A metronidazole-resistant strain of <i>Trichomonas vaginalis</i> and its sensitivity to Go 10213

Ray, D. K.; Tendulkar, J. S.; Shrivastava, Vikas; Datta, Anuja; Nagarajan, K.

doi:10.1093/jac/14.4.423

Cited by 8 publications

(4 citation statements)

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“…Modifications at the 2 position, however, are known to interfere with both the activity and the microbial spectrum [31]. Compound GO 10213 [1-methylsulfonyl-3-(1-methyl-5-nitro-2-imidazolyl)-2-imidazolidinone], which has an imidazolidinone ring structure at the 2 position [32], exerts stronger antitrichomonal activity than MTZ (Figure 1) [33,34]. GO 10213 is highly active against anaerobic bacteria, even more than metronidazole but less than niridazole.…”

Section: Antibacterial Agentsmentioning

confidence: 99%

“…GO 10213 is highly active against anaerobic bacteria, even more than metronidazole but less than niridazole. Thus, the modification of the 5-nitroimidazole at the 2 position increases not only its antitrichomonal activity but also its antibacterial activity [33,34]. Although GO 10213 may be more active than MTZ, the imidazolidinone ring in this compound has been shown to be more carcinogenic than the nitro-imidazole ring, making it less attractive therapeutically [35].…”

Section: Antibacterial Agentsmentioning

confidence: 99%

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Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Mital

2009

Sci. Pharm.

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Parasitic and bacterial infections affecting the gastrointestinal tract represent a significant cause of morbidity and mortality worldwide. Nitroheterocyclic drugs have been available since the early 1960s for the treatment of anaerobic protozoa. The application of these drugs has widened and they are presently used to treat anaerobic pathogenic bacteria and protozoa. 5-nitroimidazoles are a well-established group of antiprotozoal and antibacterial agents that inhibit the growth of both anaerobic bacteria and certain anaerobic protozoa, such as Trichomonas vaginalis, Entamoeba histolytica and Giardia lamblia. The important antibacterial and antiprotozoal activities of nitroimidazoles are associated with reductive metabolism that has led to considerable interest in nitroimidazole reduction chemistry and the synthesis of new, highly effective drugs. The present review provides a brief account of various biological activities exhibited by synthetic nitroimidazole derivatives as well as their structure-mutagenicity relationships.

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Section: Antibacterial Agentsmentioning

confidence: 99%

Section: Antibacterial Agentsmentioning

confidence: 99%

Synthetic Nitroimidazoles: Biological Activities and Mutagenicity Relationships

Mital

2009

Sci. Pharm.

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“…[29][30][31] The compounds significantly superior to the standard drug, metronidazole in caecal and hepatic amoebiasis, 32 giardiasis and trichomoniasis. 33 The superiority extends to activity against anaerobic bacteria also. Methanesulphonyl residue was introduced in 17 as a blocking group with a view to knocking it off in 18 and replacing it with an acetyl group, which was the initial lead.…”

Section: Antiamoebic Activity -Satranidazolementioning

confidence: 99%

Creative research in the chemical industry – Four decades in retrospect

Nagarajan¹

2006

J Chem Sci

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My professional research career spanning more than four decades has been largely devoted to synthetic medicinal chemistry (Ciba, Bombay-now Mumbai-21 years) followed by an equal number of years in process development of drugs, crop protection chemicals (Searle, Bombay) and drugs and speciality chemicals (Recon and Hikal, Bangalore). These efforts have involved several collaborators including many from other institutions and offered multitudinous challenges calling for continuous creativity in industrial setups. I was fortunate to have had a conducive environment to be able to respond to these challenges. I attempt to offer the readers in the ensuing pages a flavour of the excitement that has marked these years.

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“…Compound GO 10213 [1-methylsulfonyl-3-(1-methyl-5-nitro-2-imidazolyl)-2-imidazolidinone], which has an imidazolidinone ring structure at the 2 position (7) (Fig. 1), exerts stronger antitrichomonal activity than metronidazole (9,10). In this communication the antibacterial activities of compound GO 10213 are described and compared with those of metronidazole and niridazole, a 5-nitrothiazole derivative ( Fig.…”

mentioning

confidence: 99%