(E)-2-(benzo[d]thiazol-2-yl)-3-heteroarylacrylonitriles are described as a new class of selective inhibitors of acetylcholinesterase (AChE). The most potent compound in the series exhibited good AChE inhibitory activity (IC₅₀ = 64 µM). Compound 7f was found to be more selective than galanthamine in inhibiting AChE and it showed a moderate selectivity index. Kinetic studies on AChE indicated tha...

Two classes of modified analogs of 4-(thiazol-5-yl)benzoic acid-type CK2 inhibitors were designed. The azabenzene analogs, pyridine- and pyridazine-carboxylic acid derivatives, showed potent protein kinase CK2 inhibitory activities [IC50 (CK2α)=0.014-0.017μM; IC50 (CK2α')=0.0046-0.010μM]. Introduction of a 2-halo- or 2-methoxy-benzyloxy group at the 3-position of the benzoic acid moiety maintai...

The asymmetric unit of the title compound, [CdCl(2)(C(7)H(10)N(2)O(2)S)(2)], contains two complex molecules with similar configurations. The Cd(II) atoms are each six-coordinated by two thiazole N and two carbonyl O atoms from the 2-(2-amino-1,3-thiazol-4-yl)acetate ligand, and by two Cl(-) anions in a distorted octa-hedral geometry. In the crystal, intra- and inter-molecular N-H⋯Cl hydrogen bo...

PURPOSE The aim of this article is to synthesize, characterize and evaluate the antimicrobial activity of certain novel 3-methyl-5-oxo-4-(phenyl hydrazono)-4,5-dihydro-pyrazol-1-yl]-acetic acid N|-(4-substituted thiazol-2-yl)-hydrazides. METHODS The synthesized compounds were characterized by elemental analysis and IR, NMR and mass spectral data. The antimicrobial activity of novel compounds ...

Several pyridinylthiazolylazetidinones 4a-d, pyridinylthiazolythiazolidinones 5a-d and pyridinylthiazolylformazans 6a-d have been prepared from pyridinylthiazolylarylidines 3a-d. These compounds have been evaluated for insecticidal, anti-fungal and anti-bacterial activities. Compound 2-[2'-(3"-chloro-2"-oxo-4"-ohydroxyphenyl-1"-azetidinyl)-1',3'-thiazol-4'-yl) aminopyridine 4c has been found to...

A series of new 3-[(5-aryl-1,3,4-oxadiazol-2-yl)methy])benzo[d]thiazol-2(3H)-ones were synthesized by reaction of (5-substituted-2-oxobenzothiazolin-3-yl)-acetohydrazide with various aromatic acids in POCl(3) under reflux conditions. The structures of the title compounds were confirmed by ¹H-NMR, ¹³C-NMR, IR, MS and elemental analysis. Furthermore, the structure of compound 4i was determined by...

A series of substituted pyrazole, triazole and thiazole derivatives (2-13) were synthesized from 1-(naphtho[1,2-d]thiazol-2-yl)hydrazine as starting material and evaluated as androgen receptor antagonists and anti-prostate cancer agents. The newly synthesized compounds showed potent androgen receptor antagonists and anti-prostate cancer activities with low toxicity (lethal dose 50 (LD50)) compa...

In order to find a highly sensitive fluorophore, 3-azolyl-7-diethylaminocoumarin derivatives were synthesized. Both the absorption and fluorescence maxima of the coumarin-thiazole compounds showed red shifts with increases of the molar absorptivities and fluorescence intensities, in comparison with those of the corresponding coumarin-oxazole compounds. Among them, 3-(5-ethoxycarbonyl-1,3-thiazo...

A series of novel 2-(N-pyrrolidino, N-piperidino or N-morpholino)-7-phenyl(α-furoyl or α-thienyl)-[1,3]thiazolo[4,5-d]pyridazinones 10a-c, 14-16a,b was synthesized in 78-87% yields via the reaction of methyl 5-benzoyl(α-furoyl or α-thienyl)-2-aminosubstituted-thiazol-4-carboxylates 9a-c, 13a-e with hydrazine. These new compounds have been tested for their in vivo analgesic and anti-inflammatory...

Small-conductance (KCa2) and intermediate-conductance (KCa3.1) calcium-activated K channels are voltage-independent and share a common calcium/calmodulin-mediated gating mechanism. Existing positive gating modulators like EBIO, NS309, or SKA-31 activate both KCa2 and KCa3.1 channels with similar potency or, as in the case of CyPPA and NS13001, selectively activate KCa2.2 and KCa2.3 channels. We...