AbstractThis study aims to synthesize hybrid compounds “via” the coupling of sulphonamide and benzothiazole into one structure that may have improved antibacterial property. The N-(biphenyl-4-yl) thiourea (1) used for the synthesis of the targeted sulphonamides was obtained by reacting diphenylamine and ammonium thiocyanate at room temperature. Cyclization of N-(biphenyl-4-yl)thiourea gave 2-amino-6-phenylbenzothiazole (2) which reacted with benzenesulphonyl chloride and para-toulene sulphonyl chloride to give the targeted sulphonamides (3a & 3b). The synthesized compounds were characterised using melting point, infra-red spectroscopy, nuclear magnetic resonance and elemental analysis. Anti-bacterial screening of the synthesised compounds indicated that all the compounds showed anti-bacterial properties, except 2-amino-6-phenylbenzothiazole that did not show any activity on Escherichia coli.
Abstract. Moringa olifera (drumstick tree) is a medicinal plant commonly used in phytomedicine to cure and prevent diseases in Nigeria. The ethanolic extract of the leave sample showed alkaloid {(9.66 ± 0.20) %}, phenols {(0.75 ± 0.22) %}, flavonoids {(6.86 ± 0.20) %}, saponines {(8.46 ± 0.10) %}, and tannins {(1.10 ± 0.20) %}. The plant also contains nutritional nutrients such as ash {(6.08 ± 0.02) %}, protein {(23.65 ± 0.12)%}, carbohydrates {(57.01 ± 0.01)%}, fats {(2.43 ± 0.01) %}, crude fibre {(6.02 ± 0.13)%}, moisture {(9.50 ± 0.10)%} and energy {(3276 ± 0.14)%}. Antibacterial studies showed that the plant leave successfully inhibited staphylococcus aureus, Escherichia coli, Pseudomonas aeruginosa, Proteus mirabilis and Klebisiella pneumonia. Acridine diglycoside was elucidated using Bruker NMR spectroscopy in combination with FT-IR NATRIC and HREIMS (m/z) mass spectral data. This result authenticates the use of the plant leave in the treatment of infections, tumors and as an anti-inflammatory agent
Gastric ulcer is one of the common cause of hospital consultation with an increasing prevalence worldwide and it is traditionally managed with herbal medicine in the developing countries. This study investigated the gastroprotective effects of methanol extract of Eremomastax speciosa leaf in rats. Cold maceration in 80% methanol was adopted during extract preparation while gas chromatography mass spectroscopy (GC-MS) was employed in the phytochemical analysis. The doses of 25, 50 and 100 mg/kg E. speciosa were used on ethanol-and indomethacin-induced gastric ulcer models in rats. The shay rat method was used to determine the effects of ESE on gastric acidity while the anticholinergic and antihistaminic activities were investigated on isolated rabbit jejunum ex vivo. The GC-MS analysis identified six bioactive compounds. Both ESE and cimetidine significantly (p < 0.05) reduced the severity of indomethacin- and ethanol-induced gastric injuries and gastric acid contents in Shay rats. The extract elicited concentration-dependent relaxation of isolated rabbit jejunum and reduced the contraction induced by both acetylcholine and histamine in the same tissue. The findings showed that ESE protected the rats against chemical-induced gastric ulcer through anticholinergic and antihistaminic mechanisms.
The 2-phenylsulphonamide derivatives of amino acids were synthesis by simple substitution of benzenesulphonylchloride (6) with amino acids (1-5) containing pharmacological active functionalities. Structures of the synthesised compounds (7a-7e) were characterised using FT-IR, NMR(1H, 13C) and elemental analysis. The anti bacterial activities of the synthesised compounds were evaluated against gram positive bacteria: Staph and Streptococcus, gram negative bacteria: E-coli, Klebsiella, Proteus, and pseudomonas using 200 µl of 10 mg/ml and minimum inhibitory concentration (MIC) were also determined. The compounds exhibited effective anti bacterial properties though some are not more active than the standard drug ciprofloxacin.
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