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The synthesis of novel 1,2,3-triazolyl-based metronidazole hybrid analogues as potent anti-Leishmania agents using [CuL-SiO-HA] as a catalyst has been described.

The design, synthesis and biological study of several novel 1,2,3-triazolyl [Formula: see text]-hydroxy alkyl/carbazole hybrid molecules as a new type of antifungal agent has been described. In this synthesis, the N-alkylation reaction of carbazol-9-ide potassium salt with 3-bromoprop-1-yne afforded 9-(prop-2-ynyl)-9H-carbazole. The 'Click' Huisgen cycloaddition reaction of 9-(prop-2-ynyl)-9H-carbazole with diverse [Formula: see text]-azido alcohols in the presence of copper-doped silica cuprous sulphate led to target molecules in excellent yields. The in vitro antifungal and antibacterial activities of title compounds were screened against various pathogenic fungal strains, Gram-positive and/or Gram-negative bacteria. In particular, 1-(4-((9H-carbazol-9-yl) methyl)-1H-1,2,3-triazol-1-yl)-3-butoxypropan-2-ol (10e) proved to have potent antifungal activity against all fungal tests compared with fluconazole and clotrimazole as studied reference drugs. Our molecular docking analysis revealed an appropriate fitting and a potential powerful interaction between compound 10e and an active site of the Mycobacterium P450DM enzyme. The strong hydrogen bondings between [Formula: see text]-hydroxyl and ether groups in 10e were found to be the main factors that drive the molecule to fit in the active site of enzyme. The in silico pharmacokinetic studies were used for a better description of 10a-10n as potential lead antifungal agents for future investigations.

Economical and environmentally friendly syntheses of three 3,4-dihydro-1H-quinoxalin-2-ones and six 1H-quinolin-2-ones have been developed by a 1: 1 reaction of o-, m-, or p-phenylenediamine with d...

The syntheses and biological studies of O-oxime ethers having α-amino acid residues as new analogs of IPS-339 have been described. In this synthesis, the reaction of fluorene and/or benzophenone O-oxime with epichlorohydrin or epibromohydrin afforded the corresponding O-oxime ether adducts. The N-alkylation of amino acid with O-oxime ether adducts led to synthesis of new analogs of IPS-339. The products were examined for their cardiovascular property. It was demonstrated that 2-(3-(9H-fluoren-9-ylideneaminooxy)-2-hydroxypropylamino)-3-methyl-butanoic acid as the most potent compound substantially reduces the heart rate of dogs. Compounds were also evaluated for their in vitro antibacterial activity against some Gram-negative and Gram-positive bacteria. The antibacterial screening proved the considerable antibacterial activity against both groups of bacteria. The docking analysis demonstrated the appropriate fitting of 2-(3-(9H-fluoren-9-ylideneaminooxy)-2-hydroxy-propylamino)-3-methyl-butanoic acid in human β2-adrenergic receptor active site. Potential drug toxicity for some active compounds has also been predicted.

The aim of this study was to investigate the ultra-structure of the photoreceptor layer of male rats under the effect of methanol intoxication and protective effect of silymarin against the methanol toxicity. Fifteen adult male rats were divided into three groups: Control group, Experimental group I (received 4g/kg methanol by intraperitoneal injection for five days), Experimental group II (received 4 g/kg methanol by intraperitoneal injection for five days and received 250 mg/kg silymarin orally for three months). At the end of the experiment, the eyes were removed; retina was separated near the optic disc and studied by transmission electron microscope. Results showed that the retina in the experimental group I exhibited loss of outer segments and disorganization in inner segment. Increased extra cellular space, disappearance of outer limiting membrane and pyknotic nuclei were seen in this group. But normal outer segment, organized inner segment and normal outer limiting membrane were obvious after treatment with silymarin in experimental group II. These findings show that methanol causes damage in the photoreceptor layer of the rat retina and silymarin can protect the damage to retina against the methanol intoxication. Key words: Ultra-structure, photoreceptor layer, methanol intoxication, silymarin, rat.

Introduction: The photoreceptor layer of retina has important role for sight. The previous study showed that accidental formaldehyde injection caused ischemia and damage in the retina. On the other hand the erythropoietin prevents neuronal injury of ischemic damage. Objectives: The aim of this study was to survey the effect of erythropoietin on retro bulbar formaldehyde injected photoreceptor layer of rat retina. Materials and methods: 30 adult rats were used and divided into three groups: 1- control group, 2- formaldehyde group (1 ml retro bulbar injected by 10% formaldehyde solution), 3- erythropoietin group (5000 units/kg immediately intraperitoneally injected by erythropoietin after formaldehyde injection for 7 days). The photoreceptor layer of retina studied using a transmission electron microscope. Results: Our observation showed that disorganization and vacuolization in outer segment and inner segment, pyknotic and karyolysis in outer nuclear layer were seen in formaldehyde group. But the minor sign of pathology such as lightly vacuolization in inner segment were obvious in erythropoietin group. Conclusion: We concluded that formaldehyde caused damage in photoreceptor layer and erythropoietin was improvement this injury. Nepal J Ophthalmol 2016; 8(15): 10-17