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1.
Pain Med ; 23(7): 1211-1216, 2022 07 01.
Artigo em Inglês | MEDLINE | ID: mdl-35135008

RESUMO

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.


Assuntos
Bloqueio Nervoso Autônomo , Doença de Raynaud , Doenças Reumáticas , Criança , Clonidina/uso terapêutico , Humanos , Dor/complicações , Doença de Raynaud/etiologia , Doença de Raynaud/cirurgia , Doenças Reumáticas/complicações
2.
Bioorg Med Chem ; 26(15): 4551-4559, 2018 08 15.
Artigo em Inglês | MEDLINE | ID: mdl-30097361

RESUMO

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.


Assuntos
Antituberculosos/síntese química , Imidazóis/química , Mycobacterium tuberculosis/efeitos dos fármacos , Administração Oral , Animais , Antituberculosos/farmacologia , Proteínas de Bactérias/antagonistas & inibidores , Proteínas de Bactérias/metabolismo , Sítios de Ligação , Peso Corporal/efeitos dos fármacos , DNA Girase/química , DNA Girase/metabolismo , Imidazóis/farmacologia , Camundongos , Testes de Sensibilidade Microbiana , Simulação de Acoplamento Molecular , Estrutura Terciária de Proteína , Relação Estrutura-Atividade
3.
J Nepal Health Res Counc ; 21(4): 684-688, 2024 Mar 31.
Artigo em Inglês | MEDLINE | ID: mdl-38616603

RESUMO

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.


Assuntos
Deslocamento do Disco Intervertebral , Dor Lombar , Ozônio , Humanos , Oxigênio , Ozônio/uso terapêutico , Estudos Retrospectivos , Deslocamento do Disco Intervertebral/terapia , Dor Lombar/terapia , Nepal
4.
Bioorg Med Chem Lett ; 23(5): 1322-5, 2013 Mar 01.
Artigo em Inglês | MEDLINE | ID: mdl-23369537

RESUMO

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.


Assuntos
Antituberculosos/química , Antituberculosos/farmacologia , Chalconas/química , Chalconas/farmacologia , Antituberculosos/síntese química , Chalconas/síntese química , Células HEK293 , Humanos , Testes de Sensibilidade Microbiana , Conformação Molecular , Mycobacterium tuberculosis/efeitos dos fármacos , Relação Estrutura-Atividade
5.
Bioorg Med Chem Lett ; 21(13): 3966-9, 2011 Jul 01.
Artigo em Inglês | MEDLINE | ID: mdl-21641212

RESUMO

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.


Assuntos
Antituberculosos/síntese química , Antituberculosos/farmacologia , Indenos/síntese química , Indenos/farmacologia , Mycobacterium tuberculosis/efeitos dos fármacos , Animais , Antituberculosos/química , Indenos/química , Camundongos , Testes de Sensibilidade Microbiana , Estrutura Molecular , Relação Estrutura-Atividade
7.
Eur J Med Chem ; 45(9): 4379-82, 2010 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-20584563

RESUMO

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.


Assuntos
Antituberculosos/química , Antituberculosos/farmacologia , Curcuma/química , Diterpenos/química , Diterpenos/farmacologia , Antituberculosos/síntese química , Antituberculosos/isolamento & purificação , Cromatografia Líquida de Alta Pressão , Diterpenos/síntese química , Diterpenos/isolamento & purificação , Testes de Sensibilidade Microbiana , Mycobacterium tuberculosis/efeitos dos fármacos
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