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1.
Disabil Rehabil ; 44(17): 4709-4716, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-34148468

RESUMO

Purpose: Reactive balance is a critical consideration for mobility and fall avoidance, but is under-assessed among physiotherapists. The objective of this study was to explore factors influencing physiotherapist perceptions about measuring reactive balance upon completion of a 12-month theory-based, multi-component intervention to increase use of a measure of reactive balance.Methods: A qualitative descriptive approach was used. Semi-structured interviews were conducted with 28 physiotherapists treating adults with balance impairment in three urban Canadian rehabilitation hospitals that participated in the intervention. Interviews explored perceptions of reactive balance measurement and perceived changes in clinical behavior. Thematic analysis involved multiple rounds of coding, review and discussion, theme generation, and interpretation of findings through individual analysis and team meetings.Findings: Participants expressed contrasting views about integrating reactive balance measurement in their practice, despite consistent acknowledgement of the importance of reactive balance for function. Three themes were identified highlighting factors that mediated perceptions about measuring reactive balance: patient characteristics; trust between physiotherapist and patient; and the role of physiotherapist fear.Conclusions: The findings highlight that decision making for measuring reactive balance in rehabilitation settings is complex. There is a need for additional work to facilitate long-term implementation of clinical reactive balance measurement, such as refining patient criteria for administration, ensuring sufficient time to establish a trusting relationship, and developing and testing strategies to address physiotherapist fear.IMPLICATIONS FOR REHABILITATIONReactive balance is important for falls prevention and mobility, but is under-assessed among physiotherapists.This study identified three factors that influenced uptake of reactive balance measurement among physiotherapists in rehabilitation settings: patient characteristics; trust between physiotherapist and patient; and the role of physiotherapist fear.Knowledge of the identified factors may assist with design and use of reactive and other balance measurements.Strategies aimed at developing trusting relationships between physiotherapist and patient along with addressing physiotherapist fear could facilitate the uptake of clinical reactive balance measurement.


Assuntos
Fisioterapeutas , Adulto , Canadá , Humanos , Pesquisa Qualitativa
2.
Scand J Med Sci Sports ; 21(5): 653-62, 2011 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-21917016

RESUMO

This study evaluated the effect of 4 weeks of low-load resistance exercise with blood flow restriction (BFRE) on increasing strength in comparison with high-load resistance exercise (HLE), and assessed changes in blood, vascular and neural function. Healthy adults performed leg extension BFRE or HLE 3 days/week at 30% and 80% of strength, respectively. During BFRE, a cuff on the upper leg was inflated to 30% above systolic blood pressure. Strength, pulse-wave velocity (PWV), ankle-brachial index (ABI), prothrombin time (PT) and nerve conduction (NC) were measured before and after training. Markers of coagulation (fibrinogen and D-dimer), fibrinolysis [tissue plasminogen activator (tPA)] and inflammation [high sensitivity C-reactive protein (hsCRP)] were measured in response to the first and last exercise bouts. Strength increased 8% with BFRE and 13% with HLE (P<0.01). No changes in PWV, ABI, PT or NC were observed following training for either group (P>0.05). tPA antigen increased 30-40% immediately following acute bouts of BFRE and HLE (P=0.01). No changes were observed in fibrinogen, D-dimer or hsCRP (P>0.05). These findings indicate that both protocols increase the strength without altering nerve or vascular function, and that a single bout of both protocols increases fibrinolytic activity without altering selected markers of coagulation or inflammation in healthy individuals.


Assuntos
Adaptação Fisiológica , Exercício Físico/fisiologia , Perna (Membro)/fisiologia , Músculo Esquelético/fisiologia , Adolescente , Adulto , Índice Tornozelo-Braço , Velocidade do Fluxo Sanguíneo , Proteína C-Reativa/metabolismo , Feminino , Produtos de Degradação da Fibrina e do Fibrinogênio/metabolismo , Fibrinogênio/metabolismo , Humanos , Perna (Membro)/irrigação sanguínea , Masculino , Força Muscular , Músculo Esquelético/irrigação sanguínea , Condução Nervosa , Tempo de Protrombina , Fluxo Sanguíneo Regional/fisiologia , Treinamento Resistido , Ativador de Plasminogênio Tecidual/sangue , Adulto Jovem
3.
Plast Reconstr Surg ; 66(2): 211-3, 1980 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-7403311

RESUMO

The diagnosis and treatment of 20 cases of velopharyngeal incompetence without cleft palate (frank or submucosal) are discussed. A total of 16 out of 18 patients treated by a sphincter pharyngoplasty were greatly improved, and 10 have normal speech.


Assuntos
Insuficiência Velofaríngea/etiologia , Adenoidectomia/efeitos adversos , Adolescente , Cartilagem/transplante , Bochecha/cirurgia , Criança , Pré-Escolar , Feminino , Humanos , Masculino , Mucosa Bucal/transplante , Músculos Palatinos/cirurgia , Palato Mole/anormalidades , Palato Mole/cirurgia , Faringe/anormalidades , Faringe/cirurgia , Costelas/cirurgia , Distúrbios da Fala/reabilitação , Retalhos Cirúrgicos , Transplante Autólogo , Insuficiência Velofaríngea/cirurgia
4.
Int J Gynaecol Obstet ; 28(4): 355-60, 1989 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-2565258

RESUMO

A series of 155 women with gestational trophoblastic disease (GTD) was evaluated to determine the effect of age on the severity of the disease. The malignant sequelae of hydatidiform moles were of similar frequency at all ages. However, young women, less than 20 years old, had significantly less malignant GTD and significantly less metastatic malignant GTD than did older women.


Assuntos
Mola Hidatiforme/epidemiologia , Neoplasias Trofoblásticas/epidemiologia , Neoplasias Uterinas/epidemiologia , Adulto , Fatores Etários , Feminino , Humanos , Metástase Neoplásica , New York , Gravidez , Prognóstico , Fatores de Risco
5.
Disabil Rehabil ; 14(3): 152-5, 1992.
Artigo em Inglês | MEDLINE | ID: mdl-1520897

RESUMO

The rehabilitation of patients after terrorist attacks has received scant attention in the literature. A case is reported of a patient injured in a letter-bomb explosion; his injuries were bilateral hand loss, loss of one eye, and perforated ear-drums. The successful rehabilitation of this patient to normal work in 8 months is described. A rehabilitation plan for management of similar patients is given.


Assuntos
Traumatismos por Explosões/reabilitação , Traumatismos da Mão/reabilitação , Atividades Cotidianas , Adulto , Amputação Cirúrgica , Traumatismos por Explosões/fisiopatologia , Traumatismos por Explosões/cirurgia , Traumatismos da Mão/fisiopatologia , Traumatismos da Mão/cirurgia , Humanos , Masculino , Terapia Ocupacional/métodos , Próteses e Implantes , Transplante de Pele , Violência
6.
Clin Dysmorphol ; 11(4): 237-41, 2002 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-12401987

RESUMO

We report a family in which a father and his three children are affected with microstomia, micrognathia and partial or complete cleft of the hard and soft palate. The probands were non-identical twins, a boy and a girl, both noted to have the above features soon after birth. Their father was diagnosed with a submucous cleft of the palate at the age of 4 years and their older brother has milder facial features and a bifid uvula. All affected family members were demonstrated to have a fragile site on chromosome 16q22 but otherwise normal karyotypes. Of interest is a previously described family with autosomal dominant inheritance of U-shaped cleft palate, microstomia, micrognathia and oligodontia where all affected members were shown to have the fragile site at 16q22 in a proportion of their cells [Bettex et al. (1998) Eur J Pediatr Surg 8:4-8]. We propose that these two conditions are the same and represent a distinctive syndrome involving aberrant orofacial development that may be linked to the fragile site at 16q22.


Assuntos
Cromossomos Humanos Par 16 , Fissura Palatina/genética , Ligação Genética , Micrognatismo/genética , Microstomia/genética , Adulto , Criança , Pré-Escolar , Sítios Frágeis do Cromossomo , Fragilidade Cromossômica , Fissura Palatina/patologia , Saúde da Família , Feminino , Genes Dominantes , Humanos , Masculino , Micrognatismo/patologia , Microstomia/patologia , Gêmeos Dizigóticos
7.
J Capillary Electrophor ; 3(1): 1-11, 1996.
Artigo em Inglês | MEDLINE | ID: mdl-9384759

RESUMO

Conductivity detection in CE has recently become available in a commercial CE instrument. The new conductivity cell is based on an end-capillary concept. The conductivity sensor and the detection end of the fused-silica capillary are permanently encapsulated in two individually modified coupling connectors (ConTip, ConCap [both from Orion Research, Boston, MA, U.S.A.]). This open-architecture cell permits interchangeability of sensors and capillaries, while maintaining a precisely defined detection volume between those two components when inserted into the detector cell block. The detector's performance is evaluated for sensitivity, linearity, and reproducibility using low-mobility electrolytes. Electropherograms comprising a variety of ionic class separations including inorganic and organic anions, organic surfactants, alkali metals, alkaline earths, transition metals, and organic amines are shown along with separations of actual samples.


Assuntos
Cátions/análise , Condutividade Elétrica , Eletroforese Capilar/métodos , Metais/análise , Vitaminas/análise , Eletroquímica/instrumentação , Eletroquímica/métodos , Eletroforese Capilar/instrumentação , Indicadores e Reagentes , Sensibilidade e Especificidade , Espectrofotometria Ultravioleta/métodos
8.
J Cachexia Sarcopenia Muscle ; 4(4): 287-93, 2013 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24030522

RESUMO

BACKGROUND: Current research into the mechanisms of organ atrophy associated with cancer cachexia have centred on the loss of skeletal muscle, as it is one of the most profound physical changes of the disease. However, many patients with cancer cachexia also experience significant atrophy of the heart. The mechanisms causing cardiac tissue wastage in cancer cachexia are largely unknown. However, it is believed to involve a number of molecular interactions between the tumour and host. Increased levels of oxidative stress have been found in cancer cachectic skeletal muscle and has been linked to the activation of the ubiquitin proteosome system (UPS). The aim of the current study was to examine the role of oxidative stress and the UPS in the hearts of mice with cancer cachexia. METHODS: Oxidative damage to DNA (8-OH-2dG), mRNA levels of the ROS-producing enzymes NADPH oxidase (NOX), and xanthine oxidase (XDH), the antioxidant enzyme superoxide dismutase (SOD) and key components of the UPS was measured in the heart of mice with cancer cachexia. Protein expression levels of NOX enzyme subunits and SOD enzyme activity was also measured in the same heart samples. RESULTS: 8-OH-2dG levels were 1.5-fold higher in the heart of mice with cancer cachexia, and this was associated with a 1.7-fold lower level of NOX2 mRNA and twofold higher XDH mRNA in the same hearts. Cancer cachexia was also associated with a 1.5-fold lower level of SOD activity in the heart. Accompanying these pro- and antioxidant differences was a significantly higher level of mRNA for the key UPS elements MURF-1 (4.3=fold) and MAFbx (3.8-fold) in the hearts of mice with cancer cachexia. CONCLUSIONS: The current study demonstrated that cardiac atrophy of cachectic mice is associated with oxidative damage to DNA in the myocardium. The higher levels of XDH mRNA in cachectic hearts suggest that xanthine oxidase may have an important role to play in producing oxidative stress. It appears that the combination of higher XDH expression and lower SOD enzyme activity are key contributors to oxidative stress and cardiac tissue damage in cancer-induced cardiac atrophy. Oxidative stress in the myocardium as with skeletal muscle may also induce increased expression of the E3 ligases MURF-1 and MAFbx as seen in this study.

9.
Br J Plast Surg ; 34(1): 53-7, 1981 Jan.
Artigo em Inglês | MEDLINE | ID: mdl-7459525

RESUMO

Costal cartilage was harvested from cadavers less than 55 years old, stored in Cialit at a temperature of 4 degrees C and kept in a "cartilage bank" for no longer than one year. The cadaver cartilage was used largely for nasal augmentation and this paper describes the results of 67 cartilage homograft implants in patients who have been followed up for 1-8 years. These suggest that Cialit preserved cartilage homograft should be the first choice of material in nasal augmentation.


Assuntos
Cartilagem/transplante , Cialit , Compostos de Etilmercúrio , Rinoplastia , Preservação de Tecido/métodos , Seguimentos , Humanos , Costelas , Transplante Homólogo
10.
Aust N Z J Surg ; 48(5): 581-5, 1978 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-285709

RESUMO

A variety of different methods have been used for the measurement of pressures during operations on the biliary tract. However, there are few data on the experimental evaluation of the methods, and there has been no controlled comparative evaluation of the most commonly used techniques. In these experiments, we have compared the manometric technique of Caroli, the syringe barrel method of Daniel and White et alii, and the constant infusion apparatus of Cushieri. The experiments were performed in pigs because of the similarity of their biliary tract to that of man. Resting and opening pressures were recorded, and flow into the duodenum via the ampulla was measured simultaneously. The manometric and syringe barrel techniques gave highly reproducible measurements of resting and opening pressure, and valid measurements of opening pressure. The constant infusion apparatus gave reproducible measurements of resting pressure, but did not measure opening pressure. The manometric technique was shown to measure changes in the resistance of the choledochoduodenal junction in response to morphine and atropine.


Assuntos
Sistema Biliar/fisiologia , Animais , Atropina/farmacologia , Sistema Biliar/efeitos dos fármacos , Feminino , Manometria/instrumentação , Manometria/métodos , Morfina/farmacologia , Pressão , Suínos
11.
World J Surg ; 15(4): 446-51, 1991.
Artigo em Inglês | MEDLINE | ID: mdl-1891928

RESUMO

This paper describes a simple method of classification and evaluation of the functional results of replanted and revascularized parts in the hand. The results are presented in graphic form and have been analyzed to correlate various factors: injured part, cause, and zone (level) of injury. The type of injury, ischemic time and age have been studied in more detail to determine their influence of the final functional result. The series contains 187 amputated and devascularized parts of the hand in 119 patients who have undergone surgery at the Prince of Wales Hospital from 1984 through 1988. The length of cold or warm ischemic times, up to 16 hours in this series, while not affecting survival of the amputated part, does adversely affect the functional result. The survival rate of replanted parts in children was significantly less favorable than in adults, but the functional results were uniformly superior.


Assuntos
Traumatismos da Mão/cirurgia , Reimplante , Adolescente , Adulto , Idoso , Amputação Traumática/cirurgia , Criança , Pré-Escolar , Seguimentos , Traumatismos da Mão/classificação , Humanos , Pessoa de Meia-Idade
12.
Hand ; 13(2): 158-63, 1981 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-7286800

RESUMO

A new interpositional elastomeric cap was developed and used for perichondrioplasty in six rheumatoid metacarpophalangeal joints. Adequate cartilage formation occurred, and the joint contours were more normal than those achieved by previous methods.


Assuntos
Artrite Reumatoide/cirurgia , Articulações dos Dedos/cirurgia , Prótese Articular , Articulação Metacarpofalângica/cirurgia , Borracha , Humanos , Articulação Metacarpofalângica/fisiopatologia
13.
J Bacteriol ; 177(18): 5355-7, 1995 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-7665527

RESUMO

Genetic analysis of the tetA(C) gene of pBR322 indicates the importance of two-cytoplasmic loops in the TetA(C) protein (P. McNicholas, I. Chopra, and D. M. Rothstein, J. Bacteriol. 174:7926-7933, 1992). In this study, we characterized second-site suppressor mutations that suggest a functional interaction between these two cytoplasmic regions of the protein.


Assuntos
Antiporters/metabolismo , Proteínas de Bactérias/metabolismo , Plasmídeos/genética , Sequência de Aminoácidos , Antiporters/genética , Proteínas de Bactérias/genética , Códon/genética , Citoplasma , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Genes Bacterianos/genética , Dados de Sequência Molecular , Mutação Puntual , Supressão Genética , Tetraciclina/farmacologia , Resistência a Tetraciclina/genética
14.
J Paediatr Child Health ; 36(1): 69-73, 2000 Feb.
Artigo em Inglês | MEDLINE | ID: mdl-10723695

RESUMO

OBJECTIVE: True hermaphroditism is a rare cause of atypical genitalia which presents significant diagnostic and management challenges. We present the clinical and laboratory findings and management of four patients with true hermaphroditism. METHODOLOGY: Case studies from a teaching hospital and literature review. RESULTS: All four patients had atypical genitalia identified at birth. All had a palpable gonad, only one of which was palpable at birth. Three patients were 46XX (SRY -ve) and one 46XY (SRY +ve). Three patients were raised as females (two 46XX and one 46XY) and one as a male. All four patients were found to have an ovotestis present. CONCLUSIONS: The management of true hermaphroditism is controversial and requires a multidisciplinary approach. It has many implications for both the parent and child. We discuss the issues involved for the patients and their parents.


Assuntos
Transtornos do Desenvolvimento Sexual , Transtornos do Desenvolvimento Sexual/diagnóstico , Transtornos do Desenvolvimento Sexual/terapia , Feminino , Humanos , Recém-Nascido , Masculino
15.
Antimicrob Agents Chemother ; 37(8): 1624-9, 1993 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-8215274

RESUMO

Screening assays for the detection of tetracyclines and inhibitors of tetracycline efflux pumps are described. The tetracycline assay is based on the observation that the tetA(B) gene encoding the efflux pump of transposon Tn10 is induced by tetracycline. The Escherichia coli strain designed to detect tetracyclines contains a single copy of a tetA(B)-lacZ transcriptional fusion integrated into the chromosome and the tetR gene encoding the tetracycline repressor on a plasmid. The assay specifically detects tetracyclines of distinct structures, but not other classes of drugs. A strain capable of detecting inhibitors of the TetA(B) efflux pump contained the tetA(B)-lacZ fusion and, in addition, a tetA(B) structural gene lacking its transcriptional regulatory signals which mediated resistance to only 5 micrograms of tetracycline per ml. This strain was more refractory to induction by tetracycline because of the action of the pump. Inhibitors were detected in two ways: (i) beta-galactosidase induction in the presence of 5 ng of tetracycline per ml, a subinducing concentration, and (ii) growth inhibition in the presence of 5 micrograms of tetracycline per ml. A strain designed to detect inhibitors of the Tet(K) efflux pump from Staphylococcus aureus was constructed by substituting the tet(K) structural gene for the tetA(B) gene. Nocardamine and other siderophores were found to interfere with the action of tetracycline efflux pumps.


Assuntos
Transporte Biológico Ativo/efeitos dos fármacos , Tetraciclinas/análise , Elementos de DNA Transponíveis/genética , Avaliação Pré-Clínica de Medicamentos/métodos , Sinergismo Farmacológico , Indução Enzimática , Escherichia coli/efeitos dos fármacos , Escherichia coli/genética , Fermentação , Peptídeos Cíclicos/farmacologia , Sensibilidade e Especificidade , Resistência a Tetraciclina/genética , Tetraciclinas/farmacocinética , Tetraciclinas/farmacologia , beta-Galactosidase/biossíntese
16.
Med J Aust ; 173(3): 128-31, 2000 Aug 07.
Artigo em Inglês | MEDLINE | ID: mdl-10979377

RESUMO

OBJECTIVE: To investigate the role of topical negative pressure (TNP) therapy in the management of difficult wounds. DESIGN: Prospective consecutive patient series. PATIENTS AND SETTING: 30 patients referred to our tertiary plastic and reconstructive surgical service with wounds deemed unsuitable for reconstructive surgery were treated between November 1997 and the end of December 1998. The mean pretreatment duration of the wounds was 418 days (range, 8-1650 days). All wounds were at least Grade III pressure sores. INTERVENTION: Topical negative pressure therapy (TNP) using the VAC device (KCI Medical, San Antonio, USA). Suction (75-125 mmHg) was continuous for the first 48 hours, then intermittent (2 min on, 5 min off). MAIN OUTCOME MEASURES: Achievement of wound healing endpoints: (1) complete healing of the wound; (2) obliteration of the wound cavity to allow surface dressings; or (3) closure of the wound by suture or skin graft. RESULTS: TNP was successful in 26 out of 30 patients with mean therapy time of 35 days (range, 3-124 days). Healing was more rapid in acute (less than six weeks old) wounds. A reduction in the number of bacterial species and colonies was also observed during therapy. CONCLUSION: TNP can, in some circumstances, promote rapid secondary wound healing. A further randomised trial of TNP versus more traditional wound management modalities is justified.


Assuntos
Bandagens , Cicatrização , Ferimentos e Lesões/terapia , Humanos , Pressão , Estudos Prospectivos
17.
Antimicrob Agents Chemother ; 44(6): 1418-27, 2000 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-10817687

RESUMO

Protein secretion is an essential process for bacterial growth, yet there are few if any antimicrobial agents which inhibit secretion. An in vivo, high-throughput screen to detect secretion inhibitors was developed based on the translational autoregulation of one of the central protein components, SecA. The assay makes use of a SecA-LacZ fusion reporter construct in Escherichia coli which is induced when secretion is perturbed. Several compounds, including two natural product extracts, which had the ability to induce the reporter fusion were identified and the MICs of these compounds for Staphylococcus aureus strain MN8 were found to be < or =128 microg/ml. Enzyme-linked immunosorbent assay, Western blotting, and immunoprecipitation techniques were used to analyze the affects of these compounds on protein secretion. Six representative compounds presented here appear to be bona fide secretion inhibitors but were found to have deleterious effects on membranes. It was concluded that, while the method described here for identifying inhibitors of secretion is valid, screens such as this, which are directed against the membrane-bound portion of a pathway, may preferentially identify compounds which affect membrane integrity.


Assuntos
Adenosina Trifosfatases/genética , Antibacterianos/farmacologia , Proteínas de Bactérias/metabolismo , Proteínas de Transporte/genética , Proteínas de Escherichia coli , Proteínas de Membrana Transportadoras , beta-Galactosidase/genética , Adenosina Trifosfatases/metabolismo , Proteínas de Transporte/metabolismo , Escherichia coli , Genes Reporter , Proteínas Recombinantes de Fusão/efeitos dos fármacos , Proteínas Recombinantes de Fusão/metabolismo , Canais de Translocação SEC , Proteínas SecA , Staphylococcus aureus , beta-Galactosidase/metabolismo
18.
Mol Cell ; 1(1): 25-34, 1997 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-9659900

RESUMO

Mammalian cells constantly monitor and respond to a myriad of extracellular signals, often by using cell surface receptors. Two important classes of cell surface receptors include the receptor tyrosine kinases, which recognize peptide growth factors such as insulin, and the integrins, which most often mediate binding to components of the extracellular matrix. We report that the collagens serve as ligands for the previously orphan family of discoidin domain-containing receptor-like tyrosine kinases. The unexpected realization that an extracellular matrix molecule can directly serve as a ligand for receptor tyrosine kinases provides an example of ligands shared by integrins and receptor tyrosine kinases, and this finding seems likely to change prevailing views about the mechanisms by which cells perceive and respond to the extracellular matrix.


Assuntos
Colágeno/metabolismo , Proteínas da Matriz Extracelular/metabolismo , Receptores Proteína Tirosina Quinases/metabolismo , Receptores Mitogênicos/metabolismo , Proteínas de Saccharomyces cerevisiae , Animais , Células COS , Colágeno/farmacologia , Receptores com Domínio Discoidina , Relação Dose-Resposta a Droga , Proteínas da Matriz Extracelular/farmacologia , Proteínas Fúngicas/química , Proteínas Fúngicas/genética , Proteínas Fúngicas/metabolismo , Regulação Enzimológica da Expressão Gênica , Integrinas/metabolismo , Ligantes , Fosforilação , Plasmídeos , Estrutura Terciária de Proteína , Receptores Proteína Tirosina Quinases/química , Receptores Proteína Tirosina Quinases/genética , Receptores Mitogênicos/química , Receptores Mitogênicos/genética , Rabdomiossarcoma , Células Tumorais Cultivadas/química , Células Tumorais Cultivadas/efeitos dos fármacos , Células Tumorais Cultivadas/metabolismo
19.
Bioorg Med Chem Lett ; 8(18): 2451-6, 1998 Sep 22.
Artigo em Inglês | MEDLINE | ID: mdl-9873560

RESUMO

Exploration of the indole nitrogen region of Zafirlukast (1) has uncovered a potent series of cysteinyl leukotriene D4 (LTD4) antagonists. These studies showed that a variety of functionality could be incorporated in this region of the molecule without sacrificing potency. Efforts to exploit this site in order to improve oral efficacy are discussed.


Assuntos
Antagonistas de Leucotrienos/síntese química , Antagonistas de Leucotrienos/farmacologia , Proteínas de Membrana , Receptores de Leucotrienos , Compostos de Tosil/química , Animais , Cobaias , Haplorrinos , Humanos , Indóis , Modelos Químicos , Fenilcarbamatos , Ratos , Sulfonamidas , Compostos de Tosil/farmacologia
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