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New 3-(2,3-dimethyl-1-phenyl-4-pyrazolon-5-yl)-4-thiazolidones were synthesized. The structure of substances was supported by UV- and 1H-NMR spectra. Some compounds were tested in vivo for their antiinflammatory activity. Were confirmed previous results about structure-activity relationships.
Naproxen, probenecid, diclofenac, ibuprofen and indomethacin were converted to hydrazide derivatives via their methyl ester by reacting with hydrazine hydrate, which were further condensed with beta-keto esters to get the pyrazolone derivatives. The hydrazide derivatives of probenecid and diclofenac were also reacted with biphenyl acetic acid while naproxen hydrazide was reacted with p-chloro benzoic acid besides biphenyl acetic acid to synthesize their oxadiazole analogues. Some selected members of the compounds prepared were screened for their anti-inflammatory and analgesic activity.
The binary and ternary Eu(III) complexes have been prepared with four 1,3-diphenyl-4-acyl-5-pyazolones as ligands (where the four acyls are benzoyl, phenylacetyl, butyryl and choroacetyl, and the compounds are represented by DPBZP, DPPAP, DPBTP, DPCAP respectively). The composition of the complexes was determined by chemical and elementary analysis, and the structure of the complexes was characterized by FTIR spectra. The fluorescence spectra of the complexes were measured. It is indicated that the complexes emit with the characteristic fluorescence of Eu(III), the fluorescence intensity of the complexes are closely related to the substituents at the acyl at 4-position in pyrazolone ring of the ligands, depending on the ligands, the descending order of the fluorescence intensity is DPBZP > DPPAP > DPBTP > DPCAP, and that the second ligand, 1, 10-phenanthroline, remarkably intensifies the fluorescence of the complexes.
The synthesis of eight new 1-(R-pyridazinil)-3-methyl-4-(R-phenylazo)-5-pyrazolone, the structure of which was confirmed by the results of the physicochemical analysis, is presented. The preliminary tests for determining their biological action have revealed a moderate antimicrobial activity.
The results of a systematic examination of the spectra of 15 drug substances with chromophores and auxochromes in monocyclic (pyrazolone, pyrazolidin, pyridazine, pyrimidine and pyrazine) and bicyclic compounds (benzoxazol, imidazole, benzthiazole and indene) in the UV and visible range were evaluated. Influences of substituents and solvents on shifts of the E, K, B and R bands were discussed.
Even today, pyrazolone drugs still play an essential role in outpatient pain treatment. Their applications and limitations are discussed from the point of view of the general practitioner treating outpatients.
The pyrazolone derivatives aminophenazone, phenazone, and propyphenazone known as inducers are capable of inhibiting initially monooxygenase-dependent biotransformation steps. In the dose of 1.5 mmol X kg-1 they prolong the hexobarbital narcosis (max. 1 h after administration) due to a reduced hexobarbital metabolism in the liver. An influence on the N-demethylation (aminophenazone as substrate) ist not substantial. The catalytic binding site of cytochrome P-450 is not influenced. In aminophenazone- and phenazone-treated animals the inhibitory phase is followed by a stimulatory one. After the repeated administration the inhibitory phase continues up to the third measured 1 h after administration. The initially inhibitory effect of inducers seems to be caused by a mutual interference of a complete or partial binding to various forms of cytochrome P-450. However, effects on the CNS cannot be excluded.
Female pregnant rats of 2BAW strain were divided in 2 groups: the 1st, received 50 mg/kg corporal weight of sodium 1-phenyl-2,3-dimethyl-5-pyrazolon-4-methylamino-methane sulfonate (Dipyrone), single dose daily, by i.p. injections, from 16th to 20th day of pregnancy; the 2nd, received 0,5 ml of distilled water, single dose daily, by i.p. injections, during the same period. All the animals were sacrificed 2 hours after the last injection. The biochemical results of nucleic acids in the placentas and fetal livers, and the caryometric data of trophoblastic giant cells and fetal hepatocytes, demonstrated that: 1. When compared the 2 groups, as much the nucleic acids levels (RNA and DNA) of placentas as the nuclear size of trophoblastic giant cells, do not presented statistical differences; 2. The biochemical levels of nucleic acids (RNA and DNA) of fetal livers decreased, while the nuclear size of hepatocytes increased in the experimental group, with reference to control group.
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The dissociation constants of 4-(4-chlorophenylazo)-3-methyl-1-[2-hydroxy-3-morphilinopropane-1-yl]-2-pyrazolin-5-one (CAMP) has been determined potentiometrically in 0.1 M KCl and 40% (v/v) ethanol-water mixture. The stepwise stability constants of the formed complexes of Mn2+, Co2+, Ni2+, Cu2+, Zn2+, La3+, Ce3+ and UO(2)2+, with CAMP have been determined. The stability of the formed complexes were found as follows: UO(2)2+ > Ce3+ > La3+ > Mn2+ < Co2+ < Ni2+ < Cu+ > Zn2+. The thermodynamic parameters (deltaG, deltaH and deltaS) for CAMP and its complexes were evaluated and discussed. The dissociation process is non-spontaneous, endothermic and entropically unfavourable. The formation of the complexes have been found to be spontaneous, exothermic or endothermic (depending on the metal) and entropically favourable. The stoichiometries of these complexes were determined spectrophotometrically and conductometrically and indicated the formation of 1:1 and 1:2 (metal:ligand) complexes.
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