Efficient reductions of various nitroarenes with scrap automobile catalyst and NaBH4

The effect of scrap automobile catalyst (SAC), a waste material, was investigated as a catalyst for the reduction of nitroarenes to the corresponding amines with sodium borohydride in aqueous ethanol at 5-25 degrees C. Along with the observed high conversions, the SAC and NaBH4 combination also exhibits a selectively catalyzed reduction in compounds containing other reducible functionalities, such as - CN, - Br, - Cl and - I. Recycling automobile wastes into a catalyst for organic reactions will offer both environmental protection and economic advantages. As a result, an effective, easy to use, low-priced and reliable method has been developed. (C) 2015 Elsevier B.V. All rights reserved

In vitro inhibition of polyphenol oxidase by some new diarylureas

A new series of N,N'-diarylureas (1-9) was synthesized. These compounds were investigated as inhibitors of polyphenol oxidase (PPO) which had been purified from banana by an affinity gel comprised of Sepharose 4B-L-tyrosine-p-amino benzoic acid. K-i values for (1), (2), (3), (5), (6), (7) and (8) were determined as 0.285, 17.97, 0.187, 0.108, 0.063, 0.044 and 0.047 mM, respectively. Thus (2) was by far the most effective inhibitor. Interestingly, (4) and (9) behaved as an activator of PPO in this study

Synthesis and tyrosinase inhibitory properties of novel isoquinoline urea/thiourea derivatives

A new series of isoquinoline urea/thiourea derivatives (1-11) were synthesized, and their inhibitory effects on tyrosinase were evaluated. Isoquinoline urea/thiourea derivatives were obtained as a result of the reaction of 5-aminoisoquinoline with isocyanates or isothiocyanates. The result showed that all the synthesized compounds inhibited the tyrosinase enzyme activity. Among the compounds synthesized, 1-(4-chlorophenyl)-3-( isoquinolin-5-yl) thiourea (3) was found to be the most active one (Ki = 119.22 mu M), and the inhibition kinetics analyzed using Lineweaver-Burk double reciprocal plots revealed that compound 3 was a competitive inhibitor. We also calculated HOMO-LUMO energy levels, some selected the synthesized compounds (1, 4, 11, 3, 6, 2) using Gaussian software

Discovery of Potent Carbonic Anhydrase and Acetylcholinesterase Inhibitors: 2-Aminoindan beta-Lactam Derivatives

beta-Lactams are pharmacologically important compounds because of their various biological uses, including antibiotic and so on. beta-Lactams were synthesized from benzylidene-inden derivatives and acetoxyacetyl chloride. The inhibitory effect of these compounds was examined for human carbonic anhydrase I and II (hCA I, and II) and acetylcholinesterase (AChE). The results reveal that beta-lactams are inhibitors of hCA I, II and AChE. The Ki values of beta-lactams (2a-k) were 0.44-6.29 nM against hCA I, 0.93-8.34 nM against hCA II, and 0.25-1.13 nM against AChE. Our findings indicate that beta-lactams (2a-k) inhibit both carbonic anhydrases (CA) isoenzymes and AChE at low nanomolar concentrations

Reaction of cycloheptatriene derivatives with 1,3-diketones in the presence of Mn(OAc)(3)

The reactions of some 1,3-dicarbonyl compounds with cycloheptatriene derivatives in the presence of Mn(OAc)(3) were examined. Cycloheptatriene forms mainly [2+3] and [6+3] dihydrofuran addition products derived from cycloheptatriene. However, the reaction of acetylacetone with cycloheptatriene substituted with an electron withdrawing group exclusively gave products derived from the norcaradiene structure. The formation mechanism of the products as well as the role of the substituent attached to cycloheptatriene is discussed

A NEW ANTISEPTIC - FURFURYLAMINE BIGUANIDINE DERIVATIVE SYNTHESIS AND ITS EFFECT ON MULTI-DRUG RESISTANT ACINETOBACTER BAUMANNII STRAINS

Objective: The number of antiseptics used in a hospital environment are limited, hence some of them are restricted because of resistance. Furfurylamine biguanidine HCl (FBC) and furfurylamine biguanidine acetate (FBA) are new chemical antiseptics that have been developed by our group for the first time. With this research, we target to examine and investigate the antibacterial features of the new generation biguanidine derivatives against the multi-drug resistant Acinetobacter baumannii (MDRAb) strains. Method: Bactericidal efficacy was examined as per the DIN EN 1040 (DIN EN 1040, 2005) standard. A 5 log decrease in bacterial density was accepted as efficient. By the agar well diffusion method, the effects of FBC and FBA on the resistant Acinetobacter strains were investigated. Result: FBC and FBA were found as bactericidal efficient with 5 log decrease in bacterial density. FBC and FBA formed an inhibition zone of at least 15 mm in the 20 separate MDRAb strain disc diffusion tests. Conclusion: As FBC and FBA were isolated for the first time, they were deemed effective against MDRAb strains

An efficient hydrogenation of various alkenes using scrap automobile catalyst

An efficient, easy, cheap, convenient, and safe procedure for the reduction of various alkenes to the corresponding alkanes is developed by using scrap automobile catalyst as an efficient hydrogenation catalyst. This procedure not only gives high yields, but also allows recycling of automobile wastes as a catalyst in organic reactions and is representative of green chemistry. Crown Copyright (C) 2011 Published by Elsevier Ltd. All rights reserved

A NEW ANTISEPTIC - FURFURYLAMINE BIGUANIDINE DERIVATIVE SYNTHESIS AND ITS EFFECT ON MULTI-DRUG RESISTANT ACINETOBACTER BAUMANNII STRAINS

Objective: The number of antiseptics used in a hospital environment are limited, hence some of them are restricted because of resistance. Furfurylamine biguanidine HCl (FBC) and furfurylamine biguanidine acetate (FBA) are new chemical antiseptics that have been developed by our group for the first time. With this research, we target to examine and investigate the antibacterial features of the new generation biguanidine derivatives against the multi-drug resistant Acinetobacter baumannii (MDRAb) strains. Method: Bactericidal efficacy was examined as per the DIN EN 1040 (DIN EN 1040, 2005) standard. A 5 log decrease in bacterial density was accepted as efficient. By the agar well diffusion method, the effects of FBC and FBA on the resistant Acinetobacter strains were investigated. Result: FBC and FBA were found as bactericidal efficient with 5 log decrease in bacterial density. FBC and FBA formed an inhibition zone of at least 15 mm in the 20 separate MDRAb strain disc diffusion tests. Conclusion: As FBC and FBA were isolated for the first time, they were deemed effective against MDRAb strains

Synthesis, characterization, biological evaluation, and molecular docking studies of some piperonyl-based 4-thiazolidinone derivatives

Heterocyclic compounds are of particular importance among pharmacologically active compounds. In this study, some piperonyl-based 4-thiazolidinone derivatives (2a-i) were synthesized and characterized by spectroscopic assays. All molecules were tested as enzyme inhibitory factors. These compounds were effective inhibitors of the enzymes acetylcholinesterase (AChE), alpha-glycosidase (alpha-Gly), and the human carbonic anhydrase I and II isoforms (hCA I and II), with K-i values in the range of 8.90-66.51 nM for alpha-Gly, 94.8-289.5 nM for hCA I, 106.3-304.6 nM for hCA II, and 0.55-2.36 nM for AChE. The synthesized molecules were also studied theoretically. Molecular docking calculations were performed to investigate the interaction between the target protein and molecules. CA inhibitor compounds have been clinically used for almost 60 years as antiglaucoma and diuretic drugs. The inhibition of the AChE enzyme results in the blockage of ACh hydrolysis. On the contrary, the design of inhibitor compounds or/and modulators for AChE is of major interest as it is one of the most popular tools to prevent Alzheimer's disease