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This study aimed to use microwave irradiation as a green technique, not only to enhance the dyeing efficiency of disperse-colored polyester fabrics, but also to conserve resources and minimize the environmental effects. Arylazopyrazolopyrimidinones dyes 1-9 were applied to polyester fabrics at 2% shade using conventional method and microwave at 100 °C. Both the color intensity expressed as dye absorption and the fastness characteristics of the dyed fabric were investigated. The K/S values are increased by increasing the time of irradiation from 10-60 minutes. The dyed substrate displayed good light fastness, and very good fastness levels to rubbing, perspiration washing, and sublimation, respectively.

A new series of 2-aminothiazole derivatives was designed and prepared as phosphodiesterase type 5 (PDE5) regulators and COX-1/COX-2 inhibitors. The screening of the synthesized compounds for PDE5 activity was carried out using sildenafil as a reference drug. Strikingly, compounds 23a and 23c were found to have a complete inhibitory effect on PDE5 (100%) at 10 μM without causing hypotension and the limited side effect of PDE5 inhibitors, suggest a distinctive therapeutic role of these derivatives in erectile dysfunction. On the other hand, compounds 5a, 17, 21 and 23b increased the PDE5 activity (PDE5 enhancers) at 10 μM. In addition, the study includes the screening of the COX-1/COX-2 inhibition induced by the synthesized compounds. All tested compounds have an inhibitory effect against COX-1 activity (IC50 = 1.00–6.34 μM range) and COX-2 activity (IC50 = 0.09–0.71 μM range). Moreover, a molecular docking study was implemented to reveal the binding interactions of potent compounds in the binding sites of PDE5 (PDB ID 2H42), COX-1 and COX-2 (PDB ID 3LN1) enzymes. For the interaction with the PDE5 enzyme, activator compounds had a strong binding mode (HB with Gln817:A) than inhibitory derivatives. Both types of compounds are considered as PDE5 regulators. This novel finding will encourage us to discover a new pharmacological application of small chemical entities as the PDE5 enhancer, or will lower side effects as PDE5 inhibitors. All active compounds adopted the Y-shape along the COX-2 active site.

A new series of quinoline derivatives 5–12 were efficiently synthesized via one-pot multicomponent reaction (MCR) of resorcinol, aromatic aldehydes, β-ketoesters, and aliphatic/aromatic amines under solvent-free conditions. All products were obtained in excellent yields, pure at low-cost processing, and short time. The structures of all compounds were characterized by means of spectral and elemental analyses. In addition, all the synthesized compounds 5–12 were in vitro screened for their antioxidant and antibacterial activity. Moreover, in silico molecular docking studies of the new quinoline derivatives with the target enzymes, human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, were achieved to endorse their binding affinities and to understand ligand–enzyme possible intermolecular interactions. Compound 9 displayed promising antioxidant and antibacterial activity, as well as it was found to have the highest negative binding energy of -9.1 and -9.3 kcal/mol for human NAD (P)H dehydrogenase (quinone 1) and DNA gyrase, respectively. Further, it complied with the Lipinski’s rule of five, Veber, and Ghose. Therefore, the quinoline analogue 9 could be promising chemical scaffold for the development of future drug candidates as antioxidant and antibacterial agents.

In this study different Mixtures of folk plants (Artemisia monosperma and Phlomis floccose )in different proportions and different concentrations of the mixture are used to obtain new natural dyes and applying them to woolen fabric using microwave radiation and then studying the effect of extraction time and the pH of the dyeing bath on the strength of color and then studying the fastness of these dyes against light and Washing and perspiration

Our current study aims to study the effect of different metallic mordantson the new natural dyes that we were able to extract in a previous study. The extent to which the intensity of color is affected by the presence of metallic mordantshave been studied and also the effect of the concentration of each mordant on the natural dyes was investigated, and then the changes that took place on the color axes were screened, and then the fastness of the new dyes were studied after applying them to the woolen fabric

The elaboration of new small molecules that target phosphodiesterase enzymes (PDEs), especially those of type 5 (PDE5), is an interesting and emerging topic nowadays. A new series of heterocycle-based aminothiazoles were designed and synthesized from the key intermediate, 3-oxo-N-(thiazol-2-yl)butanamide (a PDE5 inhibitor that retains its amidic function), as an essential pharmacophoric moiety. The PDE5 inhibitors prevent the degradation of cyclic guanosine monophosphate, thereby causing severe hypotension as a marked side effect. Hence, an in vivo testing of the target compounds was conducted to verify its relation with arterial blood pressure. Utilizing sildenafil as the reference drug, Compounds 5, 10a, and 11b achieved 100% inhibitions of PDE5 without significantly lowering the mean arterial blood pressures (115.95 ± 2.91, 110.3 ± 2.84, and 78.3 ± 2.57, respectively). The molecular docking study revealed that the tested compounds exhibited docking poses that were similar to that of sildenafil (exploiting the amide functionality that interacted with GLN:817:A). The molecular shape and electrostatic similarity revealed a comparable physically achievable electrostatic potential with the reference drug, sildenafil. Therefore, these concomitant results revealed that the tested compounds exerted sildenafil-like inhibitory effects (although without its known drawbacks) on blood circulation, thus suggesting that the tested compounds might represent a cornerstone of beneficial drug candidates for the safe treatment for erectile dysfunction.

Condensation of β-Oxoanilide 1 with active methylene derivatives 2a,bafforded the pyridine derivative 5, and with crotononitrile afforded the pyridine 8. Compounds 9 and 11a-c were obtained by reaction of 1 with malononitrile dimer and arylidinemalononitrile 10a-10c. In contrast, when compound 1 reacted with ethoxymethylen malononitrile afforded the pyridine derivative 13. On the other hand, treatment of 1 with anthranilic acid gave the quinoline derivative 14. Also, reactions of 1 with isothiocyanate derivatives afforded compounds 16-18. The reaction of 1 with chalcone derivative afforded the pyridine derivative 22. Treatment of compound 1 with thiourea produced pyrimidine derivative 23. Furthermore, compound 1 converted into pyrimidinethione 24a and pyrimidinone 24b on treatment with a mixture of aromatic aldehydes and thiourea or urea respectively. Reaction of 24a with hydrazonyl halide, thiosemicarbazide and arylidinecyanothioacetamide afforded compounds 26, 28 and 29. Compound 29 was treated with chloroacetonitrile to afford compound 30. Six compounds from the newly synthesized were screened for antibacterial and antifungal activity against bacteria staphylococcus aureus, bacillus cereus and klebsiella pneumonia and fungi aspergillus flavus and aspergillus ochraceous, respectively. Some of the tested compounds showed significant antimicrobial activity. IR, 1H NMR, mass spectral data, and elemental analysis elucidated the structures of all the newly synthesized compounds.

β-Oxoanilide 1 reacted with acetyl isothiocyanate and ethoxycarbonyl isothiocyanate to givepyridine derivatives 6a,b and pyrimidinethiol 8 respectively. While with arylidine malononitrile gave the pyran derivative 12. Similarly, treatment of 1 with arylidine cyanoacetamide or arylidine cyanothioacetamide afforded the pyridine derivatives 13a,b, 14a,b respectively. Condensation of 1 with aromatic aldehyde obtained the cyclohexenones 19a-c. The reaction of 1 with a mixture of aromatic aldehyde and urea or thiourea gave the pyrimidine derivatives 23a,b. Treatment of compound 1 with arylidine acetophenone yield the cyclohexene derivatives 26a,b. Reaction of 1 with a mixture of ethyl cyanoacetate and sulfur yield the thiophene derivative 27. Which was reacted with formamide, potassium thiocyanate and hydrazine to afford the thienopyrimidines 28, 29 and the hydrazide derivative 30. respectively.

Condensation of 1,3-diphenylpyrazole-4-carboxaldehyde (1) with some cyclic and heterocyclic active methylene derivatives afforded the condensation products 2-5. The reaction of 1 with benzoylglycine afforded the key intermediate 4-[(1,3-diphenyl-1H-pyrazol-4-yl)methylene]-2-phenyl-1,3-oxazol-5(4H)-one (6). Also, 1 reacted with malononitrile to give 7. The later reacted with 1H-indene-1,3(2H)-dione to give 9. The oxazolone 6 reacted with some aromatic and heteroaromatic amine derivatives to yield 5-[(1H-pyrazol-4-yl)methylene]-3,5-dihydro-4H-imidazol-4-one derivatives 11a,b, 12, 13 and 15. Reacting the oxazolone 6 with acetylacetone, ethyl acetoacetate, 5,5-dimethylcyclohexane-1,3-dione and 1H-indane-1,3-(2H)-dionegave the 1H-pyrazol-4-ylmethylenepyrrolidine-2,4-dione, 1H-pyrazol-4-ylmethylenepyrrol-3-one, 1H-pyrazol-4-ylmethyleneindole-3,4-dione and 1H-pyrazol-4-ylmethyleneindeno[1,2-b]pyrrole-3,4-dione derivatives 18-21 respectively. Antibacterial activity of some of the newly synthesized compounds was studded.

Cyclocondensation of cyanothioformamides (1) with arylhydrazonomalononitriles (2) afforded the novel imidazole derivatives (4a–e) in good yields. Isothiocyanatoazobenzene (6) was allowed to react with potassium cyanide and gave the new cyanothioformamide (7) which was reacted with 4-chlorophenyl isocyanate to yield imidazolidinethione (8). Compound (8) was subjected to react with hydrochloric acid, o-phenylenediamine, 4-methylaniline, and hydrogen sulfide and furnished compounds (10), (11), (12), and (15), respectively. Also, the reactivity of thiohydantoin (15) toward some electrophilic reagents such as N,N-dimethylformamide-dimethylacetal and arylidene-malononitriles was investigated. The structure of the synthesized compounds was established by analytical and spectral data. © 2005 Wiley Periodicals, Inc. Heteroatom Chem 16:218–225, 2005; Published online in Wiley InterScience (www.interscience.wiley.com). DOI 10.1002/hc.20113