RESUMO
A series of 3-chloro-4-substituted-1-(8-hydroxy-quinolin-5-yl)-azetidin-2-ones were synthesized and evaluated for their in vitro anti-filarial activity. To pre-assess the anti-filarial behavior of synthesized compounds (V(a-f)) on a structural basis, automated docking studies were carried out with Molecular Design Suite (MDS v 3.5) into the active site of glutathione-S-transferase (GST) enzyme; scoring functions of these compounds at the active site of the GST enzyme were used for correlation with observed activity. Compounds V(e) and V(f) have shown good affinity for receptor GST, as well as in vitro anti-filarial potency.
Assuntos
Anti-Helmínticos/química , Glutationa Transferase/química , Animais , Anti-Helmínticos/síntese química , Anti-Helmínticos/farmacologia , Azetidinas , Simulação por Computador , Filariose/tratamento farmacológico , Filarioidea/efeitos dos fármacos , Glutationa Transferase/metabolismo , Modelos Moleculares , Ligação Proteica , Relação Estrutura-AtividadeAssuntos
Catarata/congênito , Disostose Mandibulofacial , Síndrome de Hallermann , Humanos , Lactente , MasculinoAssuntos
Vitamina E/sangue , Criança , Pré-Escolar , Dieta , Ácidos Graxos Essenciais , Feminino , Humanos , Lactente , Masculino , MétodosAssuntos
Anemia Macrocítica/complicações , Cabelo/anormalidades , Deficiência Intelectual , Transtornos da Pigmentação , Tremor , Criança , Pré-Escolar , Feminino , Humanos , Lactente , Recém-Nascido , Masculino , Tremor/tratamento farmacológico , Tremor/etiologia , Vitamina B 12/uso terapêutico , Deficiência de Vitamina B 12/complicaçõesRESUMO
PIP: A study undertaken in a randomly selected village with a population of 695, a majority of whom were agriculturalists or laborers living in huts or mud houses. All couples in the reproductive age group (125) were interviewed in their homes, husbands and wives separately. Couples belonged to Hindu, Muslim, and Scheduled Caste groups. Of the 250 respondents, 120 were literate. About 96% were aware that births could be prevented, with vasectomy and tubectomy the best known methods. Nearly all the respondents gave friends and relatives as the source of their information; family planning workers and posters were given as the source by less than 1/2. 86% of thoce aware of contraceptive methods found family planning acceptable, most expressing the idea that a small family was easier to raise. All of the 14% opposed to family planning were Muslims whose opposiition stemmed from their religious beliefs. 44 of the couples had adopted family planning -- 24 husbands having had vasectomies and 20 of the wives tubectomies. The reasons most often given for not accepting family planning were desire for more chidlren and fear of complications. Of the sterilized respondents, a large number of the men complained of side effects, and 5 of the women complained of excessive bleeding. All of those who expressed complaints said they would not recommend the operation. It is concluded that while awareness of family planning is at an acceptable level, the problem is to make family planning itself acceptable. 1 recommendation is that sterilized couples should receive special medical attention to make their experiences more positive.^ieng