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1.
Arch Pharm (Weinheim) ; 355(8): e2200084, 2022 Aug.
Artigo em Inglês | MEDLINE | ID: mdl-35567313

RESUMO

The conceptual layout of monoamine oxidase (MAO) inhibitors has been modified to explore their potential biological application in the case of neurological disorders for the time being. The current review article is an effort to display the summation of innovative conceptual prospects of MAO inhibitors and their intriguing chemistry and bioactivity. Based on this scenario, we emphasize the pivotal role of the benzyloxy moiety attached to scaffolds like oxadiazolones, indolalkylamines, safinamide, caffeine, benzofurans, α-tetralones, ß-nitrostyrene, benzoquinones, coumarins, indoles, chromones, and chromanone analogs, while acting as an MAO inhibitor.


Assuntos
Inibidores da Monoaminoxidase , Monoaminoxidase , Cromonas/farmacologia , Cumarínicos , Dopaminérgicos , Monoaminoxidase/metabolismo , Inibidores da Monoaminoxidase/farmacologia , Relação Estrutura-Atividade
2.
Indian J Otolaryngol Head Neck Surg ; 75(Suppl 1): 715-722, 2023 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-37206851

RESUMO

The gold standard for diagnosis of Obstructive sleep apnea (OSA) is an overnight polysomnography (PSG). However, PSG is time consuming, labour intensive and expensive. In our country PSG is not available everywhere. Therefore, a simple and reliable method of identifying patients of OSA is important for its prompt diagnosis and treatment. This study looks at the efficacy of three questionnaires to serve as a screening test for the diagnosis of OSA in the Indian population. For the first time in India, a prospective study was conducted wherein patients with history of OSA underwent PSG and were asked to fill three questionnaires-Epworth Sleepiness Score (ESS), Berlin Questionnaire (BQ) and Stop Bang Questionnaire (SBQ). The scoring of these questionnaires were compared with the PSG results. SBQ had a high negative predictive value (NPV) and the probability of moderate and severe OSA steadily increases with higher SBQ scores. In comparison, ESS and BQ had low NPV. SBQ is a useful clinical tool to identify patients at high risk of OSA and can facilitate in the diagnosis of unrecognised OSA.

3.
Comb Chem High Throughput Screen ; 26(4): 668-681, 2023.
Artigo em Inglês | MEDLINE | ID: mdl-35430964

RESUMO

BACKGROUND: Tuberculosis is one of the oldest known infectious diseases to mankind, caused by Mycobacterium tuberculosis. Although current treatment using first-line anti-tubercular drugs is proven to be effective, an infection caused by resistant strains, as in multidrug-resistant and extensive drug- resistant tuberculosis is still an impending challenge to treat. OBJECTIVE: Our objective is to focus on reporting benzimidazole derivatives that are targeting mycobacterial membrane biosynthesis, particularly the mycobacterial mycolyl-arabinogalactanpeptidoglycan complexes. From the literature survey, it has been noted that targeting Mycobacterium tuberculosis cell membrane biosynthesis is an effective approach to fight against drug resistance in tuberculosis. METHODS: Articles on benzimidazole derivatives as inhibitors of proteins responsible for the biosynthesis of the mycobacterial mycolyl-arabinogalactan-peptidoglycan complex have been selected. RESULTS: By reviewing the anti-tubercular activity of the reported benzimidazole derivatives, we have concluded that a correlation between benzimidazole derivatives and their biological activity is found. It has been noted that benzimidazole derivatives with substitution at N1, C2, C5, and C6 positions have shown a greater affinity towards target proteins. CONCLUSION: Even though scientific advancement toward the prevention of tuberculosis has been quite significant in the past few decades, infection caused by resistant strains is a major concern. We have collected data on benzimidazole derivatives that inhibit the biosynthesis of mycolic acid, arabinogalactan and, peptidoglycan. From our observations, we conclude that majority of the molecules have given anti-tubercular activity in nanomolar range. Still there are few mycobacterial membrane biosynthesis proteins where benzimidazole as an inhibitor has yet to be explored.


Assuntos
Mycobacterium tuberculosis , Tuberculose , Humanos , Peptidoglicano/metabolismo , Benzimidazóis/farmacologia , Tuberculose/tratamento farmacológico , Antituberculosos/farmacologia
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