Synthesis and evaluation of arylamidine derivatives for new antimicrobial and cytotoxic activities

ABSTRACT A series of arylamidines 3a-j was designed, synthesized and investigated for antimicrobial activity. Structures of the compounds were confirmed by IR, 1H-NMR and 13C-NMR and a 2D spectroscopic study was performed. A preliminary screening of the antimicrobial tests clearly showed that three out of ten arylamidines, viz, 3f, 3g and 3i, were effective against all the gram-negative bacteria: Klebsiella pneumoniae, Pseudomonas aeruginosa and Salmonella enteric; and against the yeast, candida albicans. Further, the Minimum Inhibitory Concentrations (MIC) against the bacteria and yeast were determined. All compounds 3a-d, 3f, 3g, 3i and 3j were also investigated for their low cytotoxic effects on tested cell lines. Compounds 3d and 3f were the most effective derivatives against HL-60 and HEp-2 cells, respectively, with IC50 value (2µg/mL), and low normal cells toxicity.

Molecular detection and antimicrobial resistance of Pseudomonas aeruginosa from houseflies (Musca domestica) in Iran

BackgroundPseudomonas aeruginosa is a common bacterium that can cause disease in humans and other animals. This study was conducted to screen for molecular detection and antimicrobial-resistant P. aeruginosa in Musca domestica in different locations in the Iranian provinces of Shahrekord and Isfahan.MethodsMusca domestica were captured by both manual and sticky trap methods, during the daytime, from household kitchens, cattle farms, animal hospitals, human hospitals, slaughterhouses and chicken farms at random locations in Shahrekord and Isfahan provinces of Iran, and subsequently transported to the laboratory for detection of P. aeruginosa. In the laboratory, flies were identified and killed by refrigeration in a cold chamber at −20 °C, then placed in 5 mL peptone water and left at room temperature for five hours before being processed. Pseudomonas isolates were preliminarily identified to genus level based on colony morphology and gram staining, and their identity was further confirmed by polymerase chain reaction.ResultsOverall blaTEM gene was recovered from 8.8 % (53/600) of the P. aeruginosa isolated from houseflies collected from the two provinces. A slightly higher prevalence (10.7 %; 32/300) was recorded in Shahrekord province than Isfahan province (7.0 %; 21/300). The locations did not differ statistically (p < 0.05) in bacterial prevalence in flies. Seasonal prevalence showed a significantly lower infection frequency during autumn.ConclusionsHouseflies are important in the epidemiology of P. aeruginosa infections.(AU)

Biosynthesis of silver nanoparticles using fresh extracts of Tridax procumbens Linn.

A simple and eco-friendly method for the synthesis of biogenic nanoparticles (NP’s) using an aqueous solution of T. procumbens fresh plant extract (leaf and stem) as a bioreductant is reported. The prepared biogenic nanoparticles were well characterized using U.V. visible spectroscopy, scanning electron microscopy, X-ray diffraction and Fourier-transform infrared spectroscopy. The particles were confirmed to be elemental crystal by X-ray diffraction. The potential applications of biosynthesized nanoparticles as antimicrobial (antibacterial and antifungal) against pathogens Escherichia coli, Vibrio cholerae, Aspergillus niger and Aspergillus flavus were demonstrated.

Characterization of Leiurus abdullahbayrami (Scorpiones: Buthidae) venom: peptide profile, cytotoxicity and antimicrobial activity

Background Scorpion venoms are rich bioactive peptide libraries that offer promising molecules that may lead to the discovery and development of new drugs.Leiurus abdullahbayrami produces one of the most potent venoms among Turkish scorpions that provokes severe symptoms in envenomated victims.Methods In the present study, the peptide profile of the venom was investigated by electrophoretic methods, size-exclusion and reversed-phase chromatography and mass spectroscopy. Cytotoxic and antimicrobial effects were evaluated on a breast cancer cell line (MCF-7) and various bacterial and fungal species.Results Proteins make up approximately half of the dry weight of L. abdullahbayrami crude venom. Microfluidic capillary electrophoresis indicated the presence of 6 to 7 kDa peptides and proved to be a highly practical peptidomics tool with better resolution when compared to conventional polyacrylamide gel electrophoresis. Mass spectroscopy analysis helped us to identify 45 unique peptide masses between 1 to 7 kDa with a bimodal mass distribution peaking between molecular weights of 1 to 2 kDa (29%) and 3 to 4 kDa (31%). L. abdullahbayrami crude venom had a proliferative effect on MCF-7 cells, which may be explained by the high concentration of polyamines as well as potassium and calcium ions in the arachnid venoms. Antimicrobial effect was stronger on gram-negative bacteria.Conclusions This work represents the first peptidomic characterization of L. abdullahbayrami venom. Considering the molecular weight-function relationship of previously identified venom peptides, future bioactivity studies may lead to the discovery of novel potassium and chloride ion channel inhibitors as well as new antimicrobial peptides fromL. abdullahbayrami venom.

Anti-microbial activity of extracts and isolates of leaves of acalypha canescana linn

The in vitro antibacterial activity of the extracts and isolates of Acalypha canescana [leaves] have been studied against bacteria [Bacillus subtilis, Staphlylococcus aureus, Proteus vulgaris, Pseudomonas aeruginosa] and fungi [Candida albicans]. The total acetone extract, total methanol extract, total chloroform extract, total benzene extract and the fractionated two isolates of acetone extract and benzene extract have shown significant activity against the organisms used, almost comparable with the standard drugs Ciprofloxacin and Clotrimazolc. This in vitro testing also resulted in activity guided isolation of four antibacterial and antifungal principles from the leaves

phytopharmacological review on genus Ailanthus

The various species of Ailanthus find extensive use in the indigenous system of medicine for various ailments. The phytochemical and biological evaluation by researchers have authenticated their usage in traditional system of medicine. In the present paper the authors compile here a comprehensive review of their use in the light of present day research

Synthesis of new pyrroles and their biological activities.

Coumarino acid hydrazides and acid hydrazide of 2-oxy 3, 5, 6-trichloropyridine were prepared in two steps. These acid hydrazides on condensation with Acetonyl acetone i.e. 2,5-hexanedione yields new pyrroles. These pyrroles showed good to moderate antimicrobial activities against Alternaria brassicicola, Aspergillus niger, E. coli and Lactobacillus.

Novel benzo-O-pyrone analogues as antimicrobial agents

New cyclic analogues derived from 8-allyl-7-hydroxy-4- methyl-2H-1-benzopyran-2-one have been synthesized. Ten of the new compounds were screened for antibacterial as well as antifungal activity. The results were presented

Synthesis of some new indole derivatives of possible antimicrobial activity

A series of indolyl arylidene hydrazones 2 [c,d], indolylamidothiazolidin-4-ones 3 [a-d], pyrazoline [4], pyrazolidin- dione [5], pyrazolone [6], 3-[3-cyano-4-aryl-2-imino [1H]-pyridin-6-yl]-indoles 8 [a-g] and 3-[3-cyano-4-aryl-2-thioxo [1H]-pyridin-6-yl]-indoles 9 [a-e] were synthesized. Some of the new compounds showed considerable antimicrobial activity against Gram +ve bacteria, yeast and fungi

New 4-substituted phenoxy quinolines of possible antimierobial activity

New series of semicarbazone and substituted thiosemicarbazones [3a-d], 7-chloro-4-[p-[4-aryl-3-cyano-2-oxo[1H] pyridin-6-yl] phenoxy] quinolines [4a-f], 7-chloro-4-[p-[4-aryl-3-cyano-2-imino[1H] pyridin-6-yl] phenoxy]quinolines [5a-e] and 7-chloro-4-[p-[4-aryl-3-cyano-2-thioxo [1H] pyridin-6-yl] phenoxy] quinoline [6a-c], were synthesized for the purpose of antimicrobial evaluation against Gram +ve, Gram -ve bacteria, yeast and fungi

Synthesis and reactions of some new substituted cyclo-hexenone tetrahydropyrimidine derivatives of expected biological activity

4-[P-chlorophenyl]-[4H]-6-[substituted styryl-cyclo-hexenonyl]- 1,2,3,4-tetrahydropyrimidine-2-thione [IV] and 5-[p-chlorophenyl]-[5H] [7-substituted styryl-cyclohexenonely]-1,2,3,4-tetrahydrothiazolo- [3,2a]-pyrimidine-3 one derivatives [V] have been synthesized. The 2- aryl-methylene [VI] and the 2-aryl-hydrazono-[VII] were also synthesized. Some of these compounds have been tested for their antimicrobial activity

Synthesis of some new quinoline derivatives of potential antimicrobial activity

A series of quinolinoxy methyl-1,3,4-oxadiazoles [2 and 3], N-imido derivatives [5,6], pyrazole [7], pyrazolone [8], pyrazolidindione [9], Schiff bases [10a-f] and 8-O [2-oxo-3-indolinylidene] acetic acid hydrazido] 5,7 diiodoquinoline [4] was prepared. Some of the new compounds showed considerable antimicrobial activity against Gram +ve and Gram -ve bacteria, yeast and fungi

New pyridazinedione derivatives: synthesis and antimicrobial activity

Various substituted and unsubstituted pyridazine-3, 6-diones were prepared in a good yield via the reaction of p-nitrobenzoic acid hydrazide with diacyltartaric acid anhydride, maleic or phthalic acid anhydride [I-IV]. Then, each pyridazinone derivative was condensed with urea, thiourea or hydrazine to afford the corresponding pyridazinotriazine or triazolopyridazine derivatives [V-XVI], respectively. The spectral properties of the products were studied and the antimicrobial activity was evaluated

Synthesis of some new benzimidazole derivatives as antimicrobial agents

Synthesis of 2-[p-4-aryl-3-cyano-2-oxo[IH] pyridin-6-yl] anilino] benzimidazoles [2a-g] and the 2-[p-[4-aryl-3-cyano-2-imino[IH] pyridin-6-yl] anilino] benzimidazoles [3a-g] were obtained in one step reaction between the 2-[p-acetylanilino] benzimidazole [1] with ethyl cyanoacetate and/or malononitrile and the appropriate aldehydes in the presence of ammonium acetate. The new compounds showed considerable antimicrobial activity against Gram +ve, Gram -ve bacteria, yeast and fungi

New synthesis of some 1,8 naphthyridines of possible antimicrobial activity

Some new 2,7-dimethyl-4-[p-[5-aryl-2-pyrazolin-3-yl] anilino] 1, 8-naphthyridines [4a-d] and other related products of the isoxazolines [5a-d] and the pyrimidines [6a-d] were synthesized for the purpose of antimicrobial evaluation. Some representative examples of 4b,c, 5a and 6a showed moderate activity against the growth of Bacillus subtilis, Staphylococcus aureus and Aspergillus niger

New antimicrobial quinazolinone derivatives

A series of quinazolin-4-ones incorporated with pyridones, iminopyridines, thiazole, semicarbazone and thiosemicarbazone moieties were synthesized. Some tested compounds showed considerable biological activity against some microorganisms