Patients suffering from pulmonary tuberculosis were investigated for the levels of isoniazid (INH) and its metabolites viz. acetyl-INH, mono and diacetyl hydrazines and ammonia. It was observed that 50% of the patients are slow inactivators of INH and almost all show an increase in circulating levels of NH3 at 6 hrs. Mono and diacetyl hydrazine levels in blood and urine were detectable in all t...

BACKGROUND The pyrazolyl ketone motif of RO3201195, which exhibits good oral bioavailability and high selectivity for p38 MAPK over other kinases, is a key pharmacophore that could find application in the treatment of Werner syndrome. RESULTS AND DISCUSSION Microwave irradiation promotes Knoevenagel condensation of a β-ketonitrile and formamidine, to give β-aminovinyl ketones, and their subse...

The reaction of the cyanoacetylhydrazine (1) with α-bromoketones (2a-c) gave the hydrazide-hydrazone derivatives 3a-c. The latter compounds underwent ready cyclization when heated in sodium ethoxide to form the 1,3,4-oxadiazine derivatives 4a-c. The reaction of 3a with hydrazines gave the 1,3,4-triazine derivatives 7a,b. Compounds 3a-c and 7a,b underwent some heterocyclizations when treated wit...

A series of novel 3, 4-methylenedioxybenzene scaffold incorporated 1,3,5-trisubstituted-2-pyrazoline derivatives was synthesised as potent antitubercular agents via chalcone intermediates by reaction with hydrazines. The structures of the compounds were confirmed by IR, 1HNMR, 13CNMR and mass spectral data. The novel pyrazolines were screened for in vitro antitubercular activity by almar blue d...

A halogenmethylsulfonyl moiety is incorporated in numerous active herbicides and fungicides. The synthesis of tribromomethyl phenyl sulfone derivatives as novel potential pesticides is reported. The title sulfone was obtained by following three different synthetic routes, starting from 4-chlorothiophenol or 4-halogenphenyl methyl sulfone. Products of its subsequent nitration were subjected to t...

New Schiff bases, hydrazones and semicarbazones derived from 1,2-dihydro-4-hydroxy-6-methyl2-oxoquinoline-3-carbaldehyde, have been synthesized. The semicarbazone was subjected to react with 2,3-dichloroquinoxaline, chloroacetic acid, and oxalyl chloride affording multiaza­ heterocycles substituted to quinolone moiety at position 3. Condensation of the 2-imidazolidinethione derivative with some...

The unexpected tendency of amines and functionalized hydrazines to reduce ethyl 3-phenylquinoxaline-2-carboxylate 1,4-di-N-oxide (1) to afford a quinoxaline 1c and mono-oxide quinoxalines 1a and 1b is described. The experimental conditions were standardized to the use of two equivalents of amine in ethanol under reflux for two hours,with the aim of studying the distinct reductive profiles of th...