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1.
J Pharm Bioallied Sci ; 15(Suppl 1): S702-S705, 2023 Jul.
Artículo en Inglés | MEDLINE | ID: mdl-37654385

RESUMEN

Background: Obstructive sleep apnea (OSA) is a sleep disorder characterized by periodic and repetitive partial or complete collapse of the upper airway during sleep, resulting in reduced ventilation (hypopnea) or absent ventilation (apnea). Materials and Methods: The present study was conducted on 100 adult OSA patients attending hospitals of Jodhpur and the dental clinic in Vyas Dental College and Hospital in Jodhpur city. The sample consisted of 65.0% males and 35.0% females, belonging to 18 years ≥60 years of age with a mean age of 47.61 ± 8.53. Results: In our study, we have used AHI for the assessment of OSA, the major significant association (P = 0.001) was seen between AHI and periodontitis. The finding suggest that the prevalence of periodontitis is greater among patient with OSA with almost 39 patients with AHI value between 11to15 having loss of attachment between 4 mm ≥8 mm. Conclusion: Obstructive sleep apnea is acting as a significant risk factor for major Dental diseases. The study concludes that there was a significant association found between oral health status and OSA patients.

2.
J Org Chem ; 81(8): 3149-60, 2016 Apr 15.
Artículo en Inglés | MEDLINE | ID: mdl-26999637

RESUMEN

The synthesis of hitherto unreported S-alkyl/aryl benzothiazole-2-carbothioate is reported from thiols, oxalyl chloride, and 2-aminothiophenols using 10 mol % n-tetrabutylammonium iodide (TBAI) as catalyst in acetonitrile through multicomponent reaction (MCR) strategy. The present protocol favored formation of benzothiazoles and thioesters via simultaneous formation of C-N and C-S bonds in good yields with a wide range of substrates. A few of the synthesized derivatives were evaluated for their antimicrobial activity against the protozoan parasite Leishmania donovani, a causative agent of visceral leishmaniasis (VL). Further, these compounds displayed no toxicity toward macrophage RAW 264.7 cells and are therefore nontoxic and effective antileishmanial leads. In silico docking studies were performed to understand the possible binding site interaction with trypanothione reductase (TryR).


Asunto(s)
Antiprotozoarios/síntesis química , Antiprotozoarios/farmacología , Benzotiazoles/síntesis química , Benzotiazoles/farmacología , Leishmania donovani/efectos de los fármacos , Macrófagos/efectos de los fármacos , NADH NADPH Oxidorreductasas/química , NADH NADPH Oxidorreductasas/efectos de los fármacos , Compuestos de Sulfhidrilo/química , Antiprotozoarios/química , Benzotiazoles/química , Sitios de Unión , Leishmania donovani/enzimología , Leishmaniasis Visceral/enzimología , NADH NADPH Oxidorreductasas/metabolismo , Ornitina Descarboxilasa/metabolismo
3.
ACS Comb Sci ; 17(11): 671-81, 2015 Nov 09.
Artículo en Inglés | MEDLINE | ID: mdl-26441303

RESUMEN

Unsymmetrical sulfides were first synthesized using combinations of a 1,3-dicarbonyl, an aromatic aldehyde and a thiol in the presence of 10 mol % ethanolic piperidine. These sulfides derivatives were subsequently converted into corresponding sulfones via oxidation in the presence of m-chloroperoxybenzoic acid (m-CPBA) at ice-bath to room temperature. The former reaction was achieved at room temperature through one-pot three-component. The later was obtained in good yields using mild reaction conditions with flexibility in choice from a range of substrates. The antimicrobial properties of the newly synthesized sulfone derivatives were investigated against the protozoan parasite, Leishmania donovani, a causative agent of visceral leishmaniasis (VL). Nine sulfone derivatives were found to be efficacious and exhibited significant antimicrobial activity. Further, these compounds were nontoxic on murine peritoneal macrophages thus eliminating potential cytoxicity in the host cells. These compounds may be indicated as potential leads in the treatment of visceral leishmaniasis.


Asunto(s)
Antiprotozoarios/farmacología , Descubrimiento de Drogas , Leishmania donovani/efectos de los fármacos , Macrófagos/efectos de los fármacos , Sulfuros/farmacología , Sulfonas/farmacología , Animales , Antiprotozoarios/síntesis química , Antiprotozoarios/química , Supervivencia Celular/efectos de los fármacos , Células Cultivadas , Técnicas Químicas Combinatorias , Cricetinae , Relación Dosis-Respuesta a Droga , Humanos , Macrófagos/parasitología , Ratones , Ratones Endogámicos BALB C , Modelos Moleculares , Estructura Molecular , Oxidación-Reducción , Pruebas de Sensibilidad Parasitaria , Relación Estructura-Actividad , Sulfuros/síntesis química , Sulfuros/química , Sulfonas/síntesis química , Sulfonas/química
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