Two dehydroacetic acid (DHA, L1H) related imine ligands, L2H and L3H were obtained in moderate yields by reacting DHA with 2,4,6-trimethylaniline and phenylhydrazine, respectively. Refluxing [Ru (η6-p-cymene)Cl2]2 with two equivalents of L1Na, L2H and L3H in methanol generated ruthenium compoun...

A solid state Eu3+ complex with dehydroacetic acid (DHA) has been synthesized and characterized by elemental analysis, UV–visible, FT-IR, FT-Raman, powder and single-crystal X-ray diffraction and optical spectroscopy studies. The complex has formula [Eu(DHA)2(H2O)5]NO3 with DHA = C8H7O4−, where...

We report a series of novel metanilamide-based derivatives 3a–q bearing the 2-mercapto-4-oxo-4H-quinazolin-3-yl moiety as tail. All compounds were synthesized by means of straightforward condensation procedures and were investigated in vitro for their inhibition potency against the human (h) ca...

A series of twenty eight molecules of ethyl 5-(piperazin-1-yl)benzofuran-2-carboxylate and 3-(piperazin-1-yl)benzo[d]isothiazole were designed by molecular hybridization of thiazole aminopiperidine core and carbamide side chain in eight steps and were screened for their in vitro Mycobacterium sm...

To develop a novel series of CDK8/19 dual inhibitors, we employed structure-based drug design using docking models based on a library compound, 4,5-dihydroimidazolo[3′,4′:3,4]benzo[1,2-d]isothiazole 16 bound to CDK8. We designed various [5,6,5]-fused tricyclic scaffolds bearing a carboxamide g...

Here, we synthesized four kinds of monomers of 3,6-dibromo-(N-phenyl)carbazole with different substituent group, DCB, DDC, DNC and DTC, respectively, and used 4-(3-bromo-9H-carbazol-9-yl)benzaldehyde to react with triphenylamine (TPA) unit and hydrazine hydrate unit, respectively, to obtain the ...

Polyhalogenated carbazoles (PHCZs) are a class of contaminants identified with persistence and bioaccumulation property from previous studies. However, the toxic effect and mechanism of PHCZs are not fully understood. In this study, eleven PHCZs, including four chlorocarbazoles, four bromocarbaz...

An extract of Acacia georginae seed has yielded several amino compounds not previously recorded as plant constituents. These include an acidic sulphur-containing amino acid, S-(2-hydroxy-2-carboxyethane-thiomethyl)-l-cysteine, and the following γ-glutamyl peptides: γ-glutamylalbizziine, γ-glu...

The isolation of two acidic dipeptides, γ-glutamylaspartic acid and α-aspartylalanine, from pig brain is described. The identification of these dipeptides was based on comparison with the authentic compounds.

SLC-0111, an ureido substituted benzenesulfonamide, is a selective carbonic anhydrase (CA, EC 4.2.1.1) IX inhibitor that is currently in Phase I/II clinical trials for the treatment of advanced hypoxic tumors complicated with metastases. Herein we report the synthesis of two series of 3/4-(3-ary...

A group of 4-[2-(4-methyl(amino)sulfonylphenyl)-5-trifluoromethyl-2H-pyrazol-3-yl]-1,2,3,6-tetrahydropyridines (11–14) possessing a variety of substituents (Me, CO2Et, H, N = O) attached to the 1,2,3,6-tetrahydropyridyl N1-nitrogen atom were synthesized and evaluated as anti-inflammatory agents...

The synthesis, structure and spectroscopic properties of luminescent Zn(II) complex containing 4-methyl-N-[2-[(E)-pyridinylmethyl]phenyl]benzosulfimide ligand are described. The Zn(II) complex was characterized by single-crystal X-ray diffraction study. Time-dependent density functional theory c...

A series of novel N4-substituted 4-(2-aminoethyl)benzenesulfonamides 5–17 have been synthesized and investigated as inhibitors of four isoforms of zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1), that is the cytosolic CA I and II, and tumor-associated isozymes CA IX and XII. Against the human C...

The synthesis and structure–activity relationship of a series of benzenesulfonamide indole inhibitors of cPLA2α are described. Substitution of the benzenesulfonamide led to analogues with 50-fold improvement in potency versus the unsubstituted benzenesulfonamide lead compound. Rat pharmacokine...

Three series of novel heterocyclic compounds (3a–3g, 4a–4g and 5a–5g) containing benzenesulfonamide moiety and incorporating a 1,2,4-triazole ring, have been synthesized and investigated as inhibitors against four isomers of the α-class carbonic anhydrases (CAs, EC 4.2.1.1), comprising hCAs ...

A novel series of thio- and seleno-acetamides bearing benzenesulfonamide were synthetized and tested as human carbonic anhydrase inhibitors. These compounds were tested for the inhibition of four human (h) isoforms, hCA I, II, IX, and XII, involved in pathologies such as glaucoma (CA II and XII)...

As a continuation of previous tests concerning new N-substituted 3-amino-4-phenyl-5-oxo-pyrazolinecarboxamide derivatives (R3, R4 and R8) of notable antibacterial activity, their antitubercular potential against different mycobacterial strains was estimated. Tests performed on virulent (referenc...

A chalcone, 1-(4-chloro phenyl)-3-(4-dimethylamino phenyl) prop-2-en-1-one, abbreviated as CDAC was synthesized by the Claisen–Schmidt condensation method and single crystals were grown by the slow evaporation technique at ambient temperature. The structural confirmation was done using 1H-NMR, ...

Halogenated 4-hydroxybenzylidene indolinones have been shown to re-sensitize methicillin-resistant Staphylococcus aureus (MRSA) and vancomycin-resistant Enterococcus faecalis (VRE) to methicillin and vancomycin respectively. The mechanism of antibiotic re-sensitization was however not previously...

Despite recent advances in molecularly directed therapy, triple negative breast cancer (TNBC) remains one of the most aggressive forms of breast cancer, still without a suitable target for specific inhibitors. Maternal embryonic leucine zipper kinase (MELK) is highly expressed in TNBC, where lev...