Synthesis and biological activity of β-acylhydrazides of aroylpyruvic acids

(Het)aroylpyruvic acids and their derivatives as promising building blocks for organic synthesis

“…The most diverse and the highest biological activities were found for (H)APA amides and hydrazides. Substances with analgesic, 31,54,59,61,62,73,94,179,190 antiinflammatory, 31, 42, 50, 54, 57 ± 60, 62, 69, 70, 72, 73, 85, 94, 179 anticonvulsant, 43,61 antiviral 69 ± 71 and antibacterial 50,51,57,58,61,62,66,69,70,73,77,86,179,190 activities have been found among this group.…”

“…Many heterocyclic compounds obtained from (H)AP possess various types of physiological activities. The pyrazoles 66 (R 1 = NHR 2 ) exhibit antiinflammatory, 31,59,62,73 analgesic 59,73 and antibacterial 62,69,128 activities with low toxicity. 5-(3-Pyridyl)-3-hydrazinocarbonylpyrazole (66, Ar = 3-pyridyl, R = NHNH 2 ) has been patented as an antitumour agent.…”

Synthesis and antibacterial activity of tetrahydroquinolin-8-ols

“…The samples were incubated in a thermostat for 20 -24 h at 37°C. The bacteriostatic effect was assessed by the presence or absence of growth of the test microbes and the active dose was estimated as the minimum concentration (MIC, mg/ml) inhibiting the growth of the test microbes [7,8].…”

Synthesis and Antimicrobial Activity of β-N-(Benzoyl)Hydrazides of 4-Aryl-2-hydroxy-4-oxo-butenoic (Aroylpyruvic) Acids

“…In addition to the signals due to aromatic protons (d = 7.21 -7.8 ppm), there is a singlet due to the methine proton (d = 6.9 -7.31). The signals from b-methylene groups are missing in the spectra of all compounds except V, which is indicative of their complete enolization [3]. The signals from protons of the amino groups of the hydrazide fragment are manifested by two singlets (10.61 -10.72 and 10.9 - 1 11.2 ppm for compounds I, III, V, VI, and VIII containing methoxy groups) or by a broad signal (8.8 -10.1 ppm for compounds II, IV, VII, and IX containing nitro groups).…”