scholarly journals In vitro activity and mechanism of action of A21978C1, a novel cyclic lipopeptide antibiotic.

1985 ◽  
Vol 27 (3) ◽  
pp. 357-362 ◽  
Author(s):  
G M Eliopoulos ◽  
C Thauvin ◽  
B Gerson ◽  
R C Moellering
Keyword(s):  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Cyclic Lipopeptide ◽  
Lipopeptide Antibiotic

scholarly journals Diphenyl Furans and Aza Analogs: Effects of Structural Modification on In Vitro Activity, DNA Binding, and Accumulation and Distribution in Trypanosomes

2007 ◽  
Vol 51 (8) ◽  
pp. 2801-2810 ◽  
Author(s):  
Amanda M. Mathis ◽  
Arlene S. Bridges ◽  
Mohamed A. Ismail ◽  
Arvind Kumar ◽  
Iris Francesconi ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Structural Modification ◽  
Human African Trypanosomiasis ◽  
Treatment Options ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Antitrypanosomal Activity ◽  
Specific Accumulation ◽  
High Concentrations

ABSTRACT Human African trypanosomiasis is a devastating disease with only a few treatment options, including pentamidine. Diamidine compounds such as pentamidine, DB75, and DB820 are potent antitrypanosomal compounds. Previous investigations have shown that diamidines accumulate to high concentrations in trypanosomes. However, the mechanism of action of this class of compounds remains unknown. A long-hypothesized mechanism of action has been binding to DNA and interference with DNA-associated enzymes. The fluorescent diamidines, DB75 and DB820, have been shown to localize not only in the DNA-containing nucleus and kinetoplast of trypanosomes but also to the acidocalcisomes. Here we investigate two series of analogs of DB75 and DB820 with various levels of in vitro antitrypanosomal activity to determine whether any correlation exists between trypanosome accumulation, distribution, and in vitro activity. Despite wide ranges of in vitro antitrypanosomal activity, all of the compounds investigated accumulated to millimolar concentrations in trypanosomes over a period of 8 h. Interestingly, some of the less potent compounds accumulated to concentrations much higher than those of more potent compounds. All of the compounds were localized to the DNA-containing nucleus and/or kinetoplast, and many were also found in the acidocalcisomes. Accumulation in the nucleus and kinetoplast should be important to the mechanism of action of these compounds. The acidocalcisomes may also play a role in the mechanism of action of these compounds. This investigation suggests that the extent of accumulation alone is not responsible for killing trypanosomes and that organelle-specific accumulation may not predict in vitro activity.

scholarly journals Design, Synthesis and In Vitro Activity of Anticancer Styrylquinolines. The p53 Independent Mechanism of Action

PLoS ONE ◽  
2015 ◽  
Vol 10 (11) ◽  
pp. e0142678 ◽  
Author(s):  
Anna Mrozek-Wilczkiewicz ◽  
Ewelina Spaczynska ◽  
Katarzyna Malarz ◽  
Wioleta Cieslik ◽  
Marzena Rams-Baron ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Design Synthesis ◽  
Independent Mechanism

scholarly journals In vitro activity and mechanism of action of a duplex and multidrug of ethynylcytidine and 5-fluorodeoxyuridine

2008 ◽  
Vol 52 (1) ◽  
pp. 651-651 ◽  
Author(s):  
I. Bijnsdorp ◽  
R. Schwendener ◽  
H Schott ◽  
S Schott ◽  
I Fichtner ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vitro Activity

Mechanism of action and in vitro activity of short hybrid antimicrobial peptide PV3 against Pseudomonas aeruginosa

2016 ◽  
Vol 479 (1) ◽  
pp. 103-108 ◽  
Author(s):  
Hamed Memariani ◽  
Delavar Shahbazzadeh ◽  
Jean-Marc Sabatier ◽  
Mojtaba Memariani ◽  
Ali Karbalaeimahdi ◽  
...  
Keyword(s):  
Pseudomonas Aeruginosa ◽  
Antimicrobial Peptide ◽  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vitro Activity

ChemInform Abstract: In vivo and in vitro Activity and Mechanism of Action of the Multidrug Cytarabine-L-glycerylyl-fluorodeoxyuridine

ChemInform ◽  
2008 ◽  
Vol 39 (13) ◽  
Author(s):  
Irene V. Bijnsdorp ◽  
Reto A. Schwendener ◽  
Herbert Schott ◽  
Iduna Fichtner ◽  
Kees Smid ◽  
...  
Keyword(s):  
Mechanism Of Action ◽  
Vitro Activity ◽  
In Vitro Activity
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