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1.
Pain Med ; 23(7): 1211-1216, 2022 07 01.
Artículo en Inglés | MEDLINE | ID: mdl-35135008

RESUMEN

OBJECTIVE: Sympathetic blocks are invaluable to prevent morbidity from Raynaud's phenomenon (RP). RP may occur in children with rheumatological disorders and causes severe pain, discoloration of digits, gangrene, and auto-amputation. We describe the planning and execution of sympathectomy blocks in children with rheumatological disorders presenting with RP. METHODS: With upper-limb involvement, ultrasound-guided stellate ganglion block (USGB) was given with ropivacaine and clonidine. When all four limbs were involved, intrathecal block with bupivacaine and clonidine was also given. RESULTS: A total of 68 sympathectomy blocks were performed: 28 bilateral USGBs, two unilateral USGBs, and 10 intrathecal injections. Multiple interventions in a single day were frequently required. For safety, all USGBs were performed with an ultrasound with strict adherence to local anaesthetic volume was maintained, with periprocedure monitoring of 2-3 hours. All blocks were performed by an experienced specialist. All children reported immediate pain relief with prevention of major amputation. CONCLUSION: With meticulous planning, monitoring, and precautions, sympathectomy of limbs in pediatric rheumatological disorders with RP can be safely undertaken. Bilateral stellate ganglion block with ultrasound is safe in children, and clonidine is a useful adjunct for vasodilation and prolongation of the effect of sympathectomies in children.


Asunto(s)
Bloqueo Nervioso Autónomo , Enfermedad de Raynaud , Enfermedades Reumáticas , Niño , Clonidina/uso terapéutico , Humanos , Dolor/complicaciones , Enfermedad de Raynaud/etiología , Enfermedad de Raynaud/cirugía , Enfermedades Reumáticas/complicaciones
2.
Bioorg Med Chem ; 26(15): 4551-4559, 2018 08 15.
Artículo en Inglés | MEDLINE | ID: mdl-30097361

RESUMEN

Arylbenzimidazoles have been synthesized as antimycobacterial agents. An efficient synthesis has been developed for 2-arylbenzimidazoles from o-phenylenediamines and aromatic aldehydes in molecular sieves-methanol system. The methodology is straightforward to get 2-arylbenzimidazoles (3a-3z) in excellent yields with high chemoselectivity over 2-aryl-1-benzylbenzimidazoles (4a-4z). All these benzimidazole analogues were evaluated against M. tuberculosis in BACTEC radiometric assay. The compounds 4y and 4z exhibited potential antitubercular activity against M. tuberculosis H37RV, MIC at 16 µM and 24 µM respectively. The best compound of the series i.e. compound 4y was well tolerated by Swiss-albino mice in acute oral toxicity. Compound 4y possessing a diarylbenzimidazole core, can further be optimized for better activity.


Asunto(s)
Antituberculosos/síntesis química , Imidazoles/química , Mycobacterium tuberculosis/efectos de los fármacos , Administración Oral , Animales , Antituberculosos/farmacología , Proteínas Bacterianas/antagonistas & inhibidores , Proteínas Bacterianas/metabolismo , Sitios de Unión , Peso Corporal/efectos de los fármacos , Girasa de ADN/química , Girasa de ADN/metabolismo , Imidazoles/farmacología , Ratones , Pruebas de Sensibilidad Microbiana , Simulación del Acoplamiento Molecular , Estructura Terciaria de Proteína , Relación Estructura-Actividad
3.
J Nepal Health Res Counc ; 21(4): 684-688, 2024 Mar 31.
Artículo en Inglés | MEDLINE | ID: mdl-38616603

RESUMEN

BACKGROUND: Low back pain due to disc herniation is a common problem causing frequent hospital visits and loss of working days with major socio-economic impact. Conservative treatments like analgesics, physiotherapy do not work in all patients. Surgical treatment has been the mainstay of treatment when indicated but is associated with anesthetic and surgical complications. Intradiscal oxygen-ozone chemonucleolysis is a minimally invasive procedure done under local anesthesia and has promising role in shrinking the bulged disc and reducing nerve root compression and related symptoms. This retrospective study was done to see how intradiscal oxygen-ozone chemonucleolysis reduces pain severity in patients with discogenic low back pain. METHODS: Retrospective data were retrieved of those patients who underwent fluoroscopy guided intradiscal oxygen-ozone chemonucleolysis with 5-6 ml of an O2-O3 mixture (concentration of 30 microgram/ml) during a period of two years in Nepal pain care and research center. Numerical pain scale (NRS) at various follow ups were compared to preprocedural NRS. RESULTS: Preprocedural NRS was 8± 13. NRS at three hours, one week, one month, three months and six months were 2± 13 (73 percent reduction), 2± 53 (68 percent reduction), 2± 27 (72 percent reduction), 1± 08 (77 percent reduction) and 1± 67 (79 percent reduction) respectively. CONCLUSIONS: Intradiscal oxygen-ozone chemonucleolysis can be a useful modality of treatment for discogenic low back pain in patients who fail to respond to conservative management and in whom surgery is not indicated.


Asunto(s)
Desplazamiento del Disco Intervertebral , Dolor de la Región Lumbar , Ozono , Humanos , Oxígeno , Ozono/uso terapéutico , Estudios Retrospectivos , Desplazamiento del Disco Intervertebral/terapia , Dolor de la Región Lumbar/terapia , Nepal
4.
Bioorg Med Chem Lett ; 23(5): 1322-5, 2013 Mar 01.
Artículo en Inglés | MEDLINE | ID: mdl-23369537

RESUMEN

Lipophilic chalcones and their conformationally restricted analogues were synthesized and evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv strain. Compounds 16, 24, 25a and 25c were found to be active MIC at 60, 30, 3.5 and 7.5 µg-mL(-1). In vitro cytotoxicity of compounds 16, 24, 25a, 25c and 26 in non-cancerous human epithelial kidney cell line (HEK-293) showed that most active compound 25a was approximately 2.85 times selective towards tubercular versus healthy cells whereas compound 24 was found to be 16 times selective.


Asunto(s)
Antituberculosos/química , Antituberculosos/farmacología , Chalconas/química , Chalconas/farmacología , Antituberculosos/síntesis química , Chalconas/síntesis química , Células HEK293 , Humanos , Pruebas de Sensibilidad Microbiana , Conformación Molecular , Mycobacterium tuberculosis/efectos de los fármacos , Relación Estructura-Actividad
5.
Bioorg Med Chem Lett ; 21(13): 3966-9, 2011 Jul 01.
Artículo en Inglés | MEDLINE | ID: mdl-21641212

RESUMEN

1-Chloro-2-formyl indenes and tetralenes have been synthesized using Vilsmeier-Haack-Arnold reaction onto indanones and tetralones. Most of these analogues exhibited antitubercular activity against Mycobacterium tuberculosis H37Rv strain with MICs ranging from 30 to 500 µg/mL. Analogue 13 was further modified to some derivatives. The most active analogue 23 showing MIC at 30 µg/mL was further evaluated for acute oral toxicity in Swiss albino mice and was found to be safe up to 300 mg/kg dose.


Asunto(s)
Antituberculosos/síntesis química , Antituberculosos/farmacología , Indenos/síntesis química , Indenos/farmacología , Mycobacterium tuberculosis/efectos de los fármacos , Animales , Antituberculosos/química , Indenos/química , Ratones , Pruebas de Sensibilidad Microbiana , Estructura Molecular , Relación Estructura-Actividad
7.
Eur J Med Chem ; 45(9): 4379-82, 2010 Sep.
Artículo en Inglés | MEDLINE | ID: mdl-20584563

RESUMEN

A labdane diterpene dialdehyde was first time isolated from the chloroform extract of rhizomes of Curcuma amada. This compound exhibited antitubercular activity (MIC=500 microg/mL) against Mycobacterium tuberculosis H(37)Rv strain in BACTEC-460 assay. Two of its semisynthetic analogues also exhibited antitubercular activity at 250-500 microg/mL. It is the first report on isolation and antimycobacterial activity of this dialdehyde from C. amada.


Asunto(s)
Antituberculosos/química , Antituberculosos/farmacología , Curcuma/química , Diterpenos/química , Diterpenos/farmacología , Antituberculosos/síntesis química , Antituberculosos/aislamiento & purificación , Cromatografía Líquida de Alta Presión , Diterpenos/síntesis química , Diterpenos/aislamiento & purificación , Pruebas de Sensibilidad Microbiana , Mycobacterium tuberculosis/efectos de los fármacos
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