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1.
J Pharm Bioallied Sci ; 15(Suppl 1): S702-S705, 2023 Jul.
Artigo em Inglês | MEDLINE | ID: mdl-37654385

RESUMO

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.
Artigo em Inglês | MEDLINE | ID: mdl-26999637

RESUMO

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).


Assuntos
Antiprotozoários/síntese química , Antiprotozoários/farmacologia , Benzotiazóis/síntese química , Benzotiazóis/farmacologia , Leishmania donovani/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , NADH NADPH Oxirredutases/química , NADH NADPH Oxirredutases/efeitos dos fármacos , Compostos de Sulfidrila/química , Antiprotozoários/química , Benzotiazóis/química , Sítios de Ligação , Leishmania donovani/enzimologia , Leishmaniose Visceral/enzimologia , NADH NADPH Oxirredutases/metabolismo , Ornitina Descarboxilase/metabolismo
3.
ACS Comb Sci ; 17(11): 671-81, 2015 Nov 09.
Artigo em Inglês | MEDLINE | ID: mdl-26441303

RESUMO

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.


Assuntos
Antiprotozoários/farmacologia , Descoberta de Drogas , Leishmania donovani/efeitos dos fármacos , Macrófagos/efeitos dos fármacos , Sulfetos/farmacologia , Sulfonas/farmacologia , Animais , Antiprotozoários/síntese química , Antiprotozoários/química , Sobrevivência Celular/efeitos dos fármacos , Células Cultivadas , Técnicas de Química Combinatória , Cricetinae , Relação Dose-Resposta a Droga , Humanos , Macrófagos/parasitologia , Camundongos , Camundongos Endogâmicos BALB C , Modelos Moleculares , Estrutura Molecular , Oxirredução , Testes de Sensibilidade Parasitária , Relação Estrutura-Atividade , Sulfetos/síntese química , Sulfetos/química , Sulfonas/síntese química , Sulfonas/química
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