The synthesis and anti-Candida activity of 1-[(3-aroyloxy-3-phenyl)propyl]-1H-imidazoles 5a-f and 1-[(3-alkyl/aralkyl/phenyl-3-phenyl)propan-3-ol]-1H-imidazoles 5g-j are reported. The influence of the ester formation and different substitutions on the anti-Candida activity of the alcohol 4 was investigated. Among the newly developed bioactive chemical entities, compounds 5b and 5c displayed minimum inhibitory concentrations (MICs) against Candida albicans and Candida pseudotropicales comparable to that of tioconazole and more potent than miconazole.
Epilepsy is a common chronic neurological disorder characterized by recurrent unprovoked seizures. There has been a considerable interest in the development of many antiepileptic and anticonvulsant agents for controlling epilepsy with fewer side effects and improvement of quality of life. Since the terms antiepileptics /anticonvulsants are used interchangeably, this article reviews their classification according to the chemical structure into: hydantoins, oxazolidinediones, succinimides, barbiturates, amides, benzodiazepines, valproic acid and its derivatives, GABA-analogues, cycloalkanes, semicarbazones, γ butyrolactones (GBLs), imidaquinazolines and pyrrolidine derivatives as well as miscellaneous compounds. In addition, the review discusses the different mechanisms of action of antiepileptic and anticonvulsant agents.
A series of novel spiroimidazolidinone derivatives 6a-d and 8a-x were synthesized and biologically evaluated for their anticonvulsant activity in the maximal electroshock seizure (MES) assay and the subcutaneous pentylenetetrazole (scPTZ) screening test. Compound 8w was the most active derivative in the scPTZ screening test with an ED50 value by about 5- and 83.6-fold lower than those of phenobarbital and ethosuximide as reference drugs, respectively. Most of the tested compounds exhibited moderate to weak activity in the MES screen test, except for 8a which displayed 100% protection at 0.09 mmol/kg. Moreover, all the test compounds did not show any minimal motor impairment in the neurotoxicity test.
A simple, rapid, and validated method for separation and determination of terbutaline enantiomers was developed. Terbutaline was separated and determined on a Vancomycin Chirobiotic V column (250 Â 4.6 mm), using a mixture of methanol, acetic acid, and triethylamine (100:0.1:0.1% v=v=v) as a mobile phase at 20 C and at a flow rate of 1 ml=min. The UV detector was set to 276 nm. Acetyl salicylic acid (aspirin) was used as an internal standard. The applied highperformance liquid chromatography (HPLC) method allowed separation and quantification of terbutaline enantiomers with good linearity (r > 0.999) in the studied range. The relative standard deviations (RSD) were 1.10 and 1.32% for the terbutaline enantiomers with accuracy of 99.80 and 99.55. The limit of detection and limit of quantification of terbutaline enantiomers were found to be 0.05
3221Downloaded by [University of Birmingham] at 01:17 23 March 2015 and 0.10 mg Á ml À1 , respectively. The method was validated through the parameters of linearity, accuracy, precision, and robustness. The HPLC method was applied for the quantitative determination of terbutaline in pharmaceutical formulations.
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