The incubated whole-cell biocatalyst of Pichia minuta JCM 3622 reduced 2-chloro-1-(3-nitrophenyl)ethanone to provide (R)-2-chloro-1-(3-nitrophenyl)ethanol with 99.2% ee in 87% isolated yield in the presence of Amberlite XAD-7 as a reservoir for the hydrophobic, crystalline and toxic substrate. T...

Four esterase inhibitors, ethylenediamine tetraacetic acid disodium (Na2EDTA), sodium fluoride (NaF), bis(4-nitrophenyl) phosphate (BNPP) and phenylmethanesulfonyl fluoride (PMSF), were evaluated for their inhibitory effects on enzymatic hydrolysis of labile phenolate esters in curcumin diethyl ...

The extraordinary stability of bridged O,O-[cobalt bis(dicarbollide)ion] O-(4-nitrophenyl)phosphorothioate [2]- and phosphate [3]- esters under alkali conditions was discovered. The hydrolysis of metallacarborane esters [2]- and [3]- was studied, and the kinetic and thermodynamic parameters were...

A series of 27 salicylanilide diethyl phosphates was prepared as a part of our on-going search for new antimicrobial active drugs. All compounds exhibited in vitro activity against Mycobacterium tuberculosis, Mycobacterium kansasii and Mycobacterium avium strains, with minimum inhibitory concent...

Both of the maleimide and carboxylic acid groups in 5-maleimidoisophthalic acid (MIPA) are reactive toward an amine group. The selective reaction between carboxylic acid and amine groups was successfully established and applied in preparation of polyamides (PA-MI) and copolyamides possessing mal...

To identify potent dual 5-HT2B and 5-HT7 receptor antagonists, we synthesized a series of novel carbonyl guanidine derivatives and examined their structure–activity relationships. Among these compounds, N-(9-hydroxy-9H-fluorene-2-carbonyl)guanidine (10) had a good in vitro profile, that is, pot...

First examples of Ag(I)-containing coordination polymers based on octahedral rhenium(III) chalcocyanide clusters, namely [{Ag(bpy)}{Ag4(bpy)4(μ-CN)}{Re6Q8(CN)6}] (Q = S in 1 or Se in 2; bpy = 2,2′-bipyridine), have been hydrothermally synthesized and characterized by single-crystal X-ray diffr...

A series of divalent nickel and copper complexes and a series of mixed-ligand nickel(II) chelates have been prepared and characterized. The general formula of the complexes is [cation]2[M(1,1-dithiolate)2] (M = Ni(II), Cu(II)), and that of the mixed-ligand is [Ni(enR)(SS)], containing the dianio...

A series of four new coordination compounds [{Cu(bpy)2(μ-CN)Cu(bpy)}2Re6S8(CN)6]·bpy·2H2O (1), [{Cu(bpy)}2(μ-CN)][{Cu(bpy)}3Re6S8(CN)6] (2) and [{Cu(bpy)(μ-CN)Cu(bpy)}2{Cu(bpy)}2Re6Q8(CN)6] (3, Q = Se; 4, Q = Te) have been synthesized by the reactions of hexanuclear rhenium(III) chalcocyani...

This report describes a new palladium catalyzed synthesis of 4-cyano-1,10-phenanthroline (nphen, 1), 4,7-dicyano-1,10-phenanthroline (dnphen, 2) and their corresponding ruthenium complexes. The two cationic complexes, [(tbbpy)2Ru(nphen)]2+ 3 and [(tbbpy)2Ru(dnphen)]2+ 4 (tbbpy = 4,4′-di-tert-bu...

Dichlorobis(triphenylphosphine)palladium(II)/tricyclohexylphosphine-catalyzed Suzuki–Miyaura cross-coupling of the 2-aryl-6,8-dibromo-1,2,3,4-tetrahydroquinolin-4-ones with arylboronic acids afforded the corresponding 2,6,8-triaryl-1,2,3,4-tetrahydroquinolin-4-ones, exclusively. The latter was ...

Novel tetrahydro-5H-benzo[e][1,4]diazepin-5-ones, several of them, containing the quinoline pharmacophore, were synthesized via a Schmidt rearrangement from their corresponding 1,2,3,4-tetrahydro-4-quinolones mediated by the NaN3/H2SO4 reaction conditions. Twelve of the obtained compounds were i...

Vinyl 2-chloroacetate was used as an efficient acyl donor for enantioselective acylation of racemic 1,2,3,4-tetrahydroquinolin-4-ols and 2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-ols with Novozyme 435 lipase. Two enantiocomplimentary tetrahydroquinolin-4-ol or tetrahydro-1H-benzo[b]azepin-5-ol deri...

2-Amino-3-benzoyl thiophenes have been widely reported to act as allosteric enhancers at the A1 adenosine receptor. Their activity can be increased considerably by appropriate substitutions at the 4- and 5-positions of the thiophene ring. Substituent size at the thiophene C-4 position seemed to ...

The 2-amino-3-(p-chlorobenzoyl)thiophene scaffold has been widely employed as a pharmacophore for the identification of small molecules acting as allosteric modulators at the adenosine A1 receptor. A new series of 2-amino-3-(p-chlorobenzoyl)-4-benzyl-5-arylthiophene derivatives, characterized by...

The synthesis process has been widely used in cobalt hydrometallurgical industry. To better operate the cobalt oxalate synthesis process, a data-driven model based hierarchical batch-to-batch optimization method is presented in this work. In the upper level of hierarchy, the proposed response su...

A series of 2-sulfonamidopyridine C-region derivatives of 2-(3-fluoro-4-methylsulfonamidophenyl)propanamide were investigated as hTRPV1 ligands. Systematic modification on the 2-sulfonamido group provided highly potent TRPV1 antagonists. The N-benzyl phenylsulfonamide derivatives 12 and 23 in pa...

The Candida rugosa lipase catalyzed esterification of butyric acid with amyl alcohol in isooctane and in solvent-free system was studied. Nearly complete conversion (>95%) of substrates was achieved using low enzyme amount of 0.5% (w/v) at 45 °C. The initial rates of esterification were attempt...

A commercial Candida rugosa lipase was immobilized into poly(N-isopropylacrylamide-co-itaconic acid) hydrogel under different pH immobilization conditions, characterized and evaluated for both hydrolytic activity in an aqueous medium and esterolytic activity in an organic medium. Although the ap...

One palladium dichloride adduct of a phosphine-pyridine ligand N-diphenylphosphanyl-2-aminopyridine (L1) [(L1)PdCl2] (1) has been prepared and structurally characterized. Compound 1 can be used as an effective catalyst for the Suzuki-Miyaura cross-coupling reactions of unreactive aryl chlorides ...