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A series of Amidrazones, Triazoles, Thiatriazole and Triazine derivatives was synthesized, and their antibacterial and antioxidant activities were evaluated. Biological screening showed that the majority of the compounds possess a moderate antibacterial activity and a significant antioxidant effects. In order to further research the compound 3a, the crystal structure was detected by X-ray diffraction. Meanwhile, the structural assignments of the new products were done on the basis of IR, 1H NMR, 13C NMR, elemental analysis and HRMS (ESI) spectroscopy.

Over the last few decades, Rumex species have been recognized as a promising source of new compounds with numerous pharmacological activities. Therefore, the antioxidant activity of Rumex tingitanus (R. tingitanus) leaves extracts was evaluated in vitro and then confirmed in vivo as well as the antidepressant-like and toxicological effects of the extracts. The ethyl acetate fraction (Rt EtOAcF) followed by hydroalcoholic extract (Rt EtOH-H2O) showed a remarkable in vitro antioxidant activity. The hydroalcoholic extract (Rt EtOH-H2O) showed significant hepatoprotective activity against carbon tetrachloride- (CCl4-) induced liver toxicity which is seen from inhibition of the malondialdehyde (MDA) accumulation and enhancement of the liver antioxidant enzymes activities. The Rt EtOH-H2O and Rt EtOAcF extracts were able to reduce the immobility time in mice and then elicited a significant antidepressant-like effect. The ethyl acetate fraction (Rt EtOAcF) was purified and resulted in the identification of a new antioxidant component called 4′-p-acetylcoumaroyl luteolin. The Rt EtOAcF and the 4′-p-acetylcoumaroyl luteolin revealed a strong antioxidant activity using DPPH test with IC50 of 11.7 ± 0.2 and 20.74 ± 0.6 μg/ml, respectively, and AAI of 3.39 and 1.92 better than that of BHT, used as control.

This study was undertaken to investigate the antibacterial and antifungal activities of Rumex tingitanus leaves extracts as well as the identification of bioactive components and their performance in meat preservation. Total phenolics and flavonoids showed the highest content of phenolics and flavonoids in the ethyl acetate fraction (Rt EtOAcF). For antimicrobial efficacy, leaves extract and derived fraction were tested for their capacity to inhibit bacterial and fungal proliferation in vitro and in vivo . The ethyl acetate fraction showed the most potent antibacterial and antifungal activities compared to the others extracts. Thus, the efficacy of this extract to inhibit the proliferation of Listeria monocytogenes in minced beef meat model was examined. This fraction eradicates the L. monocytogenes population in meat in a concentration- and time-dependent manner. A bio-guided purification of the Rt EtOAc fraction resulted in the isolation of the compound responsible for the observed antimicrobial activity. This compound was identified as luteolin by analysis of spectroscopic data. Chemical compounds isolated in this article Luteolin (PubChem CID: 5280445); p -iodonitrotetrazolium chloride (PubChem CID: 64957); Amphotericin B (PubChem CID: 5280965); Gentamicin and (PubChem CID: 6419933); Hexane (PubChem CID: 8058); Methanol (PubChem CID: 887); Ethanol (PubChem CID: 702); Dimethylsulfoxide (PubChem CID: 679); Quercetin (PubChem CID: 5280343); Gallic acid (PubChem CID: 370).

This study describes the antimicrobial and antioxidant activities of the extracts of Hammada scoparia (H. scoparia) and its major alkaloids. Total phenolic content showed that the hydroethanolic extract has the highest phenolic concentration (75.32 mg GAE/g) followed by methanolic extract (59.75 mg GAE/g) and the dichloromethane one with a concentration of 35.23 mg GAE/g. The antioxidant activities exhibited by the hydroethanolic extract and the organic ones were assessed by three methods 2,2-diphenyl-1-picrylhydrazyl (DPPH), β-carotene–linoleic acid system, and reducing activity. The hydroethanolic extract showed the highest scavenging activity (EC50 = 24 μg/mL) and a strong β-carotene–linoleate inhibition, better than the activities of the organic extracts. All the extracts, except of the hexane one, showed antibacterial activity against both Gram-positive and Gram-negative microorganisms with diameter inhibition zones ranged from 8 to 30 mm. The fractionation of the crude extract of H. scoparia afforded two major compounds, carnegine (1) and N-methylisosalsoline (2). The study of their antimicrobial activity showed that the carnegine was more active with minimal inhibitory concentration (MIC) and minimal bactericidal concentration (MBC) ranging from 0.125 to 0.5 mg/mL and 0.25–2 mg/mL, respectively. The time-kill curves of carnegine showed a potent and rapid bactericidal activity. The investigation of the antioxidant activity of these two alkaloids showed that, contrarily to the carnegine, the N-methylisosalsoline exhibited an antioxidant activity. The structure–activity relationship of these alkaloids was discussed.

The increasing insect resistance against Bacillus thuringiensis delta-endotoxins is a serious problem which makes it urgent to look for new eco-friendly strategies. Combining these toxins with other biomolecules is one of the promising strategies against insect pests. In this work, we evaluated the bioinsecticidal potential of Rumex tingitanus extracts and B. thuringiensis strain BLB250 against Spodoptera littoralis (Lepidoptera: Noctuidae) larvae. The chemical composition of the hexane extract, the most active fraction, was analyzed to validate the correlation between chemical composition and biological activity. Among the tested extracts, only the hexanic extract showed toxicity against first and second instar larvae with LC50 of 2.56 and 2.95 mg g−1, respectively. The Bacillus thuringiensis BLB250 delta-endotoxins showed toxicity with an LC50 of 56.3 μg g−1. Therefore, the investigated combinational effect of BLB250 delta-endotoxins and R. tingitanus hexane extract proved significant synergistic effect against S. littoralis larvae. The GC-MS analysis of R. tingitanus hexane extract showed the richness of this extract in phytosterols such as β and γ-sitosterol (48.91%), campesterol (6.43%), and β-amyrin (8.92%) which are known for their insecticidal activity. This novel finding highlights the potential use of this combination against insect pests to prevent the appearance of resistance problems.

Over the last few decades, Rumex species have been recognized as a promising source of new compounds with numerous pharmacological activities. Therefore, the antioxidant activity of Rumex tingitanus (R. tingitanus) leaves extracts was evaluated in vitro and then confirmed in vivo as well as the antidepressant-like and toxicological effects of the extracts. The ethyl acetate fraction (Rt EtOAcF) followed by hydroalcoholic extract (Rt EtOH-H2O) showed a remarkable in vitro antioxidant activity. The hydroalcoholic extract (Rt EtOH-H2O) showed significant hepatoprotective activity against carbon tetrachloride- (CCl4-) induced liver toxicity which is seen from inhibition of the malondialdehyde (MDA) accumulation and enhancement of the liver antioxidant enzymes activities. The Rt EtOH-H2O and Rt EtOAcF extracts were able to reduce the immobility time in mice and then elicited a significant antidepressant-like effect. The ethyl acetate fraction (Rt EtOAcF) was purified and resulted in the identification of a new antioxidant component called 4′-p-acetylcoumaroyl luteolin. The Rt EtOAcF and the 4′-p-acetylcoumaroyl luteolin revealed a strong antioxidant activity using DPPH test with IC50 of 11.7 ± 0.2 and 20.74 ± 0.6 μg/ml, respectively, and AAI of 3.39 and 1.92 better than that of BHT, used as control.

A straightforward method has been developed for the synthesis of 1-phenyl-imidazo [2,1-c][1,2,4]triazole derivatives 5a–j and 1-phenyl-[1,2,4]triazolo[4,3-a]pyrimidinones derivatives 6a–g starting from 5-amino-1-phenyl[1,2,4]triazole and p-toluenesulfonic acid (PTSA). This methodology affords a number of 1-phenyl-imidazo [2,1-c][1,2,4]triazoles 5a–j and 1-phenyl-[1,2,4]triazolo[4,3-a]pyrimidinones 6a–g in reasonable yields and short reaction times. The structures of all new compounds were elucidated using infrared, 1H and 13C NMR, and high-resolution mass spectrometry. Some of the newly synthesized compounds were screened for their antimicrobial activity. [Supplementary materials are available for this article. Go to the publisher's online edition of Synthetic Communications® for the following free supplemental resource(s): Full experimental and spectral details.]

International audience; Bioactive glass particle is used in the repair of bone defects. This material undergoes a series of surface in vivo reactions, which leads to osteointegration. We evaluated the effect of the bioactive glass synthesis, sol-gel (BG(S)) versus melting (BG(M)), associated with polyvinyl-alcohol (PVA) on in vivo bioactivity with biochemical parameters, liver-kidney histological structure and antibacterial in vitro activity. These composites were testified in many bacteria and implanted in ovariectomized rat. The serum and organs (liver and kidney) of all groups, control and treated rats, were collected to investigate the side effects of our composites, BG(S)-PVA and BG(M)-PVA, in comparison with control and ovariectomized rats. Also, the implants, before and after implantation, were prepared for analysis using physicochemical techniques such as Fourier transform infrared spectroscopy and X-ray diffraction. Our results have shown the stability of natremia, kaliemia, calcemia and phosphoremia. The histological structures of liver and kidney in implanted rats are intact compared to control and ovariectomized rats. BG(S)-PVA is characterized by a higher antibacterial effect on negative and positive gram bacteria than BG(M)-PVA. The physicochemical results have confirmed a progressive degradation of BG(S)-PVA and BG(M)-PVA, while replacing the implant by an apatite layer. But this bioactivity of BG(S)-PVA is faster than BG(M)-PVA. We can therefore confirm, on the one hand, the biocompatibility of our two implants and, on the other hand, the beneficial effect of sol-gel synthesis technique versus melting, both on the antibacterial effect and on the rapid formation of layer hydroxyapatite, and consequently on osteogenesis

International audience; The Groebke-type multicomponent reaction between 5-amino-1,2,4-triazole derivatives, aromatic aldehydes and isocyanides has been studied from the viewpoint of convenient generation of combinatorial arrays of imidazo[2,1-c][1,2,4]triazoles. The reaction is considered to proceed via the formation of an iminium species followed by a [4 + 1] cyclo addition with the isocyanides using scandium triflate as a Lewis acid catalyst. The synthesized imidazo[2,1-c][1,2,4]triazole derivatives 4a, 4b, 4f and 4g were screened for antibacterial, antifungal and antioxidant activities. Among the tested compounds, 4b followed by 4f showed potent antibacterial and antifungal activities. All of these compounds were also screened in vitro for the antioxidant activity using DPPH assay. Most of them have shown very significant antioxidant activity.

Compound (IIIc) is found to exhibit strong antibacterial and moderate antifungal activities.