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PubMed2003

Prodrugs and mutual prodrugs: synthesis of some new pyrazolone and oxadiazole analogues of a few non-steroidal anti-inflammatory drugs.

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.

Analgesics↗
PubMed2001

[The fluorescent properites of the complexes of 1,3-diphenyl-4-acyl-5-pyrazolones with Eu(III)].

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.

English Abstract↗
PubMed1988

[UV-spectrophotometry in drug control. 41. Drug substances with chromophores and auxochromes in monocyclic compounds (pyrazolone, pyrazolidine, pyridazine, pyrimidine and pyrazine) and bicyclic compounds (benzoxazole, imidazole, benzthiazole and indene)].

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.

Benzothiazoles↗
PubMed1986

Pyrazolone drugs in outpatient pain treatment.

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.

Acetaminophen↗
PubMed1985

Biphasic effect of pyrazolone derivatives on drug-metabolizing enzyme in rat liver.

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.

Aminopyrine↗
PubMed1978

[Biochemical study of nucleic acids of placenta and fetal liver and caryometric of trophoblastic giant cells and fetal hepatocytes of Rattus norvegicus albinus, during action of sodium 1-phenyl-2, 3-dimethyl-5-pyrazolon-methane sulfonate (Dipyrone) (author's transl)].

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.

Aminopyrine↗
PubMed2004

The development of novel inhibitors of tumor necrosis factor-alpha (TNF-alpha) production based on substituted [5,5]-bicyclic pyrazolones.

Novel substituted [5,5]-bicyclic pyrzazolones are presented as inhibitors of tumor necrosis factor-alpha (TNF-alpha) production. Many of these compounds show low nanomolar activity against lipopolysaccaride (LPS)-induced TNF-alpha production in THP-1 cells. This class of molecules was co-crystallized with mutated p38, and several analogs showed good oral bioavailability in the rat. Oral activity of these compounds in the rat iodoacetate model for osteoarthritis is discussed.

Administration, Oral↗
PubMed2001

Thermodynamics of substituted pyrazolone IX: potentiometric, spectrophotometric and conductometeric studies of 4-(4-chlorophenylazo)-3-methyl-1-[2-hydroxy-3-morphilinopropane 1-yl]-2-pyrazolin-5-one and its metal complexes.

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.

Azo Compounds↗
PubMed2005

Syntheses, structures, and reactivity of new pentamethylcyclopentadienyl-rhodium(III) and -iridium(III) 4-acyl-5-pyrazolonate complexes.

New [CpM(Q)Cl] complexes (M = Rh or Ir, Cp = pentamethylcyclopentadienyl, HQ = 1-phenyl-3-methyl-4R(C=O)-pyrazol-5-one in general, in detail HQ(Me), R = CH(3); HQ(Et), R = CH(2)CH(3); HQ(Piv), R = CH(2)-C(CH(3))(3); HQ(Bn), R = CH(2)-(C(6)H(5)); HQ(S), R = CH-(C(6)H(5))(2)) have been synthesized from the reaction of [CpMCl(2)](2) with the sodium salt, NaQ, of the appropriate HQ proligand. Crystal structure determinations for a representative selection of these [CpM(Q)Cl] compounds show a pseudo-octahedral metal environment with the Q ligand bonded in the O,O'-chelating form. In each case, two enantiomers (S(M)) and (R(M)) arise, differing only in the metal chirality. The reaction of [CpRh(Q(Bn))Cl] with MgCH(3)Br produces only halide exchange with the formation of [CpRh(Q(Bn))Br]. The [CpRh(Q)Cl] complexes react with PPh(3) in dichloromethane yielding the adducts CpRh(Q)Cl/PPh(3) (1:1) which exist in solution in two different isomeric forms. The interaction of [CpRh(Q(Me))Cl] with AgNO(3) in MeCN allows generation of [CpRh(Q(Me))(MeCN)]NO(3).3H(2)O, whereas the reaction of [CpRh(Q(Me))Cl] with AgClO(4) in the same solvent yields both [CpRh(Q(Me))(H(2)O)]ClO(4) and [CpRh(Cl)(H(2)O)(2)]ClO(4); the H(2)O molecules derive from the not-rigorously anhydrous solvents or silver salts.

Iridium↗