RESUMEN
BACKGROUND: During the COVID-19 pandemic, the care of hip fracture patients remains a clinical priority. To date, there is limited empirical knowledge about the impact of pandemic on the care of patients surgically treated for hip fracture, affected or not by COVID-19. OBJECTIVE: To investigate the effects of the COVID-19 pandemic on the nursing-sensitive and rehabilitation outcomes of frail patients undergoing hip fracture surgery. METHODS: A retrospective cohort study was conducted in an Italian Orthopaedic Research Institute. All patients aged ≥ 65 years admitted with fragility hip fractures between 1st March and 30th June in 2019 (group PP: pre-pandemic) and in the same period in 2020 (group P: pandemic), were compared. In the P group, COVID-19 positive patients were excluded due to the presence of a specific treatment pathway. Data on patient demographics and baseline characteristics, and peri-operative care factors were obtained from the Institute's computer-based patient-record system. The primary outcome was the incidence of any stage hospital-acquired pressure ulcers (PUs). The secondary outcome was time to first static verticalization and to first ambulation. RESULTS: Three-hundred and sixty patients were included in the study, which comprised 108 patients in PP group and 252 patients in P group. Overall PUs incidence was significantly higher in the P-group (21.8%) than in the PP-group (10.2%) (p = 0.009). Specifically, the incidence of sacral PUs was significantly lower in P-group (38.1%) vs PP-group (91%) (p = 0.004); on the contrary, the incidence of PUs localized to the heels or other body sites were significantly higher in P-group (30.9% and 30.9%, respectively) vs PP-group (0% and 9%, respectively) (p = 0.004). No significant between groups differences were found for all the secondary outcomes. CONCLUSION: In the pandemic period, nursing and rehabilitation care provided to patients with fragility hip fracture maintained high standards comparable to the pre-pandemic period. The increase in PUs incidence in the pandemic period was probably due to the older age of the patients admitted to hospital. The qualitative evaluation of the care administered and the emotional impact of the pandemic on the patients are very interesting topic which would deserve further investigation.
RESUMEN
Several new ethyl 1-methyl-5-(substituted 3,4-dihydro-4-oxoquinazolin-3-yl)-1H-pyrazole-4-acetates 2, substituted at 2 and, alternatively at, 6, 7 or 8 positions of the quinazolinone nucleus, were synthesised. The compounds were screened for their analgesic and antiinflammatory activities, acute toxicity and ulcerogenic effect. Substitution in the benzene moiety of the quinazolinone ring did not show any advantage for the analgesic activity, whereas it improved in some cases the antiinflammatory activity. Some compounds showed appreciable antiinflammatory activity and, at the same time, very low ulcerogenic index.
Asunto(s)
Pirazoles/síntesis química , Pirazoles/farmacología , Quinazolinas/síntesis química , Quinazolinas/farmacología , Analgésicos/síntesis química , Analgésicos/farmacología , Analgésicos/toxicidad , Animales , Antiinflamatorios/síntesis química , Antiinflamatorios/farmacología , Antiinflamatorios/toxicidad , Benzoquinonas/farmacología , Edema/inducido químicamente , Dosificación Letal Mediana , Espectroscopía de Resonancia Magnética , Masculino , Ratones , Peritonitis , Pirazoles/toxicidad , Quinazolinas/toxicidad , Ratas , Ratas Sprague-Dawley , Espectrofotometría Infrarroja , Úlcera Gástrica/inducido químicamenteRESUMEN
Seven pyrazolone and pyrazolidone derivates, some of them widely used as analgesic and anti-inflammatory drugs, were tested for the inhibitory property of the 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol. The data obtained clearly show that, among pyrazolone and pyrazolidone derivates, the correlation between IC50 and therapeutic potency is not always verified.
Asunto(s)
Antiinflamatorios no Esteroideos/farmacología , Citosol/metabolismo , Hidrocortisona/análogos & derivados , Hígado/metabolismo , Pirazoles/farmacología , 3-Hidroxiesteroide Deshidrogenasas/antagonistas & inhibidores , 3-alfa-Hidroxiesteroide Deshidrogenasa (B-Específica) , Animales , Citosol/efectos de los fármacos , Citosol/enzimología , Hidrocortisona/metabolismo , Técnicas In Vitro , Hígado/efectos de los fármacos , Hígado/enzimología , RatasRESUMEN
Some carboxylic acids of N(3)-pyrazole substituted 1,2,3-benzotriazin-4-(3H)-ones and- quinazolin-4-(3H)-ones were prepared and tested for the inhibitory property of 3 alpha-hydroxysteroid dehydrogenase of rat liver cytosol. The results indicated that the degree of inhibition can be used to predict the antiinflammatory potency of the compounds described.
Asunto(s)
3-Hidroxiesteroide Deshidrogenasas/antagonistas & inhibidores , Antiinflamatorios no Esteroideos/síntesis química , 3-alfa-Hidroxiesteroide Deshidrogenasa (B-Específica) , Animales , Antiinflamatorios no Esteroideos/farmacología , Ratas , Relación Estructura-ActividadRESUMEN
Some N-(pyrazol-5-yl)-2-nitrobenzamides, variably substituted in the pyrazole nucleus as well as in the amidic group, were reacted in acetic acid media with potassium nitrite and hydrochloric acid. The different chemical behaviour of the reacted pyrazole derivatives in relation to the substitution pattern in both the pyrazole nucleus and the amidic group, was observed. All compounds isolated from the reaction mixtures (4-nitroso, 4-nitro, 4-diazo and 4-chloro derivatives) were evaluated by the agar diffusion method for their "in vitro" growth inhibitory activity against Candida albicans (our collection), Candida tropicalis ATCC 13803, Saccharomyces cerevisiae ATCC 36375, Escherichia coli ATCC 25922, Staphylococcus aureus ATCC 25923 and Pseudomonas aeruginosa ATCC 27853. The 1-methylpyrazole derivatives showed larger inhibition zones than the 1-phenyl ones in the antimicrobial tests.
Asunto(s)
Antiinfecciosos/síntesis química , Compuestos de Diazonio/síntesis química , Compuestos Nitrosos/síntesis química , Pirazoles/síntesis química , Antibacterianos , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Compuestos de Diazonio/farmacología , Hongos/efectos de los fármacos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Compuestos Nitrosos/farmacologíaRESUMEN
Several new 4-diazopyrazole derivatives were synthesized by reaction of 1-(R-substituted)phenyl-3-methyl-5-benzamidopyrazoles with a sevenfold excess of nitrous acid in acetic media. The compounds were tested at 20 microM concentration for their antineoplastic activity in vitro against Raji (human Burkitt lymphoma), K562 (human chronic myelogenous leukemia) and U937 (human histiocytic lymphoma) cell lines. They showed a percent of growth inhibition in the range 23.4-100%.
Asunto(s)
Antineoplásicos/síntesis química , Pirazoles/síntesis química , Antineoplásicos/farmacología , Fenómenos Químicos , Química Física , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Pirazoles/farmacología , Células Tumorales CultivadasRESUMEN
The analgesic and antiinflammatory activities of some N,N'-bis(2-hydroxybenzoyl)-diaminoalkanes 3 a-l were studied. The compounds were prepared very conveniently by fusion of phenyl salicylate 2 and diaminoalkanes 1 a-l. The pharmacological activities were influenced by the number of carbon atoms in the polimethylenic chain. Some derivatives were more effective and less gastrolesive than salicylamide.
Asunto(s)
Analgésicos/síntesis química , Antiinflamatorios no Esteroideos/síntesis química , Diaminas/síntesis química , Hidroxibenzoatos/síntesis química , Animales , Conducta Animal/efectos de los fármacos , Fenómenos Químicos , Química , Diaminas/farmacología , Diaminas/toxicidad , Hidroxibenzoatos/farmacología , Hidroxibenzoatos/toxicidad , Dosificación Letal Mediana , Masculino , Ratones , Ratas , Ratas Endogámicas , Úlcera Gástrica/inducido químicamenteRESUMEN
Following our research on analgesic and antiinflammatory active compounds containing the pyrazole nucleus, a number of 3-(pyrazol-5-yl)-1,2,3-benzotriazin-4(3H)-ones and quinazolin-4(3H)-ones was synthetized and tested. The results of tests for analgesic, antiexudative and antioedema activities, as well as for induction of lesion in the gastric mucosa, are reported and discussed.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Pirazoles/síntesis química , Quinazolinas/síntesis química , Triazinas/síntesis química , Animales , Antiinflamatorios no Esteroideos/toxicidad , Conducta Animal/efectos de los fármacos , Fenómenos Químicos , Química , Exudados y Transudados/efectos de los fármacos , Dosificación Letal Mediana , Masculino , Ratones , Pirazoles/farmacología , Pirazoles/toxicidad , Quinazolinas/farmacología , Quinazolinas/toxicidad , Ratas , Ratas Endogámicas , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/fisiopatología , Relación Estructura-Actividad , Triazinas/farmacología , Triazinas/toxicidadRESUMEN
A number of new 3-(isoxazol-5-yl)-quinazolin-4(3H)-ones was prepared and tested, together a few analogues previously obtained, for their analgesic, antipyretic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effects. In the carrageenan rat foot edema model one of the tested compounds showed activity and LD50 comparable to that of ASA, but the ulceration index approximated zero value.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Isoxazoles/síntesis química , Quinazolinas/síntesis química , Animales , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/toxicidad , Conducta Animal/efectos de los fármacos , Isoxazoles/farmacología , Isoxazoles/toxicidad , Masculino , Ratones , Quinazolinas/farmacología , Quinazolinas/toxicidad , Ratas , Ratas Sprague-Dawley , Úlcera Gástrica/inducido químicamente , Úlcera Gástrica/patologíaRESUMEN
Some N-heterocyclic salicylamide derivatives were prepared by fusion of phenyl salicylate and heterocyclic amines, whereas other ones were synthesized by ring closure using N-salicyloyl-N'-anthranylhydrazine as starting material. All the compounds were tested for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effects, in order to ascertain if the N-substitution would offer any advantages. Some derivatives were more effective than salicylamide and ulcerogenic activity was variably lowered.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Salicilamidas/síntesis química , Animales , Antiinflamatorios no Esteroideos/toxicidad , Conducta Animal/efectos de los fármacos , Carragenina , Fenómenos Químicos , Química , Edema/inducido químicamente , Edema/tratamiento farmacológico , Exudados y Transudados/efectos de los fármacos , Dosificación Letal Mediana , Masculino , Ratones , Ratas , Ratas Endogámicas , Tiempo de Reacción/efectos de los fármacos , Salicilamidas/farmacología , Salicilamidas/toxicidad , Úlcera Gástrica/inducido químicamenteRESUMEN
Following our research on analgesic and antiinflammatory active compounds containing the pyrazole nucleus, a number of new 1-methyl- or 1-phenyl-6-(2-substitutedphenyl)-pyrazolo[3,4-d]-1,3-oxazin- 4(1H)-ones was synthesized and tested, together with a few analogues previously obtained, for their analgesic and antiinflammatory activities, as well as for their acute toxicity and ulcerogenic effects. One of the tested compounds showed activity comparable to that of phenylbutazone and, at the same time, higher LD50 and a very low ulceration index.
Asunto(s)
Antiinflamatorios no Esteroideos/síntesis química , Oxazinas/síntesis química , Pirazoles/síntesis química , Analgésicos/farmacología , Analgésicos/toxicidad , Animales , Antiinflamatorios no Esteroideos/farmacología , Antiinflamatorios no Esteroideos/toxicidad , Conducta Animal/efectos de los fármacos , Dosificación Letal Mediana , Masculino , Ratones , Oxazinas/farmacología , Pirazoles/farmacología , Úlcera Gástrica/inducido químicamenteRESUMEN
N-Isoxazolyl-2-iodobenzamides 3 and 9, with a benodanil-like structure, were synthesized by refluxing in acetic acid the corresponding benzotriazinones 2 and 8 with potassium iodide for 1 h with the aim to ascertain if they were active as fungicides against Phytophthora citricola Saw., Botrytis cinerea Pers., Rhizoctonia sp. and Alternaria sp. Among the tested iodo derivatives, compounds 3b and 9a possess interesting activities against the aforesaid fungal strains in several cases similar to that of benodanil I taken as reference drug.
Asunto(s)
Benzamidas/síntesis química , Fungicidas Industriales/síntesis química , Isoxazoles/síntesis química , Benzamidas/farmacología , Fenómenos Químicos , Química Física , Recuento de Colonia Microbiana , Hongos/efectos de los fármacos , Fungicidas Industriales/farmacología , Isoxazoles/farmacología , Espectroscopía de Resonancia Magnética , Espectrofotometría InfrarrojaRESUMEN
Several new 1-methyl-5-[substituted-4-oxo-1,2,3-benzotriazin-3-yl] -1H-pyrazole-4-acetic acids and their ethyl ester derivatives were prepared. The compounds were tested for analgesic and antiinflammatory activities, acute toxicity, ulcerogenic effect, and as in vitro inhibitors of 3 alpha-hydroxysteroid dehydrogenase (3 alpha-HSD), since it is claimed that the inhibition of such an enzyme predicts in vivo antiinflammatory activity. Some compounds were more active than phenylbutazone in the phenylbenzoquinone and acetic acid peritonitis tests, and equiactive to the same drug in the carrageenin paw edema test. All the compounds inhibited the 3 alpha-HSD, but no correlation was observed with the paw edema inhibition values. The compounds proved to possess marginal or no ulcerogenic effect, as well as low systemic toxicity.
Asunto(s)
3-Hidroxiesteroide Deshidrogenasas/antagonistas & inhibidores , Analgésicos/síntesis química , Antiinflamatorios/síntesis química , Inhibidores Enzimáticos/síntesis química , Pirazoles/síntesis química , 3-alfa-Hidroxiesteroide Deshidrogenasa (B-Específica) , Analgésicos/farmacología , Animales , Antiinflamatorios/farmacología , Inhibidores Enzimáticos/farmacología , Masculino , Ratones , Pirazoles/farmacología , RatasRESUMEN
A novel series of 3-(3-phenyl-isoxazol-5-yl) or 3-[(3-phenyl-isoxazol-5-yl)amino] substituted 4(3H)-quinazolinone derivatives was synthesized. The compounds were tested for their antineoplastic activity in vitro against Raji (human Burkitt limphoma). K-562 (human chronic myelogeneous leukemia) and U937 (human histiocytic limphoma) cell lines. The most active quinazolinones showed IC50 values in the range 16-30 microM.
Asunto(s)
Antineoplásicos/síntesis química , Isoxazoles/síntesis química , Quinazolinas/síntesis química , Antineoplásicos/química , Antineoplásicos/farmacología , Ensayos de Selección de Medicamentos Antitumorales , Humanos , Concentración 50 Inhibidora , Isoxazoles/química , Isoxazoles/farmacología , Espectroscopía de Resonancia Magnética , Quinazolinas/química , Quinazolinas/farmacología , Espectrofotometría Infrarroja , Células Tumorales CultivadasRESUMEN
New N-(5-methylisoxazol-3-yl)-2 or 3 or 4-(phenoxyacetamido)benzamides 6a-t were synthesized and tested for their in vitro antimicrobial activity against gram positive (Staphylococcus aureus ATCC 25923) and gram negative (Escherichia coli ATCC 25922 and Pseudomonas aeruginosa ATCC 27853) bacteria as well as fungi (Candida albicans ATCC 10231, Candida tropicalis ATCC 13803 and Cryptococcus neoformans ATCC 90112). Compounds 6 were devoid of antibacterial as well as antifungal activities at maximum tested concentrations of 50 micrograms/ml for bacteria and 100 micrograms/ml for yeast.
Asunto(s)
Acetamidas/síntesis química , Antiinfecciosos/síntesis química , Antiinfecciosos/farmacología , Bacterias/efectos de los fármacos , Hongos/efectos de los fármacos , Éteres Fenílicos/síntesis química , Acetamidas/farmacología , Antibacterianos , Bacterias Gramnegativas/efectos de los fármacos , Bacterias Grampositivas/efectos de los fármacos , Indicadores y Reactivos , Espectroscopía de Resonancia Magnética , Pruebas de Sensibilidad Microbiana , Éteres Fenílicos/farmacologíaRESUMEN
A series of isochromeno[4,3-c]pyrazole-5(1H)-one derivatives 7b-h were prepared and tested at 10 µM for their ability to displace specific [(3)H]flunitrazepam from bovine brain membranes. The substitution pattern of the above derivatives was shown to influence the receptor affinity. The most active compound of the series was 7e, showing a 54% inhibition of [(3)H]flunitrazepam binding. Compounds 7a-d,i were compared with the known isomers chromeno[4,3-c]pyrazole-4(1H)-ones 14a-d,i, showing that the isochromene/chromene isomerism influences the activity.
Asunto(s)
Benzopiranos/síntesis química , Benzopiranos/metabolismo , Simulación del Acoplamiento Molecular , Pirazoles/síntesis química , Pirazoles/metabolismo , Receptores de GABA-A/metabolismo , Animales , Benzopiranos/química , Bovinos , Técnicas de Química Sintética , Humanos , Unión Proteica , Conformación Proteica , Pirazoles/química , Receptores de GABA-A/químicaRESUMEN
Values of the ionization constant of acetic acid in H(2)O and D(2)O (K(HAc) and K(DAc)) and the deuterium isotope effect, ΔpK = pK(DAc) - pK(HAc), have been determined from T = 368 K to T = 548 K at p = 20 MPa, using a flow-through ac conductance cell built at the University of Delaware. Measurements were made on dilute (ionic strength â¼ 10(-4) mol·kg(-1)) solutions of acetic acid, sodium acetate, hydrochloric acid, and sodium chloride in H(2)O and D(2)O, injected in sequence at each temperature and pressure, so that systematic errors in the measured conductance of each solution would cancel. Experimental values for the molar conductivity, Λ, of the strong electrolytes were used to calculate the molar conductivity at infinite dilution, Λ°, using the Fuoss-Hsia-Fernández-Prini (FHFP) equation. These were used to calculate the molar conductivity at infinite dilution for acetic acid which was in turn used to calculate the degree of dissociation and finally the ionization constants of acetic acid. This same procedure was done for the pertinent deuterated solutes in D(2)O. Measured values of log K(HAc), log K(DAc), and ΔpK were obtained to a precision of ±0.008. The present results are in agreement with the only other accurate study at high temperatures and pressures (Mesmer, R. E.; Herting, D. L. J. Solution Chem.1978, 7, 901-913). The deuterium isotope effects, ΔpK, become independent of temperature above â¼420 K, at a value approximately 0.1 unit lower than that at 298 K. These values are ΔpK = 0.43 ± 0.01 and ΔpK = 0.51 ± 0.01, respectively. The temperature dependence of the Walden product ratio, (λ°Î·)(D(2)O)/(λ°Î·)(H(2)O), indicates a change in the relative hydration behavior of ions, whereby the effective Stokes radii of the sodium, chloride, and acetate ions in D(2)O relative to H(2)O reverse above â¼423 K. The results also suggest that the greater efficiency of the well-established proton-hopping transport mechanisms for OH(-) and H(3)O(+) at 298 K, relative to OD(-) and D(3)O(+), is significantly reduced as the temperature increases toward 548 K.