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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.

An anticipated effect of khellin, related to its chemical structure, in the photochemotherapy of amelanosis has been investigated. In a double-blind clinical study, khellin has been orally administered to 30 vitiligo patients for 4 months with subsequent exposure to natural sunlight. At the end of the trial period. 5 patients out of 30 (16.6%) repigmented 90–100%; 7 cases (23.3%) repigmented 50–60% of the vitiliginous areas treated; 11 (36.6%) repigmented 25% or less, and 7 subjects (23.3%) showed negative response. 30 control subjects failed to repigment at all. The achieved repigmentation was stable after drug cessation for a period of 1 year. These data add a previously unreported effect for the non-psoralen compound, khellin, in the therapy of vitiligo.

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.

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