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1.
Molecules ; 27(1)2021 Dec 23.
Artigo em Inglês | MEDLINE | ID: mdl-35011293

RESUMO

Ongoing resistance developments against antibiotics that also affect last-resort antibiotics require novel antibacterial compounds. Strategies to discover such novel structures have been dimerization or hybridization of known antibacterial agents. We found novel antibacterial agents by dimerization of indols and hybridization with carbazoles. They were obtained in a simple one-pot reaction as bisindole tetrahydrocarbazoles. Further oxidation led to bisindole carbazoles with varied substitutions of both the indole and the carbazole scaffold. Both the tetrahydrocarbazoles and the carbazoles have been evaluated in various S. aureus strains, including MRSA strains. Those 5-cyano substituted derivatives showed best activities as determined by MIC values. The tetrahydrocarbazoles partly exceed the activity of the carbazole compounds and thus the activity of the used standard antibiotics. Thus, promising lead compounds could be identified for further studies.


Assuntos
Antibacterianos/química , Antibacterianos/farmacologia , Staphylococcus aureus Resistente à Meticilina/efeitos dos fármacos , Antibacterianos/síntese química , Carbazóis/química , Técnicas de Química Sintética , Testes de Sensibilidade Microbiana , Estrutura Molecular , Análise Espectral , Relação Estrutura-Atividade
2.
Future Med Chem ; 14(5): 299-305, 2022 03.
Artigo em Inglês | MEDLINE | ID: mdl-34951320

RESUMO

Background: With constantly increasing resistance against the known antibiotics, the search for novel antibacterial compounds is a challenge. The number of synthetic antibacterial agents is limited. Materials & methods: We discovered novel small-molecule antibacterial agents that are accessible via a simple two-step procedure. The evaluation against Staphylococcus aureus showed antibacterial effects depending on the substituent positioning at the residues of the molecular scaffold. Additionally, we investigated the potential of the compounds to increase the antibacterial activity of tetracycline. Results: The most effective antibacterial compounds possessed a 3-methoxy function at an aromatic residue. In combination with tetracycline, we found a strong effect for a few compounds in boosting the antibacterial activity, so the first promising lead compounds with dual activities could be identified.


Assuntos
Antibacterianos/farmacologia , Bibliotecas de Moléculas Pequenas/química , Staphylococcus aureus/efeitos dos fármacos , Acridinas/química , Antibacterianos/síntese química , Antibacterianos/química , Linhagem Celular , Sobrevivência Celular/efeitos dos fármacos , Humanos , Testes de Sensibilidade Microbiana , Bibliotecas de Moléculas Pequenas/farmacologia , Relação Estrutura-Atividade
3.
Am J Orthop (Belle Mead NJ) ; 34(11): 551-61, 2005 Nov.
Artigo em Inglês | MEDLINE | ID: mdl-16375063

RESUMO

Ankle injuries are common in the general and athletic populations. These injuries constitute 21% of all sports-related injuries. The wide spectrum of sports-related ankle injuries includes ligamentous injuries, soft-tissue and osseous impingement, osteochondral lesions of the talus, tendon injuries, and fractures. Occult lesions (eg, fractures of the lateral process of the talus, fractures of the anterior process of the calcaneus, fractures of the base of the fifth metatarsal, os trigonum, stress fractures) may be missed on initial physical examination, and patients with such injuries often present to a sports clinic with persistent pain around the ankle. Because of increasing participation in sporting events, health care professionals involved in the care of athletes at all levels must have a thorough understanding of the anatomy, pathophysiology, and initial management of ankle injuries. In this review, we describe the pertinent anatomy, pathology, diagnosis, and treatment of sports-related injuries of the ankle.


Assuntos
Traumatismos do Tornozelo , Traumatismos em Atletas , Procedimentos Ortopédicos/métodos , Traumatismos do Tornozelo/diagnóstico , Traumatismos do Tornozelo/terapia , Artrografia , Traumatismos em Atletas/diagnóstico , Traumatismos em Atletas/terapia , Humanos , Imageamento por Ressonância Magnética , Índices de Gravidade do Trauma , Resultado do Tratamento
4.
Am J Orthop (Belle Mead NJ) ; 44(6): E195-8, 2015 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-26047005

RESUMO

Since 1887, approximately 50 cases of an intra-articular patellar dislocation have been reported in the worldwide literature. The vast majority of patients required an open reduction of the patella or closed reduction under general anesthesia. This injury has never been reported in association with a coronal shear fracture of the femoral condyle. A 14-year-old boy presented to our institution with his left knee locked in flexion after a direct blow. Radiographs showed the patella rotated on its horizontal axis and lying in a transverse position within the knee joint, as well as a concomitant femoral condyle fracture. After a successful closed reduction of the patella, the patient underwent open reduction and rigid fixation of the femoral condyle fracture with countersunk interfragmentary screws. At 12 months, the patient was ambulating on the left leg and had painless motion of the knee. We present a rare injury pattern in a skeletally immature patient after a direct blow to the knee. By treating the injuries in a sequential manner and providing a stable fixation construct, the patient was able to achieve a satisfactory return to function even after sustaining a considerable injury to the knee.


Assuntos
Fraturas do Fêmur/cirurgia , Fixação Interna de Fraturas , Luxação Patelar/cirurgia , Adolescente , Fraturas do Fêmur/complicações , Fêmur/cirurgia , Humanos , Articulação do Joelho/cirurgia , Masculino , Luxação Patelar/complicações , Amplitude de Movimento Articular , Resultado do Tratamento
5.
Orthop J Sports Med ; 3(5): 2325967115584883, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-26676153

RESUMO

BACKGROUND: Lack of insurance has been shown to lead to delays in seeking care as well as fewer preventive medicine visits and poorer overall health status. PURPOSE: To investigate the effects of insurance status on the timing and treatment of patients with bucket-handle meniscus tears. STUDY DESIGN: Cohort study; Level of evidence, 3. METHODS: Charts from 2004 to 2013 were retrospectively reviewed for patients diagnosed with bucket-handle meniscus tears. Patients were divided into 2 groups: insured or underinsured. The insured group included patients with commercial insurance or Medicare. The underinsured group included patients with Medicaid or Charity Care. Time intervals were categorized as <6 weeks or ≥6 weeks. RESULTS: A total of 52 patients were included in this study: 15 (29%) insured and 37 (71%) underinsured. Underinsured patients experienced delays in initial presentation to an orthopaedic surgeon (P = .004), time from magnetic resonance imaging to surgery (P = .01), and time from injury to surgery (P = .007). Repair rates were 40% and 38% (P > .999) for the insured and underinsured, respectively. Repair rates for <6 weeks from injury to surgery were 75% for insured (P = .007) and 100% for underinsured patients (P = .001). Repair rates for ≥6 weeks from injury to surgery were 0% for insured and 30% for underinsured patients. Overall, patients with an injury-to-surgery time of <6 weeks had a significantly higher repair rate (87%) than those managed >6 weeks (19%) (P < .001). CONCLUSION: Underinsured patients experience significant delays in time to presentation and overall time to surgery. However, the overall repair rate between the insured and underinsured is similar. Regardless of insurance status, patients undergoing arthroscopy within 6 weeks of injury have a significantly higher repair rate than those after 6 weeks. CLINICAL RELEVANCE: Patients undergoing arthroscopy within 6 weeks of injury have a significantly higher repair rate than those after 6 weeks.

6.
Knee ; 22(6): 672-6, 2015 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-25963730

RESUMO

Patellar sleeve fractures are easily missed injuries since plain radiographs may not show a bony fragment at the time of injury. Failure to diagnose these injuries can result in patellar instability, extensor lag, and anterior knee pain. We report a novel treatment using a Taylor spatial frame as part of a staged reconstruction to regain length of the extensor mechanism and maintain knee motion prior to performing primary repair of the avulsed patellar sleeve fragment. In our case, an 11-year-old male presented to our institution six months after sustaining a patellar sleeve fracture. Radiographic examination with the knee in extension revealed a 23-mm gap between the inferior patellar pole fragment and the remaining patella. The patient was ultimately taken to the operating room twelve months after the initial injury for placement of a Taylor spatial frame to regain length of the extensor mechanism. The patient began immediate knee range-of-motion exercises, and performed daily soft tissue lengthening of two millimeters. After four weeks of treatment the patient underwent removal of the fixator and primary repair of the patella. At final follow up six years after patellar reconstruction, the patient had an active knee range-of-motion from five degrees of hyperextension to 140° of flexion. Where current literature reports suboptimal results even when treatment is delayed for two months, in our case the patient was able to obtain a high level of function after treatment with a two-stage reconstruction using a Taylor spatial frame.


Assuntos
Fixação Interna de Fraturas/instrumentação , Fraturas Ósseas/cirurgia , Traumatismos do Joelho/cirurgia , Articulação do Joelho/cirurgia , Patela/cirurgia , Criança , Desenho de Equipamento , Fraturas Ósseas/diagnóstico por imagem , Humanos , Articulação do Joelho/fisiopatologia , Masculino , Patela/lesões , Radiografia , Amplitude de Movimento Articular
7.
Arthroscopy ; 18(9): E47, 2002.
Artigo em Inglês | MEDLINE | ID: mdl-12426556

RESUMO

We retrieved a high-molecular-weight poly-L-lactic) (PLLA) anterior cruciate ligament (ACL) interference screw (Arthrex, Naples, FL) after 30 months in vivo during revision ACL surgery. Gross, histologic, histomorphometric, and molecular weight measurements were carried out on the implant and the surrounding bone. These studies showed a 75% decrease in the molecular weight of the screw, with implant fragmentation and new bone formation adjacent to the screw and graft. Healing of the graft within the bony tunnel with no significant inflammatory reaction had occurred. The clinical implications of these findings are that this implant dissolves slowly, and it was physically present at 30 months in vivo. It is a safe, nonreactive alternative to traditional metal interference screws used for ACL graft fixation. It will eventually be substituted by bone and will eliminate some of the problems associated with metallic devices.


Assuntos
Implantes Absorvíveis , Ligamento Cruzado Anterior/cirurgia , Artroscopia , Parafusos Ósseos , Poliésteres , Cicatrização , Adulto , Ligamento Cruzado Anterior/patologia , Lesões do Ligamento Cruzado Anterior , Traumatismos em Atletas/patologia , Traumatismos em Atletas/cirurgia , Remoção de Dispositivo , Seguimentos , Humanos , Masculino , Peso Molecular , Período Pós-Operatório , Recidiva , Ruptura/cirurgia
8.
Foot Ankle Int ; 25(10): 712-5, 2004 Oct.
Artigo em Inglês | MEDLINE | ID: mdl-15566702

RESUMO

BACKGROUND: Appropriate suture selection is necessary in providing mechanical stability to soft tissue reconstructions. Caprolactone/glycolide (Panacryltrade mark) became a popular suture, possessing excellent handling properties; however, clinical observations questioned the knot security of caprolactone/glycolide. Caprolactone/glycolide is still available on many commercial suture anchor systems. This study compared the security of the knots and ultimate tensile strength of braided caprolactone/glycolide suture to that of a commonly used suture material, braided polyester (Ethibondtrade mark). MATERIALS: Suture knots of No. 2 braided polyester suture and No. 2 braided caprolactone/glycolide suture were submersed in a physiologic saline solution and stressed using a continuous (non-cyclic) load, simulating a single maximal loading event in a clinical setting. Continuous loading was done to achieve clinical suture knot failure (3-mm knot slippage), then continued until catastrophic suture failure (suture breakage) occurred. Ten trials of each suture were tested. RESULTS: Force required to cause knot slippage of 3 mm was greater for braided polyester than for braided caprolactone/glycolide (p <. 0001, unpaired Students' t-test). Forces resulting in catastrophic failure were greater for braided polyester than braided caprolactone/glycolide (p = .0284, unpaired Students' t-test). CONCLUSIONS: These data have important implications in the selection of suture materials for repair of soft tissue injuries. In the clinical setting, a single maximal loading event may result in suture failure. These data indicate that braided polyester possesses superior in-vitro mechanical properties and suggest that braided polyester may provide greater security in-vivo than braided caprolactone/glycolide suture.


Assuntos
Dioxanos/normas , Poliésteres/normas , Polietilenotereftalatos/normas , Suturas/normas , Teste de Materiais , Estresse Mecânico , Técnicas de Sutura/instrumentação , Resistência à Tração
9.
J Bone Joint Surg Am ; 94(2): 118-20, 2012 Jan 18.
Artigo em Inglês | MEDLINE | ID: mdl-22257997

RESUMO

BACKGROUND: Ethyl chloride topical anesthetic spray is labeled as nonsterile, yet it is widely used during injection procedures performed in an outpatient setting. The purpose of this study was to investigate the sterility of ethyl chloride topical anesthetic spray applied before an injection. Our a priori hypothesis was that application of the spray after the skin has been prepared would not alter the sterility of the injection site. METHODS: We conducted a prospective, blinded, controlled study to assess the effect of ethyl chloride spray on skin sterility. Fifteen healthy adult subjects (age, twenty-three to sixty-one years) were prepared for mock injections into both shoulders and both knees, although no injection was actually performed. Three culture samples were obtained from each site on the skin: one before skin preparation with isopropyl alcohol, one after skin preparation and before application of ethyl chloride, and one after ethyl chloride had been sprayed on the site. In addition, the sterility of the ethyl chloride was tested directly by inoculating cultures with spray from the bottles. RESULTS: Growth occurred in 70% of the samples obtained before skin preparation, 3% of the samples obtained after skin preparation but before application of ethyl chloride, and 5% of the samples obtained after the injection site had been sprayed with ethyl chloride. The percentage of positive cultures did not increase significantly after application of ethyl chloride (p = 0.65). Spraying of ethyl chloride directly on agar plates resulted in growth on 13% of these plates compared with 11% of the control plates; this difference was also not significant (p = 0.80). CONCLUSIONS: Although ethyl chloride spray is not sterile, its application did not alter the sterility of the injection sites in the shoulder and knee.


Assuntos
Anestésicos Locais/administração & dosagem , Cloreto de Etil/administração & dosagem , Pele/microbiologia , Adulto , Humanos , Injeções Intra-Articulares , Joelho , Pessoa de Meia-Idade , Estudos Prospectivos , Ombro , Método Simples-Cego , Esterilização/métodos , Adulto Jovem
12.
Clin Orthop Relat Res ; 438: 204-8, 2005 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-16131892

RESUMO

UNLABELLED: Feet are prone to bacterial contamination. We hypothesized that chlorhexidine scrub and isopropyl alcohol paint provide superior local flora reduction than povidone-iodine scrub and paint. Patients with intact, uninfected skin having clean elective foot and ankle surgery were prospectively enrolled and randomly assigned to skin preparation with povidone-iodine (Group 1) or chlorhexidine scrub and isopropyl alcohol paint (Group 2). Culture swabs (aerobic, anaerobic, acid fast, fungus, and routine antibiotic sensitivity) were taken from all web spaces, nail folds, toe surfaces, and proposed surgical incision sites. One-hundred twenty-seven patients were enrolled (mean age, 46 years; range, 16-85 years). Sixty-seven patients were assigned to Group 1; 60 patients were assigned to Group 2. In Group 1, 53 of 67 patients (79%) had positive cultures; in Group 2, 23 of 60 patients (38%) had positive cultures. These data indicate that chlorhexidine and alcohol provide better reduction in bacterial carriage than povidone-iodine. Based on these data, we recommended chlorhexidine as the surgical preparatory agent for the foot and ankle. LEVEL OF EVIDENCE: Therapeutic study, Level I-1a (significant difference). See the Guidelines for Authors for a complete description of levels of evidence.


Assuntos
Anti-Infecciosos Locais/administração & dosagem , Clorexidina/administração & dosagem , Procedimentos Ortopédicos , Pele/efeitos dos fármacos , Infecção da Ferida Cirúrgica/prevenção & controle , Adolescente , Adulto , Idoso , Idoso de 80 Anos ou mais , Tornozelo/microbiologia , Tornozelo/cirurgia , Antibioticoprofilaxia , Bactérias/efeitos dos fármacos , Bactérias/crescimento & desenvolvimento , Contagem de Colônia Microbiana , Medicina Baseada em Evidências , Feminino , Pé/microbiologia , Pé/cirurgia , Fungos/efeitos dos fármacos , Fungos/crescimento & desenvolvimento , Humanos , Masculino , Pessoa de Meia-Idade , Povidona-Iodo/uso terapêutico , Pele/microbiologia
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