic analogues inhibit the photosynthetic electron transport chain.

Alternariol and monomethylalternariol are natural phytotoxins produced by some fungal strains, such as Nimbya and Alternaria. These substances confer virulence to phytopathogens, yet no information is available concerning their mode of action. Here we show that in the micromolar range alternariol 9-methyl ether is able to inhibit the electron transport chain (IC50 = 29.

Organocatalysis in the three-component Povarov reaction and investigation by mass spectrometry.

A diastereoselective three-component cascade reaction, catalyzed by p-sulfonic acid calix[4]arene, provides a unique method to access diverse julolidine derivatives in high yields. Additionally, the reaction was also monitored by mass spectrometry and the mechanistic pathway uncovered.

Induction of G₂/M arrest, caspase activation and apoptosis by α-santonin derivatives in HL-60 cells.

Sesquiterpene lactones (SLs) are natural products with a variety of biological activities. Previously, we demonstrated the cytotoxic effects of three new α-santonin derivatives on different tumor cell lines with low toxic effects upon peripheral human leukocytes. Here, we evaluated the mechanism of action triggered by these derivatives.

Chemical characterization of volatile compounds of Lantana camara L. and L. radula Sw. and their antifungal activity.

A comparative study of the chemical composition of essential oils of two very similar species of the Verbenaceae family (Lantana camara and L. radula) revealed that the main components of essential oil of L. camara were germacrene-D (19.

Seasonal variation in the chemical composition and antimicrobial activity of volatile oils of three species of Leptospermum (Myrtaceae) grown in Brazil.

This study investigates the seasonal variation of three species of Leptospermum (Myrtaceae) grown in Brazil. The chemical composition of the volatile oils of L. flavescens and L.

Synthesis and biological evaluation of 2,5-bis(alkylamino)-1,4-benzoquinones.

A series of twelve 2,5-bis(alkylamino)-1,4-benzoquinones were prepared in yields ranging from 9-58% via the reaction between p-benzoquinone and various amines. The structures of the synthesized compounds were confirmed by IR, 1H- and 13C-NMR and MS analyses. The phytotoxicity of the 2,5-bis(alkylamino)-1,4-benzoquinones was evaluated against two crop species, Cucumis sativus and Sorgum bicolor, at 1.

Synthesis and phytotoxic activity of new pyridones derived from 4-hydroxy-6-methylpyridin-2(1H)-one.

Commercial dehydroacetic acid was converted into 4-hydroxy-6-methylpyridin-2(1H)-one (3), which was then condensed with several aliphatic aldehydes to produce seven new title compounds in variable yields (35-92%). Reaction of 3 with alpha,beta-unsaturated aldehydes resulted in the formation of condensed pyran derivatives 4g' and 4h'. A mechanism is proposed to explain the formation of such compounds.

Synthesis and phytogrowth properties of oxabicyclic analogues related to helminthosporin.

This investigation describes the synthesis and biological evaluation of a series of oxabicyclic analogues related to the helminthosporins. Four oxabicycles were prepared by [4+3] cycloaddition of an oxyallyl carbocation, generated in situ from 2,4-dibromopentan-3-one, with selected furans. Functional group manipulations of the oxabicyclic architecture generated nine further derivatives.

Evaluation of the chemical composition of Brazilian commercial Cymbopogon citratus (D.C.) stapf samples.

The concentration and the chemical composition of the essential oils obtained from different samples of Cymbopogon citratus were evaluated. Among the 12 samples investigated (11 dried leaf samples and fresh plant leaves), seven presented essential oil concentrations within the threshold established by the Brazilian legislation. The moisture content was also determined and the majority of the samples presented humidity contents near 12%.

Synthesis of new phytogrowth-inhibitory substituted aryl-p-benzoquinones.

Reaction of [(2-alkyloxy)methyl]-1,4-dimethoxybenzene 10 (alkyl=butyl, hexyl, decyl, tridecyl, tetradecyl, hexadecyl, and octadecyl) with ceric ammonium nitrate in order to produce p-benzoquinones (=cyclohexa-2,5-diene-1,4-diones) afforded 5-[(alkyloxy)methyl]-2-(4-formyl-2,5-dimethoxyphenyl)benzo-1,4-quinones 12a-12g in yields that varied from 46 to 97%, accompanied by 2-[(alkyloxy)methyl]benzo-1,4-quinones 11a-11g in only small quantities (< or =5%). These quinones resemble the natural phytotoxic compound sorgoleone, found in Sorghum bicolor. This reaction exemplifies a general procedure for the synthesis of novel aryl-substituted p-benzoquinones.