Design,synthesis, antinociceptive,and anti-inflammatory properties of thiazolopyrimidine derivatives

Ten 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one derivatives were synthesized and evaluated. A series of heterocyclic, 2-(substituted benzylidene)-7-(4-chlorophenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one were synthesized by reaction of 7-(4-chloro phenyl)-5-(furan-2-yl)-2H-thiazolo[3,2-a]pyrimidin-3(7H)-one with appropriately substituted aldehydes in the presence of anhydrous sodium acetate and glacial acetic acid. The antinociceptive activity was evaluated by tail-flick technique, anti-inflammatory activity was evaluated by carrageenan-induced paw edema test and their ulcerogenicity index was determined. The para-substituted methyl, hydroxy, fluoro, chloro, bromo, and nitro derivatives showed significant antinociceptive and anti-inflammatory activities. The detailed synthesis, spectroscopic data, and pharmacological screening of the synthesized compounds were reported.     

Hepatoprotective activity of 1-(4-(Dimethylamino)Benzylidene)-5-(2-Oxoindolin-3-ylidene) Thiocarbohydrazone in rats

The aim of the present study was to evaluate the hepatoprotective activity of 1-(4-(dimethylamino)benzylidene)-5-(2-oxoindolin-3-ylidene) thiocarbohydrazone, a novel isatin derivative against carbon tetrachloride (CCl₄)-induced hepatotoxicity in rats. Hepatic damage was induced by administration of CCl₄ (1 ml/kg, b.w., p.o.) in combination with liquid paraffin (1:1) as a single dose. The hepatotoxic rats were treated with test compound at doses of 50 or 100 mg/kg for three days and liver damage biomarkers, including activities of serum glutamate pyruvate transaminase (SGPT), serum glutamate oxaloacetate transaminase (SGOT), serum alkaline phosphatase (ALP), and levels of total serum bilirubin (TB) measured in blood samples. Results demonstrated that treatment with test compound at doses of 50 or 100 mg/kg to hepatotoxic rats produced a significant dose-dependent reduction of elevated SGOT, SGPT, ALP activities and TB levels indicating a hepatoprotective effect that was confirmed by histopathological examination of liver tissues. The study results confirmed the hepatoprotective activity of 1-(4-(dimethylamino)benzylidene)-5-(2-oxoindolin-3-ylidene) thiocarbohydrazone in rats.     

Synthesis and in vitro biological evaluation of 3, 4-annelated coumarin-pyrimido-pyrimidine systems

3,4-Annelated coumarin-pyrimido-pyrimidine systems (7-imino-8-mercapto-7H-5-oxa-7a,9,12-triaza-benzo[a]anthracen-6-one 2 and 8-hydroxy-7-imino-10-methyl-7H-5-oxa-7a,9,12-triaza-benzo[a]anthracen-6-one 3) were synthesized by the action of 4-amino-2-mercapto-pyrimidine, 2-amino-4-hydroxy-6-methylpyrimidine, respectively, on 4-chlorocoumarin-3-carbonitrile 1. The synthesized compounds were examined for in vitro antibacterial activity against 4 bacterial cultures: Staphylococcus aureus, Streptococcus pneumonia, Escherichia coli, and Aeromonas Salmonicida. The antibacterial activity of synthesized compounds 2 and 3 was compared to antibacterial activity of novobiocin as a standard drug.     

Relationships between octan‐1‐ol/water partition coefficients,aqueous activity coefficients and reversed phase HPLC capacity factors of alkylbenzenes,chlorobenzenes, chloronaphthalenes and chlorobiphenyls

Linear relationships between logarithms of octan‐1‐ol/water partition coefficients (K_d,oct), aqueous activity coefficients (y_aq) and extrapolated RP HPLC capacity factors (k‘_w) are found for four types of aromatic hydrocarbons (alkylbenzenes and poly‐chlorinated benzenes, ‐naphthalenes and ‐biphenyls).

Both log K,_d,oct and logk‘_w increase with the increasing number of chlorine or methyl‐ene substituents. These increases of log K,_d,oct and log k‘_w are proportional and almost independent of the parent compound. In addition, these increases are linear to increases of logy_aq. The slopes of logk‘_w‐logy_aq and log K,_d,oct‐logv_aq relationships deviate significantly from 1.0. This suggests that the activity coefficients of the test compounds in both octan‐1‐ol and in the stationary phase of the RP column increase after substitution of aromatic compounds with methylene or chlorine.     

Synthesis,structural elucidation,electro-chemical behaviour and fungitoxic activity of transition metal(II) mixed-ligand complexes with some Schiff bases

The Schiff bases, potassium salt of salicylidene-β-alanine [KHL], bis(benzylidene)ethylenediamine [SB¹] and thiophene-o-carboxaldene-p-toluidine [SB²], and mixed-ligand complexes with Mn(II), Co(II), Ni(II), Cu(II), Zn(II), and Cd(II) have been prepared. They were characterized by elemental analyses, magnetic susceptibility measurements, thermogravimetric analyses (t.g.a.), infrared spectra and electronic spectra. The mixed-ligand complexes were found to have the general composition [M(L)(SB)(H₂O)]. All the mixed-ligand complexes were found to have six-coordinated octahedral geometry. The fungitoxic activity of the ligands, metal salts, control (DMSO), bavistin, emcarb, and mixed-ligand complexes were screened against Aspergillus niger, Fusarium oxysporum and Aspergillus flavus. All the mixed-ligand complexes show higher fungitoxic activity as compared to the Schiff bases, metal nitrate and control (dimethyl sulphoxide, DMSO), and moderate fungitoxic activity as compared to the fungicides (bavistin and emcarb).     

Antibacterial and antimutagenic activitiy of extracts and essential oil from (Tunisian) Pistacia lentiscus

Aqueous and flavonoid-enriched extract as well as essential oil (EO) obtained from leaves of Pistacia lentiscus were assessed for antibacterial and antimutagenic activities. Antibacterial activity of different extracts and EO were evaluated against six bacterial strains. A marked inhibitory effect was observed against Salmonella typhimurium, whereas lower activity was observed against Staphylococcus aureus, Pseudomonas aeruginosa, and Salmonella enteritidis. EO showed significant inhibitory effects against Salmonella typhimurium, Salmonella enteritidis and Staphylococcus aureus. The antimutagenic activity of the different extracts against Aflatoxin B₁ (AFB₁) and sodium azide was demonstrated with the Salmonella typhymurium assay. The number of revertants per plate decreased significantly when the plant extracts were added to the assay system using Salmonella typhimurium TA100, TA98 and TA1535.     

Nerve conduction studies in sprayers occupationally exposed to mixture of pesticides in a mango plantation at Lucknow,North India

In this study, nerve conduction, organochlorine (OC) pesticide residues in blood and cholinesterase activity levels of pesticide sprayers employed in mango plantations at Lucknow, North India, were determined. Fifty-two sprayers from mango plantations who regularly spray mixture of pesticides like organophosphates (OP), OCs, and carbamates were considered as exposed group. Eighteen subjects with similar socio-economic status of exposed group, who do not handle pesticides, were selected as controls. Questionnaire-based interviews related to personal and occupational histories of the study subjects were carried out. Sprayers did not use any personal protective equipment during pesticide handling. The blood-pesticide analyses of sprayers show higher mean values of hexachlorohexane (HCH), γ-HCH, δ-HCH, total HCH, op-DDT compared with the controls. Acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) activites were significantly reduced among sprayers. Risk of motor nerve conduction deficits was observed in sprayers with low AChE activity. Negative correlation of motor and sensory nerve conduction deficits was observed with the duration of exposure and age among sprayers. The study demonstrated that the prolonged exposure to mixture of pesticides, ergonomic factors, decline in cholinesterase activity may lead to nerve conduction dysfunction. The findings suggest the need for controlled use of pesticides in the plantation and indicated the need for training and implementation of hygiene practices like proper usage of personal protective equipments.     

Antifungal activity of volatile metabolites emitted by mycelial cultures of saprophytic fungi

The antifungal activity of molecular identified Chilean saprobiontic fungi, Trichoderma viride, Schizophyllum commune and Trametes versicolor, on the fungal plant pathogens Botrytis cinerea and Fusarium oxysporum, and the saprotrophic mould Mucor miehei was investigated using two types of inhibition bioassay: (1) bi-compartmented Petri dishes and (2) two Erlenmeyer flasks connected by their upper parts. The chemical composition of volatile organic compounds (VOCs) released by saprobiontic fungi was also investigated using headspace solid-phase microextraction (SPME) and gas chromatography/mass spectrometry (GC-MS) analysis. Of the saprobiontic fungi evaluated, one isolate of S. commune showed the highest inhibitory activity against B. cinerea and M. miehei, 86.0±5.4 and 99.5±0.5% respectively. The volatile profiles of fungal isolates were shown to contain a different class of compounds. The major components in the headspace of mycelial cultures were 6-pentyl-α -pyrone (T. viride), ethanol and β -bisabolol (S. commune), and a sesquiterpene alcohol (Tr. versicolor). This is the first study reported on the release of VOCs by Chilean native fungi and their antifungal activity wrt. plant pathogenic fungi.     

Radioactive Isotopes of Strontium,Caesium and Plutonium in Sediments of the Northern Adriatic Sea

Changes in nitrification rates of an acid grassland soil with and without air drying have been monitored over 9 days, after first flushing native nitrate from the soils with deionised water. The results confirmed that full re-establishment of nitrification after air drying takes several days, supporting the hypothesis that any immediate first flush of nitrate from air-dried soils originates from cell lysis or flushing of ‘stored’ nitrate. Ammonium spiking confirmed that nitrification was not ammonium substrate limited. It was also found that ammonium accumulates in the soil during the drying process, providing a substrate pool once the population of nitrifiers has re-established. Over the first week of incubation, nitrate immobilisation was less conspicuous in the soil that had been rewetted after air drying compared with the incubated field moist soil.     

二氯苯醌对斑马鱼胚胎发育及超氧化物歧化酶的影响

2,6-二氯-1,4-苯醌（2,6-dichloro-1,4-benzoquinone,2,6-DCBQ）作为一种新型消毒副产物,因其高检出率及高含量的特点而备受人们关注.本研究以斑马鱼胚胎为实验材料探究了2,6-DCBQ的发育毒性.结果发现：斑马鱼胚胎在8~24 hpf（器官发育形成时期）对2,6-DCBQ暴露最为敏感,死亡率最高;2,6-DCBQ安全浓度为27.15 μg·L^-1,属于极度危险外源化学物.在本实验中,2,6-DCBQ对斑马鱼的生长没有显著影响,但高浓度（100和150 μg·L^-1）2,6-DCBQ会显著增加斑马鱼胚胎及仔鱼的畸形率.在实验过程中还发现,高浓度（≥ 80 μg·L^-1）2,6-DCBQ会明显抑制斑马鱼胚胎的心率.此外,≥ 30 μg·L^-1 2,6-DCBQ可提高超氧化物歧化酶（Superoxide dismutase,SOD）的活性,并影响Cu/ZnSOD和MnSOD的正常转录.本研究较全面地探究了2,6-DCBQ对斑马鱼早期发育阶段的发育毒性,可为2,6-DCBQ的毒性研究提供可靠证据.