Novel Broad-Spectrum Bis-(Imidazolinylindole) Derivatives with Potent Antibacterial Activities against Antibiotic-Resistant Strains

Panchal, Rekha G.; Ulrich, Ricky L.; Lane, Douglas; Butler, Michelle M.; Houseweart, Chad; Opperman, Timothy J.; Williams, John D.; Peet, Norton P.; Moir, Donald T.; Nguyen, Tam Luong; Gussio, Rick; Bowlin, Terry L.; Bavari, Sina

doi:10.1128/aac.01709-08

Cited by 48 publications

(62 citation statements)

References 23 publications

Supporting

Mentioning

Contrasting

Unclassified

Order By: Relevance

“…Although effective against bubonic plague, this vaccine was not efficiently protective against pneumonic plague and caused significant side effects (11). The emergence of multiple antimicrobial resistance in Y. pestis (72) and the lack of a safe and effective vaccine have been the impetus for the search for new inhibitory drugs as well as a better vaccine (48,49).…”

mentioning

confidence: 99%

Biosafety Level 2 Model of Pneumonic Plague and Protection Studies with F1 and Psa

et al. 2010

View full text Add to dashboard Cite

Attenuated Yersinia pestis pgm strains, such as KIM5, lack the siderophore yersiniabactin. Strain KIM5 does not induce significant pneumonia when delivered intranasally. In this study, mice were found to develop pneumonia after intranasal challenge with strain KIM5 when they were injected intraperitoneally with iron dextran, though not with iron sulfate. KIM5-infected mice treated daily with 4 mg iron dextran died in 3 days with severe pneumonia. Pneumonia was less severe if 4 mg iron dextran was administered only once before infection. The best-studied experimental vaccine against plague currently consists of the Yersinia pestis capsular antigen F1 and the type 3 secreted protein LcrV. The F1 antigen was shown to be protective against KIM5 infections in mice administered iron dextran doses leading to light or severe pneumonia, supporting the use of an iron dextran-treated model of pneumonic plague. Since F1 has been reported to be incompletely protective in some primates, and bacterial isolates lacking F1 are still virulent, there has been considerable interest in identifying additional protective subunit immunogens. Here we showed that the highly conserved Psa fimbriae of Y. pestis (also called pH 6 antigen) are expressed in murine organs after infection through the respiratory tract. Studies with iron dextran-treated mice showed that vaccination with the Psa fimbrial protein together with an adjuvant afforded incomplete but significant protection in the mouse model described. Therefore, further investigations to fully characterize the protective properties of the Psa fimbriae are warranted.

show abstract

mentioning

confidence: 99%

Biosafety Level 2 Model of Pneumonic Plague and Protection Studies with F1 and Psa

et al. 2010

View full text Add to dashboard Cite

show abstract

“…They are a very important category of compounds that play a key role in cell physiology and are probable intermediates for numerous biological reactions. Indole derivatives correspond to scores of important modules of therapeutic agents in medicinal chemistry such as anti-cancer [22] , anti-oxidant [23] , anti-rheumatoidal [24] , anti-HIV [25,26] , anti-microbial [27][28][29] , anti-inflamatory [30] , analgesic [31] , antipyretic [32] , anti-convulsant [33,34] , anthelmintic cardiovascular [35] , selective COX-2(cyclooxygenase-2) inhibitory activities [36][37][38][39] (which is an enzyme accountable for inflammation and pain) and DNA binding ability [40] . Furthermore, countless essential indole derivatives are used in disease management, for example, the non-steroidal anti-inflammatory drug indomethacin (Indocin ® ), the beta blocker pindolol (Viskin ® ) for management of high blood pressure (hypertension), the psychedelic, dimethyltryptamine (DMT) [41] and…”

Section: Indoles In Medicinal Chemistrymentioning

confidence: 99%

Indoles as anticancer agents

et al. 2015

View full text Add to dashboard Cite

show abstract

“…[3][4][5] Among different structures, notable attention has been given to rational design, synthesis and characterisation of the structure-activity relationship of diarylamidines, small molecules that bind through noncovalent interaction to the minor groove of B-DNA. [6][7][8] Diarylamidines have a wide range of potential therapeutic applications, such as ACIS inhibitors, 9 antiparasitic, 10,11 antifungal, 12 antibacterial, 13,14 antiviral 15 and anticancer agents. 4,6,16,17 Until now, pentamidine, 1,5-bis(4-amidinophenoxy)pentane, is the only one of this class with significant human clinical use.…”

Section: Introductionmentioning

confidence: 99%

Synthesis, DNA Interactions and Anticancer Evaluation of Novel Diamidine Derivatives of 3,4-Ethylenedioxythiophene

Stolić¹,

Avdičević²,

Bregović³

et al. 2012

Croat. Chem. Acta

View full text Add to dashboard Cite

Abstract. Eight novel diamidino 3,4-ethylenedioxythiophene-2,5-dicarboxanilides (5a-h), obtained by condensation reaction of 3,4-ethylenedioxythiophene-2,5-dicarbonyl chloride and corresponding 3-or 4-aminobenzamidines, were evaluated for interactions with double-stranded DNA and RNA, and their cytotoxicity was assayed against the panel of human cancer cell lines. All compounds preferentially bind into the minor groove of DNA and had higher affinity for DNA than for RNA. Compounds 5a-h showed a moderate antiproliferative effect toward the panel of seven carcinoma cells line, whereby the highest inhibitory potential was displayed by compound 5a with unsubstituted amidino moieties in para position.

show abstract

Novel Broad-Spectrum Bis-(Imidazolinylindole) Derivatives with Potent Antibacterial Activities against Antibiotic-Resistant Strains

Cited by 48 publications

References 23 publications

Biosafety Level 2 Model of Pneumonic Plague and Protection Studies with F1 and Psa

Biosafety Level 2 Model of Pneumonic Plague and Protection Studies with F1 and Psa

Indoles as anticancer agents

Synthesis, DNA Interactions and Anticancer Evaluation of Novel Diamidine Derivatives of 3,4-Ethylenedioxythiophene

Contact Info

Product

Resources

About