SYNTHESIS AND ANTIMICROBIAL EVALUATION OF SOME NEW BENZTHIAZOLE OXIME ETHER DERIVATIVES

Some new oxime ether derivatives containing benzthiazole heterocyclic nuclei are synthesized. The reaction of 2-mercapto benzthiazole with α-halo ketones followed by reaction with hydroxylamine gave oxime derivatives which on reaction with alkyl halides viz. ethyl chloride, n-propyl chloride, and n-butyl chloride in absolute ethanol afforded the target compounds 4a-l. The structure of all the synthesized compounds was confirmed by spectroscopic methods like mass and NMR. All compounds after structural confirmation were tested for biological activities.

Design, Synthesis of a Novel Banana-Shaped Compounds via Esterification

Schiff's Bases were synthesized from the reaction of p-amino benzoic acid and alkoxybenzaldehyde in absolute ethanol and reacted with (E)-3-((4-hydroxybenzylidene) amino) phenol used DCC (N,N'-Dicyclocarbodiimide) and DAMP (4-(Dimethylamino) pyridine ) to 3-(((E)-4-((4-(((E)-4 alkoxy benzylidene) amino) benzoyl) oxy) benzylidene) amino) phenyl4- (E)- 4-alkoxy benzyli dene ) amino) benzoate. The structures of the products were confirmed by their melting points, FT-IR, 1HNMR spectra.

Experimental Research on Intratumoral Injection of Sal Ammoniac Extract in the Treatment of Mouse Liver Cancer

Objective: To study the effect of sal ammoniac extract on the treatment of liver cancer and analyze its possibility of replacing absolute ethanol. Methods: Sixty Kunming mice (5-6 weeks old, 18-22g in weight, male and female in half) were selected and inoculated with 0.1 ml of 1:4 ascitic diluent from mouse liver cancer H22 under the axilla of the right limb. After tumor formation, they were randomly divided into 3 groups with 20 mice in each group. Normal saline (NS), sal ammoniac extract (N), and absolute ethanol (E) were injected into the tumor once a day for four times. The death, tumor weight, tumor inhibition rate, lactate dehydrogenase (LDH), and succinate dehydrogenase (SDH) expression of the mice in each group were analyzed. Results: In the course of treatment, 3 mice died in the normal saline group, 2 mice died in the sal ammoniac treatment group, and 7 mice died in the absolute ethanol group. The tumor weight of the normal saline group, sal ammoniac treatment group, and absolute ethanol group were 1.88 ± 0.26, 1.41 ± 0.49, and 1.51 ± 0.46, respectively. The tumor inhibition rates were 0%, 31.0%, and 21.6%, respectively. Comparing the sal ammoniac treatment group and the normal saline group, t = 3.5133, p = 0.0013; comparing the absolute ethanol group and the normal saline group, t = 2.7926, p = 0.0093. The expression of LDH was 81 ± 10, 51 ± 11, and 32 ± 9 in the normal saline group, sal ammoniac treatment group, and absolute ethanol group, respectively, while the expression of SDH was 80 ± 10, 51 ± 10, and 51 ± 12 in the normal saline group, sal ammoniac treatment group, and absolute ethanol group, respectively. Comparing the LDH of the sal ammoniac treatment group with that of the saline group, t = 8.4264, p = 0.0000; comparing the absolute ethanol group and normal saline group, t = 13.8763, p = 0.0000. Comparing the SDH of the sal ammoniac treatment group with that of the normal saline group, t = 8.1455, p = 0.0000; comparing the absolute ethanol group with the normal saline group, t = 7.2197, p = 0.0000. Conclusion: The traditional Chinese antitumor medicine, sal ammoniac and its main effective components have good antitumor effect, which can be further popularized and applied in clinical practice.

Synthesis, Characterization and in vitro Antibacterial Activity of Novel 1,2,4-Triazine and 1,2-Diazepine Derivatives

In this work we describe a simple method to synthesis novel 3-[(pyridine-2-ylamino)methyl]-1,6-dihydro-1,2,4-triazine-5(2H)-one (3) and 1-(N-pyridine-2-ylglycyl)-1,2-diazepine-3,7-dione (4). Firstly, adding ethyl chloroacetate to a solution of KOH and 2-amionpyrdine and refluxed in absolute ethanol for 5 hours afforded the target ethyl-N-pyridin-2-ylglycinate (1), then refluxing of compound (1) with hydrazine hydrate in absolute ethanol for 6 hours yield 2-(pyridine-2-ylamino)acetohydrazide (2). Chloroacetamid and glutaric acid were refluxed with compound (2) in absolute ethanol for 20 and 21 hours to afford the compounds 3-[(pyridine-2-ylamino)methyl]-1,6-dihydro-1,2,4-triazine-5(2H)-one (3) and 1-(N-pyridine-2-ylglycyl)-1,2-diazepine-3,7-dione (4), respectively. Structures of the synthesized compounds were supported by means of FTIR, CHN elemental analysis, and NMR (1H, 13C) spectroscopic analysis. The synthesized compounds were evaluated for their in vitro antibacterial activity against Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, Staphylococcus aureus, Bacillus cereus, and Enterococcus faecalis. The inhibition zones were measured, expressed in mm, and the minimum inhibitory concentration (MIC) is reported in μg/mL. The results show that compounds (3) and (4) have a significant antimicrobial activity with the highest MIC value against all tested bacteria.

Synthesis Characterization and Studying Antibacterial Activity of some New Pyrazol Derivatives

This research involved the conversion of sulfadiazine into compound 2-chloro-N-(4-(N-(pyrimidin-2-yl) sulfamoyl) phenyl) acetamide [A] through the reaction of sulfadiazine with chloroacetyl chloride in the presence of diethylamine in dimethylformamide as solvent. Then prepared the hydrazine derivative of sulfadiazine 2-hydrazinyl-N-(4-(N-(pyrimidin-2-yl) sulfamoyl) phenyl) acetamide [B] through the interaction of compound [A] with hydrazine in dimethylformamide as solvent. Followed by chalcones preparation [C1, C2, C3, C4, and C5] from the reaction of 4-aminoacetophenone with some aromatic aldehydes in a basic medium in absolute ethanol using an ice bath. Pyrazoline derivatives [BC1, BC2, BC3, BC4, and BC5] were prepared from the reaction of the hydrazine derivative of sulfadiazine [B] with chalcones in a basic medium in the presence of absolute ethanol. The pyrazole derivatives [IBC1, IBC2, IBC3, IBC4, and IBC5] were prepared from the reaction of the hydrazine derivative of sulfadiazine [B] with chalcones in the presence of glacial acetic acid and then the product was oxidized using Iodine. Synthesized compounds have been studied by their melting points, and characterized by C.H.N.S analysis, FT-IR and 1H-MNR spectroscopy and studied of biological activity.

Comparative Evaluation of the Sterilization Effect of Six Kinds of Commercial Disinfectants against Four Pathogenic Bacteria

In this work, we systematically investigate the sterilization effect of six kinds of commonly used commercial disinfectants, including the DuPont Virkon disinfectant, peracetic acid disinfectant, sodium hypochlorite, bromogeramine disinfectant, water-soluble allicin, and absolute ethanol, against the Escherichia coli, Staphylococcus aureus, Monilia albican and Clostridium sporogenes. The inhibition zone was used to qualitatively determine the antibacterial effects of the six disinfectants, and then the minimum two-fold dilution method was used to quantitatively determine the minimum inhibitory concentration and minimum bactericidal concentration of the six disinfectants on the four pathogens. The result illustrated that the antibacterial effect of peracetic acid disinfectant is the best, and clostridium sporogenes is the most sensitive to it, followed by bromogermine disinfectant, which can inhibit the four pathogenic bacteria at the concentration recommended by the manufacturer. The antibacterial effect of DuPont Virkon disinfectant, sodium hypochlorite, water-soluble allicin and absolute ethanol is not as good as expected, and cannot inhibit the four kinds of pathogenic bacteria at the recommended concentration. In summary, the antibacterial effect of peracetic acid disinfectant is the strongest, followed by the bromogermine disinfectant, DuPont Virkon disinfectant, sodium hypochlorite and water-soluble allicin. The absolute ethanol exhibits the worst antibacterial properties.

A Modification of Cell-Lysis for High-Quality Intact RNA of Bacillus Subtilis Extracted From the Culture Under Different Physiological Stages

High quality RNA products from bacterial cells are required for the molecular study. Sample preparation to acquire the high-quality RNA especially the Gram-positive bacteria like Bacillus sp., the model organism, remains a critical burden toward the integration of full molecular downstream analyses although several methods have been proposed including conventional or kit-based protocols. Those techniques were simply developed using the cell samples at certain growth stages unless some molecular studies require RNA samples gathered under different physiological stages of growth and process conditions. Herein, we developed the simple yet effective cell-lysis technique prior to RNA extraction by modifying the commercial kit-based protocols. Bacillus subtilis TL7-3 was used as the model organism in this study. Lysozyme loading (20 mg/mL) as well as the incubation time (30 min) and temperature (37 °C) was responsible for cell lysis and increased RNA concentration in the samples. Invert mixing rather than centrifugation and vortexing prevented RNA damage during protein precipitation by absolute ethanol. This was confirmed by the RNA Integrity Number (RIN) values greater than 8.0 of all RNA extracted from both vegetative cells and endospores of B. subtilis TL7-3. Additionally, absolute ethanol is preferable to our less-than-1-h protocol for protein precipitation as indicated from the higher ratios of A260/A280 and those of A260/A230 of the RNA products than 2.0 and 2.1, respectively. From the findings mentioned above, we successfully developed the modified RNA extraction protocol applicable for the intact cells of Gram-positive bacteria like Bacillus sp. at varied physiological and morphological stages.

Production of Disinfectants (Hand Sanitizers)

Hand sanitizer is a supplement or alternative to hand washing with soap and water. The production of hand sanitizers from locally grown medicinal plants namely; wild spinach, turmeric, garlic) and camphor was achieved by obtaining the plants, grinding and performing ethanolic extraction for 72hrs on them. This ethanolic extract in combination with glycerin and absolute ethanol were used for the final preparation. Turmeric and garlic failed the hand sanitizer ‘s approval test based on their colour and pungent smell, but wild spinach and camphor were found to be good candidates for hand sanitizers production here in Nigeria and inclusion of such products here could increase hand hygiene compliance levels.