Antibacterial Evaluation of Some Schiff Bases Derived from 2-Acetylpyridine and Their Metal Complexes

A series of Schiff bases derived from 2-acetylpyridne and their metal complexes were characterized by elemental analysis, NMR, FT-IR and UV-Vis spectral studies. The complexes were screened for anti-bacterial activity against Methicillin-resistant Staphylococcus aureus (MRSA), Acinetobacter baumanni (AC), Klebsiella pneumonie (KB) and Pseudomonas aeruginosa (PA) using the disc diffusion and micro broth dilution assays. Based on the overall results, the complexes showed the highest activities against MRSA while a weak antibacterial activity was observed against A. baumanii and P. aeruginosa

Two new polymorphs of 2,6-diaminopyrimidin-4(3H)-One Monohydrate

The title compound, C4H6N4O center dot H2O, crystallized simultaneously as a triclinic and a monoclinic polymorph from an aqueous solution of 2,4-diaminopyrimidin-6-ol. Previously, an orthorhombic polymorph was isolated under the same experimental conditions. The molecular geometric parameters in the two present polymorphs and the previously reported orthorhombic polymorph are similar, but the structures differ in the details of their crystal packing. In the triclinic system, the diaminopyrimidinone molecules are connected to one another via N-H...O and N-H...N hydrogen bonding to form infinite chains in the [011] direction. The chains are further hydrogen bonded to the water molecules, resulting in a three-dimensional network. In the monoclinic system, the diaminopyrimidinone molecules are hydrogen bonded together into two-dimensional networks parallel to the bc plane. The water molecules link the planes to form a three-dimensional polymeric structure

Synthesis of 2 '-(5-Chloro-2-Hydroxybenzylidene) benzenesulfanohydrazide schiff base and its anti-ulcer activity in ethanol-induced gastric mucosal lesions in rats

Purpose: To study the anti-ulcer activity of 2'-(5-Chloro-2-hydroxybenzylidene) benzenesulfanohydrazide Schiff base against ethanol-induced gastric mucosal lesions in rats. Methods: 2'-(5-Chloro-2-hydroxybenzylidene) benzenesulfano-hydrazide (Cl-BzSO-HAP) was synthesized, and structurally characterized by elemental analysis, FT-IR, H-1-NMR and C-13-NMR. Its preventive activity against ulcer induced by absolute ethanol in Sprague-Dawley rats were studied in vivo. Twenty four Sprague Dawley (SD) rats (12 males and 12 females) were assigned equally into 4 groups (n = 6), including negative control and positive control groups. The third group received a low oral dose of the compound (50 mg/kg) while the fourth group was administered a high oral dose (100 mg/kg). The degree of gastric lesion formation was assessed. Prior to dosing, the animals were fasted overnight. Results: Cl-BzSO-HAP showed significant preventive activity against ulcer induced by absolute ethanol. Oral administration of the compound (both low and high doses) prior to ethanol administration inhibited gastric lesion formation by 88.0 and 94.9%, respectively, compared to 82.7% for the positive control, cimetidine. Conclusion: Extensive gastric necrosis in rats induced by absolute ethanol was prevented by administration of Cl-BzSO-HAP resulting in reduced or total absence of lesions

Assessment of wound healing potential of copper (II) Bis [N'-((5-chloro-1H-indol-3-YL) methylene) nicotinohydrazide] on experimentally-induced excision wounds in rats

Copper (II) Schiff base derivatives are frequently used for the treatment of many disorders. The aim of current study was to investigate the effects of the Schiff base derivatives on rats of wound healing enclosure and histology of granulation tissues in rats. Wound healing activity of Copper (II) Bis [N'-((5-chloro-1H-indol-3-YL) methylene) nicotinohydrazide] which is shortly called CI-indole-nicotinic, was perused by specifing the percentage of wound closure after tropical application of the compound. Four groups of animals were treated respectively with 0.2mL of gum acacia, 0.2mL of Intrasite gel, 0.2mL of CI-indole-nicotinic (50 mg/mL) and 0.2mL of CI-indole-nicotinic (100 mg/mL) for 10 days to assess the gross rate of wound enclosure, histology and endogenous enzymes parameters. The results indicated the affective capacity of CI-indole-nicotinic inj tissue regenetration and healing the injured skin. Grossing on day 5 and day 10 declared that the compound significantly accelerated the rate of wound healing. Histology of granulation tissues indicated remarkably the angiogenesis augmentation and increased fibroblasts and collagen formation as well as reduction in flammatory cells balance in CI-indole-nicotinic-treated groups compared to control group. Moreover, the compund represented dose-dependent levels of superoxide dismutase (SOD) and slight lipid peroxidation enzyme - malondialdedhyde (MDA) inhibition in granulation tissue. The acute toxity examination displayed no nephorotoxic or hepatotoxic side effects. In conclusion, wound healing capability of CI-indole-nicotinic compund could possibly attribute to enhance collagen deposition in granulation tissue and antioxidant activity of the compound

A schiff base-derived copper (II) complex is a potent inducer of apoptosis in colon cancer cells by activating the intrinsic pathway

Metal-based drugs with extensive clinical applications hold great promise for the development of cancer chemotherapeutic agents. In the last few decades, Schiff bases and their complexes have become well known for their extensive biological potential. In the present study, we examined the antiproliferative effect of a copper (II) complex on HT-29 colon cancer cells. The Cu(BrHAP)2 Schiff base compound demonstrated a potent tiproliferative effect in HT-29 cells, with an IC50 value of 2.8

Chemopreventive evaluation of a Schiff base derived copper (II) complex against Azoxymethane-induced colorectal cancer in rats

Background: Based on the potential of Schiff base compounds to act as sources for the development of cancer chemotherapeutic agents, this in vivo study was performed to investigate the inhibitory properties of the synthetic Schiff base compound Cu(BrHAP)2 on colonic aberrant crypt foci (ACF). Methodology: This study involved five groups of male rats. The negative control group was injected with normal saline once a week for 2 weeks and fed 10% Tween 20 for 10 weeks, the cancer control group was subcutaneously injected with 15 mg/kg azoxymethane once per week for two consecutive weeks, the positive control group was injected with 15 mg/kg azoxymethane once per week for two consecutive weeks and 35 mg/kg 5-fluorouracil (injected intra-peritoneally) for 4 weeks, and the experimental groups were first injected with 15 mg/kg azoxymethane once per week for two consecutive weeks and then fed 2.5 or 5 mg/kg of the Schiff base compound once a day for 10 weeks. Application of the Schiff base compound suppressed total colonic ACF formation by up to 72% to 74% (P,0.05) when compared with the cancer control group. Analysis of colorectal specimens revealed that treatments with the Schiff base compound decreased the mean crypt scores in azoxymethane-treated rats. Significant elevations of superoxide dismutase, glutathione peroxidase and catalase activities and a reduction in the level of malondialdehyde were also observed. Histologically, all treatment groups exhibited significant decreases in dysplasia compared to the cancer control group (P,0.05). Immunohistochemical staining demonstrated down-regulation of the PCNA protein. Comparative western blot analysis revealed that COX-2 and Bcl2 were up-regulated and Bax was down-regulated compared with the AOM control group. Conclusion: The current study demonstrated that the Cu(BrHAP)2 compound has promising chemoprotective activities that are evidenced by significant decreases in the numbers of ACFs in azoxymethane-induced colon cancer