A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. ...

A series of twelve fluorinated and non-fluorinated potential histone deacetylase inhibitors 25 was synthesized and their inhibitory activity was tested against rat liver histone deacetylase. The new inhibitors involve an enzyme binding element consisting of asparagine, glutamine or different sho...

[Ru(bpy)2(bqdiBr2)](PF6)2 ([1](PF6)2, bpy = 2,2′-bipyridyl, bqdiBr2 = 3,6-dibromo-1,2-benzoquinone diimine) was synthesized by the reaction of 3,6-dibromo-1,2-phenylenediamine with [RuCl2(bpy)2] in air, and the reactivity of [1](PF6)2 in Pd-catalyzed cross-coupling reactions with metalated thio...

New polymeric membrane (PME), modified carbon paste (MCPE), and coated wire (CWE) selenite ion-selective electrodes based on 5,10,15,20-tetrakis-(4-methoxyphenyl)-21H,23H-porphyrin-Co(II) (CoTMeOPP) are reported. The best composition was the electrode containing 2% CoTMeOPP as the active materia...

A purely organic and high-spin polyradical molecule was synthesized, along the non-Kekulé and non-disjoint design of the π-conjugated poly(1,2-phenylenevinylene) backbone pendantly 4,6-substituted with the robust arylaminium radicals. 4,6-Bis(bis(4-methoxyphenyl)amino)-2-bromostyrene was synth...

The toxic action of a series of O-alkyl, O-substituted-phenyl alkyl- and aryl-phosphonates and phosphonothionates have been evaluated by correlating the linear free energy parameters for steric (Es), electronic (σ), and polar (σ∗) effects with topical LD50 to the house fly and oral LD50 to the...

The metabolism of a single, dermal dose of 50 mg/kg of [14C]tri-o-cresyl phosphate (TOCP) was studied in male rats. TOCP was applied to an unprotected, preclipped area on the back of the neck. Three animals were sacrificed on each of 0.5, 1, 2, 5 and 10 days following application. Radioactivity ...

Ethyl 2-(4-bromophenyl)-1-(2,4-dichlorophenyl)-1H-4-imidazolecarboxylate (TG41) enhanced the binding both of γ-aminobutyric acid (GABA) and of flunitrazepam to rat cerebral cortical membranes. Electrophysiological recordings from Xenopus oocytes expressing various recombinant GABAA receptor sub...

The paper reported the synthesis and antifungal properties and mechanism of action of a series of 2-substituted methylthio-5-(2,4-dichlorophenyl)-1,3,4-oxadiazole/thiadiazole and their corresponding sulfones. The preliminary biological test showed these compounds exhibit moderate to good antifun...

A series of 14 ethyl 1-(2,4-dichlorophenyl)-1H-pyrazole-3-carboxylates has been synthesized from the cyclocondensation reaction of ethyl 4-methoxy-2-oxoalk[cycloalk]-3-enoates [EtO2CC(O)C(R2) = C(R1)OR, where R = H, Me; R1 = Pr, Ph, 4-MeOC6H4, 4-MeC6H4, 4-FC6H4, 4-ClC6H4, 4-BrC6H4, 4-NO2C6H4, fu...

A series of 2-mercapto-6-phenylpyrimidine-4-carboxylic acid derivatives (7a‒c, 8a‒e, 9a‒e and 10a‒e) as novel xanthine oxidase inhibitors were designed based on molecular docking, and synthesized by a new method using ketoenol acids and thiourea as the starting materials. In vitro activity assay...

The work describes a discovery of new chemical family of potent ligands for the 5-HT6 serotonin receptors. During the search for new histamine H4 receptor antagonists among 1,3,5-triazine derivatives, compound 2 (4-benzyl-6-(4-methylpiperazin-1-yl)-1,3,5-triazin-2-amine) was found. Compound 2, w...

A series of novel nitrofuranyl methyl N-heterocycles based on the structure of IIIM-MCD-211 were designed and synthesized. Compounds 6d, 8b and 12a show excellent activity against MTB H37Rv strain (MIC: 0.031–0.062 μg/mL) roughly comparable to INH and IIIM-MCD-211. In addition, a three-dimensi...

A variety of trifluoromethylated bi- and terphenyls were prepared by site-selective Suzuki–Miyaura cross-coupling reactions of various dihalogenated trifluoromethyl-substituted benzene derivatives. The reactions proceed with excellent site-selectivities.

PPARs are ligand-activated transcription factors that govern lipid and glucose homeostasis and play a central role in cardiovascular disease, obesity, and diabetes. Herein, we present screening results for a series of chiral 2-(4-chloro-phenoxy)-3-phenyl-propanoic acid derivatives, some of which...

We report here the transformation of 3/5-trifluoromethylpyrazoles derivative into the corresponding NH-pyrazole-3/5-carboxylic acids. Moreover, from 4- or 5-iodinated-3/5-trifluoromethylpyrazoles building blocks and the use of Suzuki–Miyaura or Negishi reactions followed by the trifluoromethyl ...

A method for the preparation of aryl- and heteroarylamine products by triethylphosphine-mediated deoxygenative coupling of nitroarenes and boronic acids is reported. This method provides access to an array of functionalized (hetero)arylamine products from readily available starting materials und...

Reaction of the potassium salts of N-thiophosphorylated thioureas of common formula RNHC(S)NHP(S)(OiPr)2 [R = pyridin-2-yl (HLa), pyridin-3-yl (HLb), 6-amino-pyridin-2-yl (HLc)] with Cu(PPh3)3I in aqueous EtOH/CH2Cl2 leads to mononuclear [Cu(PPh3)2La,b–S,S′] (1, 2) and [Cu(PPh3)Lc–S,S′] (3) ...

Ferric oxyhydroxides are natural scavengers of antimony, thus, they contribute significantly to antimony immobilization in soils and sediments. Recent studies, however, usually omit microbial influence on geochemically stable antimony-ferric oxyhydroxide association. Therefore, we have evaluated...

Water contamination by toxic compounds has become one of the most serious problems worldwide. Catalytic reduction using metal nanoparticles offer opportunities for environmental benefits. In this study, cellulose acetate-ferric oxide nanocomposite (CA/Fe2O3) was prepared and used as support for ...