A new series of alkylthio imidazole analogues of captopril, an ACE inhibitor used in the treatment of hypertension, was designed and synthesized in order to obtain agents more active than captopril with less side effects. All the compounds thus prepared were purified and characterized by IR, NMR and Mass analytical instruments.

In a previous study we have investigated the monoamine oxidase (MAO) inhibitory properties of a series of 8-sulfanylcaffeine analogues. Among the compounds studied, 8-[(phenylethyl)sulfanyl]caffeine (IC(50) = 0.223 μM) was found to be a particularly potent inhibitor of the type B MAO isoform. In an attempt to discover potent MAO inhibitors and to further examine the structure-activity relations...

The synthesis of a series of purine analogues of the acyclonucleoside compound 14 (acyclovir) is described. Compounds in this series have been shown to have pronounced activity against herpes virus-type l(HSV-1). The anti-viral activities of other analogs whose syntheses were recently reported [1] by us are also described

Infrared spectra of some deuterio analogues of carboxylic acids in heavy water have been investigated and their spectral behavior in carbonyl stretching frequency region have been interpreted in terms of their structural behavior in aqueous solutions. It has been shown that a linear relationship exists between carbonyl stretching frequency of solvated acids at infinite dilution and their...

The nitrogen mustard derivatives of 4-phenylbutyric acid and L-phenylalanine, called chlorambucil (Chl) and melphalan (Mel), respectively, have been incorporated into several peptide hormones, including luteinizing hormone-releasing hormone (LH-RH). The alkylating analogues of LH-RH were prepared by linking Chl, as an N-acyl moiety, to the complete amino acid sequence of agonistic and antagonis...

Nucleoside analogues have proven to be a highly successful class of anti-cancer and anti-viral drugs. The therapeutic efficacy of nucleoside analogues is dependent of their intracellular phosphorylation. Two cellular nucleoside kinases, deoxycytidine kinase (dCK) and UMP-CMP kinase (CMK) are critical for phosphorylation of cytidine analogues. These kinases provide two first steps of activation ...

a quantitative structure-activity relationship (qsar) study was conducted for the prediction of inhibitory activity of 1-phenyl[2h]-tetrahydro-triazine-3-one analogues as inhibitors of 5-lipoxygenase. the inhibitory activities of the 1-phenyl[2h]-tetrahydro-triazine-3-one analogues modeled as a function of molecular structures using chemometrics methods such as multiple linear regression (mlr) ...