Phytochemicals and enzymes inhibitory potentials of leaves and rootbarks of Sarcocephallus latifolius (smith): In vitro and in silico investigations.

In this study, bioactive compounds were isolated and characterized from the leaves and root-barks extracts of S.latifolius, with subsequent in vitro experimental investigations for antihyperglycemic potentials on α-amylase and α-glucosidase enzymes. Thirteen bioactive compounds were identified, including 10-Hydroxystrictosamide (2) and Quinovic acid-3-O-α-L-rhamnosyl-28-O-β-d-glucopyranosyl ester (8), using chromatographic, nuclear magnetic resonance spectroscopy (NMR), and mass spectrometry (MS) techniques.

Mono and di -C-H acetoxylation of 2-aryloxyquinoline-3-carbaldehydes.

2-Aryloxyquinolines are well known for various biological activities. In this report, we have developed a novel protocol for introducing an acetoxy functional group on the aryl sp carbon of 2-aryloxyquinoline-3-carbaldehyde using a palladium catalyst for the first time. Interestingly, this C-H acetoxylation reaction is highly chemo- and site-selective.

Synthesis, crystal structure and in-silico evaluation of arylsulfonamide Schiff bases for potential activity against colon cancer.

This report presents a comprehensive investigation into the synthesis and characterization of Schiff base compounds derived from benzenesulfonamide. The synthesis process, involved the reaction between N-cycloamino-2-sulfanilamide and various substituted o-salicylaldehydes, resulted in a set of compounds that were subjected to rigorous characterization using advanced spectral techniques, including H NMR, C NMR and FT-IR spectroscopy, and single-crystal X-ray diffraction. Furthermore, an in-depth assessment of the synthesized compounds was conducted through Absorption, Distribution, Metabolism, Excretion and Toxicity (ADMET) analysis, in conjunction with docking studies, to elucidate their pharmacokinetic profiles and potential.

N-Cycloamino substituent effects on the packing architecture of ortho-sulfanilamide molecular crystals and their in silico carbonic anhydrase II and IX inhibitory activities.

In the search for new `sulfa drugs' with therapeutic properties, o-nitrosulfonamides and N-cycloamino-o-sulfanilamides were synthesized and characterized using techniques including H NMR, C NMR and FT-IR spectroscopy, and single-crystal X-ray diffraction (SC-XRD). The calculated density functional theory (DFT)-optimized geometry of the molecules showed similar conformations to those obtained by SC-XRD. Molecular docking of N-piperidinyl-o-sulfanilamide and N-indolinyl-o-sulfanilamide supports the notion that o-sulfanilamides are able to bind to human carbonic anhydrase II and IX inhibitors (hCA II and IX; PDB entries 4iwz and 5fl4).

Antifouling Polyethersulfone-Petrol Soot Nanoparticles Composite Ultrafiltration Membrane for Dye Removal in Wastewater.

Engineered nanoparticles are known to boost membrane performance in membrane technology. Hitherto, tunable properties that lead to improved hydrophilicity due to increased surface oxygen functionalities upon oxidation of petrol soot have not been fully exploited in membrane filtration technology. Herein, the integration of oxidized petrol soot nanoparticles (PSN) into polyethersulfone ultrafiltration membranes produced via phase inversion technique for dye removal in wastewater is reported.

Synthesis of substituted N-(2'-nitrophenyl)pyrrolidine-2-carboxamides towards the design of proline-rich antimicrobial peptide mimics to eliminate bacterial resistance to antibiotics.

The treatment of diseases is under threat due to the increasing resistance of disease-causing bacteria to antibiotics. Likewise, free radical-induced oxidative stress has been implicated in several human disease conditions, such as cancer, stroke and diabetes. In the search for amino acid analogues with antibacterial and antioxidant properties as possible mimics of antimicrobial peptides, substituted N-(2'-nitrophenyl)pyrrolidine-2-carboxamides 4a-4k and N-(2'-nitrophenyl)piperidine-2-carboxamides 4l-4n have been synthesized via a two-step, one-pot amidation of the corresponding acids, using thionyl chloride with different amines in dichloromethane.

Synthesis, crystal structure and docking studies of tetracyclic 10-iodo-1,2-dihydroisoquinolino[2,1-b][1,2,4]benzothiadiazine 12,12-dioxide and its precursors.

The title compound, 10-iodo-1,2-dihydroisoquinolino[2,1-b][1,2,4]benzothiadiazine 12,12-dioxide, CHINOS (8), was synthesized via the metal-free intramolecular N-iodosuccinimide (NIS)-mediated radical oxidative sp-C-H aminative cyclization of 2-(2'-aminobenzenesulfonyl)-1,3,4-trihydroisoquinoline, CHNOS (7). The amino adduct 7 was prepared via a two-step reaction, starting from the condensation of 2-nitrobenzenesulfonyl chloride (4) with 1,2,3,4-tetrahydroisoquinoline (5), to afford 2-(2'-nitrobenzenesulfonyl)-1,3,4-trihydroisoquinoline, CHNOS (6), in 82% yield. The catalytic hydrogenation of 6 with hydrogen gas, in the presence of 10% palladium-on-charcoal catalyst, furnished 7.

Phytochemical study of , a medicinal plant grown in Nigeria.

(Schumach.) Milne-Redhead. (Leguminosae) is used for various medicinal purposes in African countries.

Chemical and biological studies on Bridelia ferruginea grown in Nigeria.

Phytochemical investigation of the methanolic extract of dried leaves of Bridelia ferruginea led to the isolation and identification of fourteen compounds (1-14): compound 1 [mixture of palmitic, stearic and oleic acids], stearyl monoester of 2-O-β-ᴅ-glucosylglycerol (2), 6β-hydroxy-(20R)-24-ethylcholest-4-en-3-one (3a), 6β-hydroxy-(20R)-24-ethylcholest-4,22-dien-3-one (3b), lutein (4), vomifoliol (5), corilagin (6), kaempferide-3-O-β-ᴅ-glucoside (7), myricetin (8), isomericitrin (9), isoquercetin (10), myricitrin (11), quercitrin (12), rutin (13), and β-sitosterol glucoside (14). The total extract exhibited moderate activity towards CB2 receptor and 90% inhibition against leishmanial pathogen Trypanosoma brucei. Compound 4 exhibited 73% displacement in CB2 receptor with IC 56.

Antioxidant and Free Radical Scavenging Capacity of Seed and Shell Essential Oils Extracted from Abrus precatorius (L).

Essential oils from plants have been proven safe as natural antioxidants, and few are already marketed as digestive enhancers as well as in prevention of several degenerative diseases. This study evaluated the antioxidant capacity of seed and shell essential oils of Abrus precatorius (L), a herb used for ethno-medicinal practices in Nigeria. The essential oils were obtained by hydro-distillation.

Effect of Flabellaria paniculata Cav. extracts on gastric ulcer in rats.

Background: The leaves and root of Flabellaria paniculata (Malpighiaceae) are frequently used in the treatment of wounds and ulcers in Nigerian folk medicine. The purpose of this study was to compare the effect of ethanolic extracts from the leaves (FPL) and root (FPR) of F. paniculata on gastric ulcers in rats.

Room temperature synthesis and antibacterial activity of new sulfonamides containing n,n-diethyl-substituted amido moieties.

Sulfonamide drugs which have brought about an antibiotic revolution in medicine are associated with a wide range of biological activities. We have synthesized a series of α-tolylsulfonamide, 1-11 and their substituted N,N-diethyl-2-(phenylmethylsulfonamido) alkanamide derivatives, 12-22 in improved and excellent yields in aqueous medium at room temperature through highly economical synthetic routes. The chemical structures of the synthesized compounds 1-22 were confirmed by analytical and spectral data such as IR, (1)H- and (13)C-NMR, and mass spectra.

Composition and antioxidant activities of leaf and root volatile oils of Morinda lucida.

Morinda lucida (L.) Benth. (Rubiacae) is used in traditional medicine in many West African countries for the treatment of various human diseases.

Phenolic contents, antioxidant and antibacterial activities of Hymenocardia acida.

This study investigates the antioxidant and antibacterial activities of aqueous and methanolic extracts from Hymenocardia acida Tul. (Hymenocardiaceae). The inhibition values of the extracts and quercetin were found to be very close, with no significant differences at a concentration of 0.

The Baylis-Hillman approach to quinoline derivatives.

Baylis-Hillman reactions of 2-nitrobenzaldehydes with various activated alkenes afford adducts that undergo reductive cyclisation to quinoline derivatives. The chemo- and regioselectivity of cyclisation appears to be influenced by the choice of both the substrate and the reagent system, and competing reactions have been observed.