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1.
J Enzyme Inhib Med Chem ; 34(1): 1388-1399, 2019 Dec.
Artículo en Inglés | MEDLINE | ID: mdl-31392901

RESUMEN

Fourteen novel dipeptide carboxamide derivatives bearing benzensulphonamoyl propanamide were synthesized and characterized using 1H NMR, 13C NMR, FTIR and MS spectroscopic techniques. In vivo antimalarial and in vitro antimicrobial studies were carried out on these synthesized compounds. Molecular docking, haematological analysis, liver and kidney function tests were also evaluated to assess the effect of the compounds on the organs. At 200 mg/kg body weight, 7i inhibited the multiplication of the parasite by 81.38% on day 12 of post-treatment exposure. This was comparable to the 82.34% reduction with artemisinin. The minimum inhibitory concentration (MIC) in µM ranged from 0.03 to 2.34 with 7h having MIC of 0.03 µM against Plasmodium falciparium. The in vitro antibacterial activity of the compounds against some clinically isolated bacteria strains showed varied activities with some of the new compounds showing better activities against the bacteria and the fungi more than the reference drug ciprofloxacin and fluconazole.


Asunto(s)
Antibacterianos/farmacología , Antifúngicos/farmacología , Antimaláricos/química , Antimaláricos/farmacología , Dipéptidos/química , Dipéptidos/farmacología , Sulfonamidas/farmacología , Animales , Antibacterianos/síntesis química , Antibacterianos/química , Antifúngicos/síntesis química , Antifúngicos/química , Antimaláricos/síntesis química , Bacterias/efectos de los fármacos , Dipéptidos/síntesis química , Hongos/efectos de los fármacos , Ratones , Pruebas de Sensibilidad Microbiana , Pruebas de Sensibilidad Parasitaria , Plasmodium falciparum/efectos de los fármacos , Ratas , Sulfonamidas/química
2.
Eur J Med Chem ; 135: 349-369, 2017 Jul 28.
Artículo en Inglés | MEDLINE | ID: mdl-28460310

RESUMEN

Sulphonamides and carboxamides have shown large number of pharmacological properties against different types of diseases among which is malaria. Twenty four new carboxamide derivatives bearing benzenesulphonamoyl alkanamides were synthesized and investigated for their in silico and in vitro antimalarial and antioxidant properties. The substituted benzenesulphonyl chlorides (1a-c) were treated with various amino acids (2a-h) to obtain the benzenesulphonamoyl alkanamides (3a-x) which were subsequently treated with benzoyl chloride to obtain the N-benzoylated derivatives (5a-f, i-n and q-v). Further reactions of the N-benzoylated derivatives or proline derivatives with 4-aminoacetophenone (6) using boric acid as a catalyst gave the sulphonamide carboxamide derivatives (7a-x) in excellent yields. The in vitro antimalarial studies showed that all synthesized compounds had antimalarial property. Compound 7k, 7c, 7l, 7s, and 7j had mean MIC value of 0.02, 0.03, 0.05, 0.06 and 0.08 µM respectively comparable with chloroquine 0.06 µM. Compound 7c was the most potent antioxidant agent with IC50 value of 0.045 mM comparable with 0.34 mM for ascorbic acid. In addition to the successful synthesis of the target molecules using boric acid catalysis, the compounds were found to have antimalarial and antioxidant activities comparable with known antimalarial and antioxidant drugs. The class of compounds reported herein have the potential of reducing oxidative stress arising from malaria parasite and chemotherapeutic agent used in the treatment of malaria.


Asunto(s)
Antimaláricos/farmacología , Malaria/tratamiento farmacológico , Simulación del Acoplamiento Molecular , Plasmodium falciparum/efectos de los fármacos , Sulfonamidas/farmacología , Antimaláricos/síntesis química , Antimaláricos/química , Relación Dosis-Respuesta a Droga , Estructura Molecular , Pruebas de Sensibilidad Parasitaria , Relación Estructura-Actividad , Sulfonamidas/química
3.
West Afr J Med ; 16(3): 184-90, 1997.
Artículo en Inglés | MEDLINE | ID: mdl-9329289

RESUMEN

The family planning aspects of the practice of traditional healers in Ibadan, a large city in south west Nigeria, was investigated by means of a questionnaire survey of 193 traditional healers. The findings revealed that between 13% and 53% agreed with certain cultural beliefs which tend to increase fertility and that their perceptions of ideal child spacing is most commonly 2-3 years. Only 13% think a couple should have a specified number of children; a large proportion think the number should be "as God wills" (42%) or as many as the couple has resources to cope with (42%). Nearly all think that traditional healers and orthodox health professional should work together in the area of family planning. While most of them recommend traditional methods of contraception (such as beads and herbs) to their clients, up to 22% recommend modern family planning methods such as condoms and oral contraceptive pills. The implications of these findings for family planning programmes and the possibility of the involvement of traditional healers in the promotion of modern family planning methods are discussed.


PIP: The family planning aspects of the practice of traditional healers in Ibadan, a large city in southwest Nigeria, was investigated by means of a questionnaire survey of 193 traditional healers. The findings revealed that between 13% and 53% agreed with certain cultural beliefs that tend to increase fertility and that their perceptions of ideal child spacing is most commonly 2-3 years. Only 13% thought a couple should have a specified number of children; a large proportion thought the number should be "as God wills" (42%) or as many as the couple has resources to support (42%). Nearly all thought that traditional healers and orthodox health professionals should work together in the area of family planning. While most of them recommend traditional methods of contraception (such as beads and herbs) to their clients, up to 22% recommend modern family planning methods such as condoms and oral contraceptives. The implications of these findings for family planning programs and the possibility of the involvement of traditional healers in the promotion of modern family planning methods are discussed.


Asunto(s)
Actitud del Personal de Salud/etnología , Características Culturales , Servicios de Planificación Familiar , Conocimientos, Actitudes y Práctica en Salud , Medicinas Tradicionales Africanas , Adulto , Anciano , Intervalo entre Nacimientos , Servicios de Planificación Familiar/métodos , Femenino , Fertilidad , Humanos , Masculino , Persona de Mediana Edad , Nigeria , Encuestas y Cuestionarios , Salud Urbana
4.
Appl Geogr ; 9(2): 123-33, 1989 Apr.
Artículo en Inglés | MEDLINE | ID: mdl-12282011

RESUMEN

"This paper is concerned with ascertaining the impact of population on the spatial pattern of public service provision in Nigeria.... Using a set of population and revenue variables as explanatory variables, a step-wise multiple regression model was employed to determine the impact of these variables on the provision of selected public services. The results of the analyses show that urban population is generally more important than total population in explaining the spatial pattern of public services. Generally speaking, the revenue variables are even more important in this regard, especially the internal revenue of states.... One implication of these results is that ability to pay, rather than need, is the basis for public service provision in Nigeria. Thus, the richer and more developed states are better off than the less developed ones, irrespective of population size."


Asunto(s)
Demografía , Economía , Renta , Modelos Teóricos , Densidad de Población , Bienestar Social , África , África del Sur del Sahara , África Occidental , Países en Desarrollo , Nigeria , Población , Dinámica Poblacional , Investigación , Factores Socioeconómicos
5.
Soc Sci Med ; 17(9): 591-5, 1983.
Artículo en Inglés | MEDLINE | ID: mdl-6879259

RESUMEN

The frequency of hospital trips among the inhabitants of Nigeria's rural areas is affected by several factors. One obvious factor is the distance between potential patients and hospital facilities. And given the paucity of hospital facilities in rural areas, the distance factor is obviously an important one. However, the main focus of this paper is on the effect of some socio-economic and demographic characteristics on the frequency of hospital trips by rural inhabitants. The location of hospitals in close proximity to the user-population does not necessarily guarantee the full utilization of the facilities.


Asunto(s)
Hospitales/estadística & datos numéricos , Admisión del Paciente/tendencias , Población Rural , Adulto , Factores de Edad , Femenino , Humanos , Masculino , Persona de Mediana Edad , Nigeria , Factores Socioeconómicos
6.
Soc Sci Med ; 16(22): 1971-7, 1982.
Artículo en Inglés | MEDLINE | ID: mdl-7157031

RESUMEN

Elaborate health programmes have always been an important feature of national development plans in Nigeria, especially since independence in 1960. The aspect of the programmes that is examined in this paper is the geographical distribution of medical facilities. The policy objectives in this regard have been to improve access to facilities and personnel by distributing them equally according to population, and to correct the rural urban imbalance in the system. But how far have these objectives been realized? In an attempt to answer this question, the situation in Bendel State is examined in some detail and the results show that the rural urban imbalance is still evident. Correlation analyses showed that areas that have a comparatively large urban population have more facilities and personnel than areas that are predominantly rural. Also, three step-wise multiple regression analyses revealed that Urban population is a far more important factor than total population in explaining the distribution of hospitals, hospital beds and doctors. The doctor/population ratios are exceedingly high for the predominantly rural areas, over 1:70,000 in some cases. These ratios are far in excess of 1:14,000 which was the national target for 1980. All these show that some important policy objectives of the health programmes have not been realized.


Asunto(s)
Política de Salud , Recursos en Salud/provisión & distribución , Accesibilidad a los Servicios de Salud , Programas Nacionales de Salud , Área sin Atención Médica , Nigeria , Salud Rural , Salud Urbana
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