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1.
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
2.
Indian J Otolaryngol Head Neck Surg ; 64(4): 330-2, 2012 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-24294572

RESUMO

A study was conducted to determine why there was a delay in detection of hearing loss in congenitally hearing impaired children in rural India. It was found that although the parents of these children visited a primary care physician, relevant information regarding investigation and rehabilitation of hearing loss was not available to the patient. In the absence of a universal hearing screening programme in this country, it is a matter of importance to strengthen this aspect of community otolaryngology in the undergraduate ENT programme. There is also a need for continuing medical education programmes for primary care physicians regarding available methods of investigation and rehabilitation for a hearing impaired person.

3.
Indian J Otolaryngol Head Neck Surg ; 64(3): 230-2, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23998025

RESUMO

Tympanoplasty has been the mainstay of treatment in chronic otitis media. In a non cholesteatomatous chronic otitis media, there has been much debate whether a cortical mastoidectomy is required or not. Creating an aerating mastoidectomy in cases of blocked aditus ad antrum helps in reducing the recurrence. However, the status of aditus is not always known unless a mastoidectomy is performed. In this study we try to find out if there is any clinical clue regarding a blocked aditus ad antrum by looking at the tympanic membrane. Fourty-three cases of cortical mastoidectomies were retrospectively studied in this series. Patency of aditus ad antrum was analyzed with respect to presence of myringosclerosis and the status of middle ear mucosa. In this study myringosclerosis was found to be significantly associated with a blocked aditus while no such association was found with the status of middle ear mucosa. The presence of myringosclerosis may indicate a blocked aditus ad antrum and performing a cortical mastoidectomy in such cases may help in creating an aerated mastoid, thereby possibly reducing the recurrence rate.

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