Anti-Pneumocystis carinii pneumonia activity of dicationic 2,4-diarylpyrimidines

Kumar, Arvind; Dw, Boykin; Wilson, W. David; Jones, S. K.; Bender, B. K.; Dykstra, Christine C.; Hall, J. E.; Tidwell, R. R.

doi:10.1016/0223-5234(96)83970-5

Cited by 34 publications

(18 citation statements)

References 27 publications

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“…Analogs of furamidine in which the furan ring has been replaced by pyrrole [136], thiophene [136], and other five-membered ring units have been studied [137]. We have also replaced the central ring with six-membered rings including pyridine [138], pyrimidine [139][140][141], pyridazine [137], and triazine [142]. While these modifications have led to a number of compounds with both significant DNA affinity and antimicrobial activity, especially in the pyrimidine series, none appeared to have significant advantages over the furan analogs.…”

Section: Antimicrobial Activity Of Furamidine and Analogsmentioning

confidence: 99%

Dicationic DNA Minor Groove Binders as Antimicrobial Agents

Tidwell¹,

Boykin

2002

Small Molecule DNA and RNA Binders

159

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Section: Antimicrobial Activity Of Furamidine and Analogsmentioning

confidence: 99%

Dicationic DNA Minor Groove Binders as Antimicrobial Agents

Tidwell¹,

Boykin

2002

Small Molecule DNA and RNA Binders

159

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“…45 We have also studied the replacement of the central five membered furan ring by pyrrole, 52 thiophene 52 and other five membered ring units. 53 The central five membered furan ring has also been replaced by the six member ones pyridine, 54 pyrimidine, [55][56][57] pyridazine, 53 and triazine. 58 These modifications have led to compounds with both potent DNA affinity and antimicrobial activity, however none appeared to be more advantageous than the furan analogs and a number showed much reduced activity.…”

Section: Antimicrobial Activity Of Furamidine and Its Analogsmentioning

confidence: 99%

Antimicrobial activity of the DNA minor groove binders furamidine and analogs

Boykin¹

2002

J. Braz. Chem. Soc.

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Análogos arílicos de diamidinas da pentamidina e do berenil que interagem com a fenda menor de DNA estão sendo sintetizados com amplo espectro de atividade antimicrobiana. Várias séries de análogos da furamidina, 1,5-bis[4-amidinofenil]furano foram descritas e apresentaram boa potência quando administradas de forma intravenosa. Entretanto, elas foram inativas quando administradas oralmente. As pró-drogas do tipo amidoxima e carbamato dessas furamidinas são potentes quando administradas oralmente. Atualmente uma dessas pró-drogas, a bis-O-metiloxima está em estudos clínicos de Fase II.Aryl diamidine analogs of pentamidine and berenil that bind to the minor groove of DNA have been developed which show broad spectrum antimicrobial activity. Several series of analogs of 2,5-bis[4-amidinophenyl]furan (furamidine) have been described which are quite effective when given intravenously, however they are ineffective on oral administration. Amidoxime and carbamate prodrugs of furamidine are quite effective when given orally. One of these prodrugs, a bis-O-methylamidoxime is currently in Phase II clinical trials.

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“…[1][2][3][4][5] A number of aromatic diamidines have been shown to bind to the minor groove of ORDER REPRINTS 2998 PAVLIČ IĆ AND KARMINSKI-ZAMOLA DNA and to exhibit useful antimicrobial activities. [6][7][8][9] A number of hypothesis for the mode of antimicrobial action of aryl diamidines have been proposed. 10 Recently, amidino-substituted-diphenyl-furans have been demonstrated diverse pharmacological activities.…”

Section: Introductionmentioning

confidence: 99%