With an intention to synergize the antimicrobial activity of 1,3-diphenyl pyrazole and chromene derivatives, 20 hybrid compounds were synthesized and evaluated for their antimicrobial activity. Structures of the newly synthesized compounds were established by elemental analysis and spectral data. All compounds were evaluated for their antimicrobial activity against Gram positive and Gram negative bacteria and antifungal activity by a well diffusion method. Compounds

A series of 2-thienyl substituted derivatives of thiazoles, oxazoles and spiro(indole-azole) were synthesized. The structures of the synthesized compounds were confirmed by IR, NMR and mass spectral data.

A new series of benzazole, thiazolidinone and azetidin-2-one derivatives incorporating to pyrazole moiety were synthesized by condensation of 1,3-diphenyl-1H-pyrazol-4-carboxaldehyde with different nucleophiles. The structures of the newly synthesized compounds were confirmed by analytical and spectral methods. Some of these compounds were evaluated for their antihyperglycemic and renoprotective activities. Three compounds showed remarkable anti-diabetic potency, whereas other five compounds showed significant renoprotective activity.

A novel series of pyrazoline and thiazole derivatives incorporating 2-pyrazolin-5-one moiety were synthesized starting from α,β-unsaturated ketones under the effect of hydrazine derivatives and thiosemicarbazide. The obtained pyrazolines 4a,b were treated with different reagents to afford N-substituted pyrazolines 5a,b-8a,b. N-Thiocarbamoyl pyrazolines 12a,b were cyclized using phenacyl bromide, 2,3-dichloroquinoxaline, and monochloroacetic acid afforded the novel pyrazolinyl thiazoles 13a,b-16a-f. The newly synthesized compounds were characterized by analytical and spectral data.J. Heterocyclic Chem., 00, 00 (2014).© 2014 HeteroCorporation pyrazolines 3a,b were formed. The presence of N-acetyl group was established using IR and 1 H-NMR spectra. While condensing 1a,b with hydrazine hydrate in ethanol, 3-(3methyl-5-oxo-1-phenyl-2-pyrazolin-4-yl)-5-aryl-2-pyrazolines 4a,b were obtained. The reaction includes formation of hydrazones intermediate and then addition of NH 2 of hydrazones to the double bond. Upon acetylation of the pyrazolines 4a,b by acetic acid, N-acetyl pyrazolines 3a,b were obtained. Moreover, the aforementioned pyrazoline derivatives 4a,b were converted into the corresponding substituted N-pyrazolines 5a,b-8a,b through their reaction with various reagents such as chloroacetyl chloride, phenyl isothiocyanate, benzenesulfonyl chloride, and benzoyl chloride, respectively.The structures of products 5a,b-8a,b were evidenced by their spectra (IR, 1 H-NMR, 13 C-NMR, and MS) and elemental analyses (see Experimental section and Table 1).N-phenyl pyrazolines 9a,b were obtained upon condensing with phenyl hydrazine in hot ethanol. The presence of N-phenyl group in 9a or 9b was elucidated from spectral data and EIMS, which is in agreement with their molecular weights. The isooxazoline derivatives 10a,b were obtained through condensation of 1a,b with hydroxyl amine in hot ethanol containing anhydrous sodium acetate. The spectroscopic data and elemental analysis were constituent with the structures of compounds 10a,b.On the other hand, binucleophile compound like ophenylenediamine was condensed with 1a,b in ethanol Scheme 1. Reagents: (i) NH 2 NH 2 .H 2 O/HCOOH; (ii) NH 2 NH 2 .H 2 O/AcOH; (iii) NH 2 NH 2 .H 2 O/EtOH; (iv) AcOH; (v) ClCH 2 COCl/toluene; (vi) PhNCS/ EtOH; (vii) PhSO 2 Cl/pyridine; (viii) PhCOCl/pyridine; (ix) PhNHNH 2 /EtOH; (x) NH 2 OH.HCl/EtOH, AcONa; (xi) o-phenylenediamine/EtOH.Scheme 2. Reagents: (i) NH 2 CSNHNH 2 /EtOH, NaOH; (ii) PhCOCH 2 Br/EtOH; (iii) 2,3-dichloroquinoxaline/EtOH; (iv) ClCH 2 COOH/AcOH, AcONa;(v) ArCHO/AcOH, AcONa; (vi) ClCH 2 COOH, ArCHO/AcOH, AcONa.Month 2014 2-Pyrazolin-5-One-

Aim and Objective: A series of new 2-pyrazoline analogues were synthesized. The structures of the synthesized compounds were elucidated by the analytical and spectroscopic data. Some selected compounds were screened for the anti-inflammatory activity by using animal model of carrageenan-induced paw edema in mice. Additionally, the analgesic and acute toxicity of these compounds were evaluated and exhibited reasonable results. The anti-oxidant and anti-inflammatory effects of these compounds were established by measuring the contents of malondialdehyde (MDA), reduced glutathione (GSH), nitric oxide (NO), and tumor necrosis factor alpha (TNF-α) in the edema paw tissue. Materials and Methods: All chemicals and reagents used in current study were of analytical grade. Melting points were determined using APP. Digital ST 15 melting point apparatus and are uncorrected. FT-IR spectra were recorded on a Pye-Unicam SP3-100 spectrophotometer in KBr pellet. All 1H and 13C NMR spectra were recorded on AVANCE-III (400 MHz) High Performance FT-NMR Spectrometer Brucker (Switzerland) and some 1H NMR spectra were recorded on Varian EM-360L NMR Spectrophotometer (60 MHz) (USA) in CDCl3 or DMSO-d6 as solvent. Chemical shifts are reported in δ units and the coupling constants (J) are reported in hertz. C, H, N and S analyses were performed with a Vario EL C, H, N, S Analyzer. Carrageenan (product number C1013) was obtained from Sigma-Aldrich (USA). Results: The structures of the compounds were confirmed by IR, 1H NMR, 13C NMR, and elemental analyses. The results of pharmacological activity revealed that compounds 5, 6, 7, and 15 could be recognized as potential multi-potent anti-inflammatory. Conclusion: A simple and suitable method for the synthesis of new pharmacophore was reported. We have designed nineteen heterocycles related to pyrazoline ring, and evaluated eleven of them for their antiinflammatory, analgesic and acute toxicity activities. Compounds 5, 6, 7, and 15 proved to be the interesting compounds, they have high anti-inflammatory activity. However, all the selected compounds show remarkable analgesic activity.