Synthesis, Chemical Characterization and Antibacterial Activity of Some Novel Triazole Substituted 5-Oxo-Imidazoline Derivatives

5-oxo-imidazoline rings have been reported to possess various biological activities such as antibacterial, anticancer, antifungal, and anthelmintic activities. These activities also include anticonvulsant, and anthelmintic.   These observations and findings prompted to synthesize the novel triazolo substituted 5-oxo-imidazoline derivatives.  In the present investigation, a series of 10 new 1-trazolyl-5-oxo-imidazolinones were synthesized in good yield by using appropriate synthetic methods and have been established on the basis of their M.P., TLC, FT-IR, 1H-NMR, 13C-NMR data.  Also, all the compounds were evaluated for the possible antibacterial activity by cup-plate agar diffusion method by measuring % zone of inhibition.  Streptomycin at the concentration of 50?g/ml was used as standard drug.  Of all the tested compounds, A6 exhibited significantly high potency against the various gram positive and gram negative organisms used in the investigation

In Vitro Lipid Peroxidation and Antimicrobial Activity of Mucuna pruriens Seeds

The present investigation is aimed to carry out the in vitro lipid peroxidation and antimicrobial activities of the methanol extract of Mucuna pruriens (MEMP) (Family: Fabaceae) seeds. Lipid peroxidation was monitored by the change in optical density of the prepared concentrations (10-320 μg/ml) and the % inhibition was calculated. Ascorbate/FeSO4-induced peroxidation was inhibited by standard antioxidants such as quercetin, L-ascorbic acid and MEMP. Moreover, the % inhibition of the methanol extract increased with increase in concentration. IC50 value for the MEMP, L-ascorbic acid and quercetin for lipid peroxidation was found to be 217.25 μg/ml, 41 μg/ml and 19.75 μg/ml respectively. The antimicrobial activity of MEMP was determined by disc diffusion method with various Gram positive and Gram-negative microorganisms. MEMP showed broad-spectrum antimicrobial activity against all the tested microorganisms except Staphylococcus aureus ML 152 and Vibrae cholera 14035. The results obtained in the present study indicate that MEMP can be a potential source of natural antioxidant and antimicrobial agent

Antitumor Activity and in vivo Antioxidant Status of Mucuna pruriens (Fabaceae) Seeds against Ehrlich Ascites Carcinoma in Swiss Albino Mice

The aim of the present study is to evaluate the antitumor effect and antioxidant role of Mucuna pruriens (Family: Fabaceae) against EAC bearing Swiss albino mice. The effect of methanol extract of Mucuna pruriens (MEMP) on tumor growth and host's survival time was studied by the following parameters: tumor volume, packed cell volume, viable and non-viable cell count and life span of the host. MEMP was administered at a 125 and 250mg/kg b.w. once a day for 14 days, after 24 h of tumor inoculation. Decrease in tumor volume, packed cell volume, and viable cell count were observed in MEMP treated animals when compared to EAC treated animals. Treatment with MEMP at a dose of 125 and 250mg/kg increased the mean survival time to 29.5 ± 0.55 and 34 ± 0.2 days respectively. The extract also decreased the body weight of the EAC tumor bearing mice. Hematological studies reveal that the Hb content was decreased in EAC treated mouse, whereas restoration to near normal levels was observed in extract treated animals. There was a significant decrease in RBC count and increase in WBC counts in extract treated animals when compared to EAC treated animals. The study was also extended to estimate the liver biochemical parameters such as LPO, GSH, and antioxidant enzymes like SOD, CAT etc. Treatment with MEMP decreased the levels of lipid peroxidation and increased the levels of glutathione (GSH), superoxide dismutase (SOD) and catalase (CAT). The results suggest that the methanol extract of Mucuna pruriens seeds exhibits significant antitumor and antioxidant effects in EAC bearing mice

Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds

From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer mononuclear ruthenium (II) compounds for antinociceptive and antitumor activities.status: publishe

Antinociceptive and antitumor activity of novel synthetic mononuclear Ruthenium (II) compounds

Background: From the thousands of years, metal compounds have been used in medicine for treatment of various diseases including various types of cancers. Ruthenium was seen as a promising metal due to its similar kinetics to platinum and its lower toxicity. Therefore, we aimed to evaluate the newer mononuclear ruthenium (II) compounds for antinociceptive and antitumor activities. Materials and Methods: Ruthenium (II) compounds were evaluated for antinociceptive and antitumor activity using the various in vitro and in vivo models. The compounds were injected to mice at concentrations of 1 and 2 mg kg -1 intraperitoneally and were screened for antinociceptive activity, and the antiproliferative effect was evaluated against murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) using MTT assay. Results: The results for antitumor activity clearly indicated that compound R 1 was potent cytotoxic agent than R 2 with IC 50 values ranging from 4-6 μM for R 1 , whereas IC 50 values for compound R 2 ranging from 65-103 μM. The compounds have shown a significant anti-inflammatory effect in carrageenan and dextran models but do not having the central analgesic activity, this indicating that the antinociceptive activity is related to the peripheral nervous system. The results for 5-Lipoxygenase (5-LOX) activity showed that both R 1 and R 2 compounds were found to be significant 5-LOX inhibitory activity with IC 50 values of 14.35 μg ml-1 and 29.24 μg ml-1 respectively. Conclusion: These findings concluded that the new ruthenium compounds might be the promising antiproliferative agents as these compounds showing significant 5-LOX inhibitory activity and potential agents in the management of pain related disorders

Microwave assisted synthesis, characterization of some new isatin and thiophene derivatives as cytotoxic and chemopreventive agents

In obtaining some new cytotoxic and chemopreventive agents with potent antiproliferative activity against cancer cells, a series of new β-isatin aldehyde-N,N′-thiocarbohydrazone, bis-β-isatin thiocarbohydrazones, bis-β-isatin carbohydrazones, N,2-bis(thiophen-2-ylmethylidene) thiocarbohydrazone and N,2-bis(thiophen-2-ylmethylidene) carbohydrazone derivatives was synthesized by microwave oriented reaction and evaluated for their in vitro cytotoxic activity. The newly synthesized compounds were characterized based on spectral (FT-IR, NMR, MS) analyses. The inhibitory effects of synthesized compounds on the proliferation of murine leukemia cells (L1210), human T-lymphocyte cells (CEM) and human cervix carcinoma cells (HeLa) were assayed by using MTT assay. The compounds were also tested for their inhibitory effects on Epstein-Barr virus early antigen (EBV-EA) activation induced by 12-Otetradecanoylphorbol-13-acetate (TPA). In vitro evaluation of these schiff bases revealed mild to moderate cytotoxic activity in a dose dependent manner. The results of the in vitro inhibitory activities of synthetic compounds against EBVEA activation with IC50 ranges from 485-535 (mol ratio/32pmol/TPA). Chlorine group containing derivatives did not show increased inhibitory activity against tumor promoter TPA induction. Sulphur containing derivatives also did not show a high inhibitory potency in this system. © 2012 Bentham Science Publishers.status: publishe

Synthesis, spectroscopic characterization, antineoplastic, in vitro-cytotoxic, and antibacterial activities of mononuclear ruthenium(II) complexes

The synthesis, antineoplastic, cytotoxic, and antibacterial activities of Ru(II) complexes derived from quinazoline and thiosemicarbazone ligands are reported. These complexes have been prepared and characterized by UV-Vis, IR, H-1-NMR, FAB-mass spectroscopy, and elemental analysis. The ligands and resulting complexes were subjected to in vivo antineoplastic activity against a transplantable murine tumor cell line Ehrlich ascites carcinoma (EAC) and in vitro cytotoxic activity against human cancer cell line Molt 4/C-8, CEM, and murine tumor cell line L 1210. The ruthenium complexes show promising biological activity especially in decreasing tumor volume and viable ascitic cell counts. These complexes prolonged the life span of mice bearing EAC tumors by 10-52%. In vitro evaluation of these ruthenium complexes revealed cytotoxic activity from 0.29 to 2.9 mu mol L-1 against Molt 4/C-8, 0.22 to 2.1 mu mol L-1 against CEM and 0.42 to 4.7 mu mol L-1 against L1210 cell proliferation, depending on the nature of the compound. The metal complexes are more active than the parent ligand and exhibit mild to moderate antibacterial activity.status: publishe

Synthesis, spectroscopic characterization, in vitro cytotoxic and structure activity relationships of some mononuclear Ru(II) complexes

New mononuclear Ru(II) complexes [Ru(A) 2 (B)} 2 +, where A= 2,2'-bipyridine/1,10-phenanthroline and B= 3,4,5-tri-OCH3-DPC, 4-CH3-DPC, 4-N(CH3) 2 -DPC, 4-NO 2 -DPC, N-BITSZ, PTSZ and PINH, were prepared and characterized by spectroscopic methods. The in vitro cytotoxic activities of the complexes and their corresponding ligands were investigated against the human cancer Tly MPh ocyte cell lines molt 4/c8 and CEM and the murine tumor leukemia cell line L 1 210, human promyelocytic leukemia cells (HL-60) and Bel-7402 liver cancer cells by MTT assay. The complexes [Ru(A) 2 (B)} 2 + (A= 1,10-phenanthroline, B= 3,4,5-tri-OCH3-DPC) exerts rather more potent activities against all of these cell lines, especially for CEM and L 1 210. Ru complexes and structure-activity relationships and anticancer mechanisms are also discussed. © 2013 Taylor and Francis.status: publishe