Novel conformationally restricted analogues of agomelatine were synthesized and pharmacologically evaluated at MT₁ and MT₂ melatoninergic receptors. Replacement of the N-acetyl side chain of agomelatine by oxathiadiazole-2-oxide (compound 3), oxadiazole-5(4H)-one (compound 4), tetrazole (compound 5), oxazolidinone (compound 7a), pyrrolidinone (compound 7b), imidazolidinedione (compound 12), thi...

the imine intermediate generated by the addition of primary amine to the cinnamaldehyde is trapped by the n-isocyaniminotriphenylphosphorane (ph3pnnc) and a carboxylic acid, and leads to the formation of the corresponding iminophosphorane intermediate. the 1,3,4-oxadiazole derivatives are formed via intramolecular aza-wittig reaction of the iminophosphorane intermediate. the reactions were comp...

Three new types of terminally connected ABA-heterotrimesogens and heterodimesogens, composed of a bent 3,5-diphenyl-1,2,4-oxadiazole central unit and one or two rod-shaped 4-cyanobiphenyl cores or one 2-phenyl-1,3,4-thiadiazole core, connected by flexible spacers, have been synthesized, and their mesomorphic behavior was studied by optical polarizing microscopy (PM), differential scanning calor...

1,3,4-oxadiazole derivatives constitute a group of biologically important compounds that have been used as analgesic, anti-inflammatory, antibacterial, antifungal, antispasmodic, or psychotropic drugs in addition to their role plant growth regulation and monoamine oxidase inhibition. This study focused on the use microwaves synthesis oxadiazole containing thiazolidinediones, which are promising...

Tert-butyl carbazate (1) reacted with ammonium thiocyanate and phenyl isothiocyanate to afford the corresponding 5-tert-butoxy-4H-1, 2, 4-triazole-3-thiol (3) 5-tert-butoxy-4-phenyl-2H1, 2, 4-triazole-3(4H)-thione 5 respectively. Compound (1) also reacted with carbon disulfide and potassium hydroxide to afford 5-tert-butoxy-1, 3, 4-oxadiazole-2(3H)-thione 6. Treatment of 6 with methyl iodide, 2...

IN THE TITLE SYDNONE COMPOUND [SYSTEMATIC NAME: 3-(4-meth-oxy-phen-yl)-1,2,3-oxadiazol-3-ium-5-olate], C(9)H(8)N(2)O(3), the essentially planar oxadiazole ring [maximum deviation = 0.005 (1) Å] is inclined at a dihedral angle of 30.32 (8)° with respect to the benzene ring. In the crystal, adjacent mol-ecules are inter-connected by inter-molecular C-H⋯O hydrogen bonds into sheets lying parallel ...

Proxazole or 3-α-phenylpropyl-5-β-diethylaminoethyl-1, 2 4-oxadiazole citrate, is an unusual drug because it possesses both anti-inflammatory and antispasmodic proper ties (1) and because each of these two properties has some uncommon features. The anti inflammatory action takes place mostly against edematous responses and is devoid of ul cerogenic effects which are instead produced ...

A series of biaxial V-shaped, shape-persistent molecules has been synthesised by stepwise coupling of phenylene ethynylene arms to an oxadiazole bending unit. Studies of their thermotropic nematic phases point to phase biaxiality.