The facile regioselective synthesis of the P(iii) substituted thiazol-2-thione 2 is presented. Reaction of 2 with hydrogenperoxide-urea, elemental sulfur and selenium resulted in P(v) chalcogenide thiazol-2-thiones 3-5. All compounds were characterized using (31)P, (1)H, (13)C NMR, IR and elemental analyses and, additionally, by the single-crystal X-ray diffraction technique. Oxidative desulfur...

The parallel solution-phase synthesis of a new combinatorial library of 3-[4-(R1-coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acid amides 9 has been developed. The synthesis involves two steps: 1) the synthesis of core building blocks - 3- [4-(coumarin-3-yl)-1,3-thiazol-2-ylcarbamoyl]propanoic acids, 6 - by the reaction of 3-(omega-bromacetyl)coumarins 1 with 3-amino(thioxo)methylcarbamoy...

In this study, eight new ethyl {2-[3,4-diaryl-3H-thiazol-2ylidenamino]thiazol-4-yl}acetate were synthesized by reacting ethyl [2-(3-aryl(thiouredio)thiazol-4-yl]acetate and phenacyl bromides in ethanol. The solid was filtered and recrystallized from ethanol. The chemical structures of the synthesized compounds were proven by elemental analysis, IR, 1H-NMR and MS spectral data. The compounds wer...

A series of 2-(benzo[d]thiazol-2-ylthio)-N-(2-oxoindolin-3-ylidene)acetohydrazide (3a3g), 2-(benzo [d]thiazol-2-ylthio)-N-(2,4’-dioxospiro[indolin-3,2’-thiazolidin)-3’yl)acetamide (4a-4g) and 2'-((benzo[d]thiazol-2-ylthio)methyl)spiro[indoline-3,5'thiazolo[4,3-b][1,3,4]oxadiazol]-2-ones (5a-5g) have been synthesized and screened for their anti-inflammatory, analgesic and antibacterial activitie...

Degeneration of the dopaminergic nigrostriatal system and of noradrenergic neurons in the locus coeruleus are important pathological features of Parkinson's disease. There is an urgent need to develop therapies that slow down the progression of neurodegeneration in Parkinson's disease. In the present study, we tested whether the highly specific metabotropic glutamate receptor 5 antagonist, 3-[(...

The treatment of cis-[PtCl2(XylNC)2] with thiazol-2-amines in a 2:1 ratio leads to regioisomeric mixture two binuclear complexes. These regioisomers are products kinetic and thermodynamic control capable regioisomerization. When the same reaction is carried out 5-fold excess thiazol-2-amine, nucleophile able react situ-formed platinum(II) complexes, yielding new type bis-carbene platinum specie...

In a search for new leads towards potent antibacterial agents, an array of novel N-[2-(3 ́chloro-2 ́-oxo-4 ́-substitutedaryl-1-azetidinyl)-1-3-thiazol-4-yl]diphenylamine 4(a-e) and N-[2-(2 ́substitutedaryl-4 ́-oxo-1 ́3 ́-thiazolidin-3 ́-yl)-1,3-thiazol-4-yl]diphenylamine 5(a-e) have been synthesized from N-(2-substitutedbenzylidenylimino-1,3-thiazol-4-yl)diphenylamine 3(a-e). Structure of all the synth...

Human neutrophil elastase (HNE) is a potent serine protease belonging to the chymotrypsin family and is involved in a variety of pathologies affecting the respiratory system. Thus, compounds able to inhibit HNE proteolytic activity could represent effective therapeutics. We present here the synthesis of new thiazol-2-(3H)-ones as an elaboration of potent HNE inhibitors with an isoxazol-5-(2H)-o...

Adenosine monophosphate-activated protein kinase (AMPK) has been identified as one of the major targets for antidiabetic drugs. This study describes two AMPK-activating agents 2-(benzo[d]thiazol-2-ylmethylthio)-6-ethoxybenzo[d]thiazole and 2-(propylthio)benzo[d]thiazol-6-ol, that increase the rate of glucose uptake in L6 myotubes and also augment glucose-stimulated insulin secretion in INS-1E β...

Novel 2-(1,5-bis(aryl)penta-1,4-dien-2-yl)benzo[d]thiazol (5a,b) and 2-(((1S,2S,E)-2(benzo[d]thiazol-2-yl)-1,5-di-arylpent-4-en-1-yl)thio)aniline (6a,b) derivatives were obtained by addition of 2aminobenzothiol to bis-benzylidinecyclobutanones (3a,b). The structures of the obtained compounds were characterized using the spectroscopic methods (NMR, IR, Elemental Analysis). Compounds 5a,b showed ...