Synthesis, characterization and reactions of 2-deoxo-5-deazaalloxazines.

5-Deazaflavins and their homologues have been known as potential riboflavin antagonists, bioreductives, and compounds with potent antitumor activity. 2-Amino-4-methylquinoline-3-carbonitrile (2) was prepared as unreported starting material for several interesting 2-deoxo-5-deazalloxazine derivatives. Cyclization of 2 using formamide afforded the 2,4-deoxo-5-deazaalloxazine derivative 7, which was subjected to deamination with nitrous acid to give the 2-deoxo-5-deazaalloxazine (8). The compound 8 was also obtained via 13 by treating the latter with refluxing formic acid or formamide and used as a precursor for synthesis of several 2-deoxo-5-deazaalloxazines 18, 19, 20, 21 and 22. The pharmacological and biological properties of these compounds are still under investigation.

3-Bromomethyl-propyphenazone as a new derivatization reagent for high performance liquid chromatography of captopril and hydrochlorothiazide with UV-detection.

3-Bromomethyl-propyphenazone (BMP) was used as a derivatization reagent for the detection and quantification of captopril (CAP) and hydrochlorothiazide (HCT) by high performance liquid chromatography using Zorbax C8 column, and 0.05M sodium acetate, acetonitrile, methanol (14:17:4; pH 6.5) as mobile phase system with UV-detection at 254 nm. The cited reagent reacts with the mercapto and amino groups of CAP and HCT in acetone using anhydrous potassium carbonate as hydrobromide acceptor. The reaction was completed within 30 min for CAP and 60 min for HCT with heating at 105 +/- 5 degrees C in mini-reaction vial. The linear concentration ranges for both CAP and HCT were 8 to 160 and 6 to 140 ng per injection, respectively. The derivatized captopril was synthesized and confirmed with spectral analysis. This method was applied for determination of spiked captopril in human urine after extraction with Extrelut-20 column using ethyl acetate:isopropanol (85:15 v/v) as eluant.

Toxic effect of ethanolic extract of Nerium oleander (Apocynaceae) leaves against different developmental stages of Muscina stabulans (Diptera-Muscidae).

Nerium oleander (Apocynaceae) is evergreen shrubs widely used for ornamental purpose in mediterranean region. The present investigation, revealed for the first time the insecticidal effect of ethanolic extract from leaves of this plant against 2nd instar larvae of the medically important false stable fly Muscina stabulans (Diptera: Muscidae). LC50 of the extract was 113.66 ppm. This dose delayed larval and pupal duration suppressed oviposition and decreased adult longevity of the survivors. Morphogenic abnormalities were recorded and photographed in larval, pupal and adult stages, which were produced from treating 2nd instar larvae with different concentrations of the extract.

Fault-tolerant training for optimal interpolative nets.

The optimal interpolative (OI) classification network is extended to include fault tolerance and make the network more robust to the loss of a neuron. The OI net has the characteristic that the training data are fit with no more neurons than necessary. Fault tolerance further reduces the number of neurons generated during the learning procedure while maintaining the generalization capabilities of the network. The learning algorithm for the fault-tolerant OI net is presented in a recursive formal, allowing for relatively short training times. A simulated fault-tolerant OI net is tested on a navigation satellite selection problem.

Synthesis and biological activity of some new benzimidazolyl-azetidin-2-ones and -thiazolidin-4-ones.

Arylidene-2-aminobenzimidazoles (1) were prepared by condensation of 2-aminobenzimidazole with aromatic aldehydes. Cyclocondensation of mercaptoacetic acid, chloracetylchloride and phthaloyl glycyl chloride on 1 giving the corresponding 4-thiazolidinones (2) and azetidinones (3 and 4) respectively, in good yields. The biological activities of the prepared compounds were screened against several strains of bacteria.

Synthesis of some new heterocyclic 1,3,4-oxadiazoles with antibacterial activity.

2-N-Aryl/heterocyclic carboxamidomethylthio-5-p-chlorophenyl-1,3,4-oxadiazoles have been synthesized by the reaction of 1 and N-aryl/heterocyclic-2-chloracetamides in presence of basic medium. 2 and 3 react with heterocyclic thiols in ethanolic potassium hydroxide to give 3-S-substituted-mercaptomethyl-5-substituted-phenyl-1,3,4-oxadiazol-2-thione 5 and 6 respectively. Tert. amines react with 2 to yield the corresponding amino chlorides in good yield. Some of the prepared compounds were tested as antibacterials against Gram-positive and Gram-negative organism.