Using the Density Functional Theory (DFT) level by means of 3-21G, 6-31G and 6-31+G (d) basissets, the structural optimization of isolated Pyrazole and Pyrazoline was done in the gas phase. Then,the calculation about the solvent effect on the stability energies of Pyrazole and Pyrazoline wasperformed for the ten solvents using PCM model method at B3LYP/6-31+G(d) and then the dielectriceffects o...

Although cannabinoids are efficacious in laboratory animal models of inflammatory pain, their established cannabimimetic actions diminish enthusiasm for their therapeutic development. Conversely, fatty acid amide hydrolase (FAAH), the chief catabolic enzyme regulating the endogenous cannabinoid N-arachidonoylethanolamine (anandamide), has emerged as an attractive target for treating pain and ot...

We have previously shown that the endocannabinoid anandamide and its metabolically stable analog (R)-methanandamide produce vasorelaxation in rabbit aortic ring preparations in an endothelium-dependent manner that could not be mimicked by other CB(1) cannabinoid receptor agonists (Am J Physiol 282: H2046-H2054, 2002). Here, we show that (R)-methanandamide and abnormal cannabidiol stimulated nit...

Herein, we report a new method of synthesis N-acylureas (E1–5) via reaction dibenzoylhydrazine carboxamide (N,2-bis(4-methoxybenzoyl)hydrazine-1-carboxamide) (C) and various benzylamines. Preparation was performed by the treatment 5,6-diaryl-3-methylthio-1,2,4-triazine (B) with Oxone which leads to oxidation triazine ring cleavage in high yield (82%). Five benzylamine derivatives containing dif...

The title compound, C(23)H(19)N(3)O(2), was synthesized by the 1,3-dipolar cyclo-addition reaction of N-phenyl-α-diazo-acetamide and chalcone. In the mol-ecule, the pyrazoline ring assumes an envelope conformation. Weak inter-molecular C-H⋯O hydrogen bonding is present in the crystal structure.

In the title compound, C(23)H(17)Cl(3)N(4)O, the benzene rings are oriented with respect to the pyrazole ring at dihedral angles of 39.9 (2) and 72.90 (13)° for the chloro-phenyl and di-chloro-phenyl rings, respectively. Inter-molecular C-H⋯N and C-H⋯Cl inter-actions are observed in the crystal packing.

The asymmetric unit of the title compound C25H19N5OS, contains two mol-ecules, A and B. In mol-ecule A, the dihedral angles between the pyrazole ring and the C-bound phenyl group, the N-bound phenyl group and the thia-diazole ring are 32.30 (14), 52.25 (14) and 34.94 (12)°, respectively. The corresponding angles in mol-ecule B are 33.32 (14), 50.67 (15), and 70.30 (12)°, respectively. In the cr...

Abstract Pyrazolo[3,4-b]pyridine is a privileged scaffold found in many small drug molecules that possess wide range of pharmacological properties. Efforts to further develop and exploit synthetic methodologies permit the functionalization this heterocyclic moiety warrant investigation. To end, series novel 1,3-disubstituted pyrazolo[3,4-b]pyridine-3-carboxamide derivatives have been prepared b...