54384-73-5Relevant academic research and scientific papers
One-step synthesis, crystallographic studies and antimicrobial activity of new 4-diazopyrazole derivatives
Daidone,Bajardi,Plescia,Raffa,Schillaci,Maggio,Benetollo,Bombieri
, p. 461 - 468 (2007/10/03)
A number of new 4-diazopyrazole derivatives were prepared by the reaction of 1-R-3-methyl-5(R1-substituted)benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic medium. The compounds were tested for activity against Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Staphylococcus epidermidis, Streptococcus faecalis, Listeria monocytogenes, Candida albicans, Candida tropicalis and Paecilomyces varioti. The highest microbial susceptibility was shown by Gram-positive bacteria, with minimum inhibitory concentrations (MIC) in the range 0.5-12.5 μg/mL. For S aureus the R1 substituents were screened utilizing the Topliss operational scheme. The 4-nitro group was found to be the best substituent. We also tested the compounds 41,o,p, found to be the most active in the test against S aureus ATCC 25923, on ten clinical S aureus strains, five of which were sensitive and five resistant to methicillin. The above compounds were active in the range 2-8 μg/mL against methicillin-resistant S aureus strains. An X-ray analysis of compounds 4i and 4q is reported.
A NEW ROUTE TO THE SYNTHESIS OF IMIDAZOPYRAZOLES
Vicentini, Chiara Beatrice,Veronese, Augusto Cesare,Giori, Paolo,Guarneri, Mario
, p. 6171 - 6172 (2007/10/02)
A new synthesis of imidazopyrazoles, obtained through cyclisation of 4-nitroso-5-alkylamino-pyrazoles, is described.
A NEW SYNTHESIS OF 1,3-THIAZIN-4-ONES VIA 1,3-OXAZINIUM SALTS FROM N-ACETOACETYLCARBOXAMIDES.
Yamamoto, Yutaka,Azuma, Yutaka,Ohnishi, Shuhei
, p. 851 - 856 (2007/10/02)
In the formation of 1,3-oxazinium salts from N-acetoacetylcarboxamides (1), the effect of acids such as 70percent perchloric acid (3a), 98percent sulfuric acid (3b), 36percent hydrochloric acid (3c), saturated hydrogen chloride-ethanol solution (3d), trifluoroacetic acid (3e), and acetic acid (3f) was examined by the established method leading to the pyrazole (5) via 1,3-oxazinium salt (2), and the order was as follows; 3a > 3b > 3e 3d >3c (3f was uneffective).The result was applied to synthesize 2-substituted 1,3-thiazine derivatives (7a-e, 8a,b) via 1,3 oxazinium salts from 1a-f and hydrogen sulfide in the presence of acetic anhydride in satisfactory yields.
Pyrazolodiazepines. 2. 4-Aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e][1,4]diazepin-7(1H)-ones as antianxiety and anticonvulsant agents
DeWald,Lobbestael,Butler
, p. 1562 - 1569 (2007/10/05)
A series of 4-aryl-1,3-dialkyl-6,8-dihydropyrazolo[3,4-e][1,4] diazepin-7(1H)-ones was synthesized and screened for psychotropic activity. In animals, a number of these pyrazolodiazepinones had strong CNS effects similar to diazepam. One compound, 4-(2-fluorophenyl)-6,8-dihydro-1,3,8 trimethylpyrazolo[3,4-e][1,4)diazepin-7(1H)-one (54), is being studied in the clinic as a component of a new animal anesthetic Tilazol.
