this work described a simple and efficient synthesis of dialkyl 3-(alkylamino)-1-aryl-1h-pyrazole-4,5-dicarboxylates via a three component reaction between arylhydrazine, alkylisocyanid and dialkylacetylenedicarboxylates in the presence of phenylisocyanate and α-fe2o3 nanoparticles. eco friendly, solvent-free conditions, excellent yields, and short reaction times, inexpensive and readily availa...

Inhibition of the cyclin dependent kinase 2 (CDK2) is a well-known cancer treatment approach. Based on molecular docking simulation analysis, two new series 2-(1-(4-methoxyphenyl)-2-(phenylsulfonyl)ethylidene)hydrazineylidene)-2,5-dihydrothiazole as CDK-2 inhibitors were designed. The lead compound IV (5-benzoyl-N2-phenyl-1,3-thiazole-2,4-diamine) was modified and optimized prior to this analys...

Inhibitions of the relatively highly purified flavoenzyme, bovine kidney mitochondrial monoamine oxidase, previously described in Paper I (Erwin, V. G., and Hellerman, L., J. Biol. Gem., 242, 4230 (1967)), by several agents of current interest have been investigated. The inhibitors include Nmethyl-N-(Z-propynyl)benzylamine (pargyline), (+)-fransphenylcyclopropylamine (d form of tranylcypromine)...

The arylamine N-acetyltransferase (NAT) enzymes have been found in a broad range of both eukaryotic and prokaryotic organisms. The NAT enzymes catalyse the transfer of an acetyl group from acetyl Co-enzyme A onto the terminal nitrogen of a range of arylamine, hydrazine and arylhydrazine compounds. Recently, several NAT structures have been reported from different prokaryotic sources including S...

HD formation from either Da and Hz0 or Hz and DzO is shown to be catalyzed by Nz-fixing extracts of Azotobacter vinelandii. The activity parallels nitrogenase but not hydrogenase activity and is not catalyzed by the sites of nitrogenase responsible for either ATP-dependent Hz evolution or competitive inhibition by Hz of Nz fixation. Requirements in addition to nitrogenase are NB, ATP, and reduc...

The NATs (arylamine N-acetyltransferases) are a well documented family of enzymes found in both prokaryotes and eukaryotes. NATs are responsible for the acetylation of a range of arylamine, arylhydrazine and hydrazine compounds. We present here an investigation into the catalytic triad of residues (Cys-His-Asp) and other structural features of NATs using a variety of methods, including site-dir...

Mixed-ligand hydride complexes OsHCl(CO)(PPh3)2L (2) [L = P(OMe)3, P(OEt)3] were prepared by allowing OsHCl(CO)(PPh3)3 (1) to react with an excess of phosphite P(OR)3 in refluxing toluene. Dichloro compounds OsCl2(CO)(PPh3)2L (3, 4) were also prepared by reacting 1, 2 with HCl. Treatment of hydrides OsHCl(CO)(PPh3)2L (2), first with triflic acid and then with an excess of RN3 afforded organic a...

Vilsmeier-Haack reaction of 2,3,3-trimethyl-3H-benzo[g]indole, then aqueous basic work-up, leads to benzo[g]indol-2-ylidene- malondialdehydes. These react with various arylhydrazines and quinolin-2-ylhydrazine to form 3,3-dimethyl-2-(1-aryl-1H-pyrazol-4-yl)- 3H-benzo[g]indoles in good yields.

interest in agrochemicals and drugs. Aryl group substituted pyrazoles and imidazoles, in particular, have been studied because their biological activities are strongly dependent on their substituents on the pyrazole ring system. 1,5-Diaryl substituted pyrazole (SR141716A, 1), which has a hydrazide group on the 3-position of the pyrazole ring, has recently been synthesized and identified as the ...