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At least 289 records · Page 16Linked to original sources
PubMed1997

Lipoxygenase inhibitors, Part 6. Synthesis of new tetrahydropyrazine and other heterocyclic compounds by reaction of hydrazonoyl chlorides.

Cyclization reactions of alpha-ketoarylhydrazonoyl chlorides with various dinucleophiles lead to new 1,4-benzothiazine, quinoxaline, tetrahydropyrazine, thiazole, and thiadiazoline derivatives of methyl butanoate or methyl 5-oxopentanoate. The inhibition of 5-lipoxygenase (LO) was determined by monitoring the leukotriene B4 (LTB4) formation of human polymorphonuclear leukocytes (PMNL). The IC50 values for the most active compounds with an arylhydrazone structure were found to lie between 0.7 and 7.5 microM.

Heterocyclic Compounds↗
PubMed1982

Thiomethylation and thiohydroxylation--a new pathway of metabolism of heterocyclic compounds.

1. G.l.c.--mass spectral analysis of t.l.c. fractions of urine samples of patients treated with 5-(2-chloroethyl)-4-methylthiazole (clomethiazole), has revealed two minor metabolites, each with two sulphur atoms. 2. Their structures were found to be 2-methylthio-clomethiazole and 5-acetyl-4-methyl-2-mercapto-thiazole, formed by thiomethylation and thiohydroxylation, respectively, of the original compound. 3. The structures of six other minor metabolites resulting from side-chain degradation have been elucidated. 4. The occurrence of metabolites with substituents at position 2 of the heterocyclic nucleus is assumed to be initiated by oxidative attack at the nitrogen, followed by nucleophilic substitution in position 2.

Chemical Phenomena↗
PubMed2001

Facile synthesis and biological evaluation of heterocyclic compounds containing diazepam.

Diazepamoxadiazoles 4, 5, 6, 12, 14 and 22 were prepared with the binary form system. Diazepamthiadiazoles 15, 20 and Diazepamtriazoles 7, 8, 9, 17, 18, 19 and 21 were also shapely synthesized. Some of these compounds were screened to test their antibacterial activity against E. coli and B. subtilis compounds 15 and 20 show potent activity against these bacteria.

Anti-Bacterial Agents↗