scholarly journals In-vitro activity of lytic peptides alone and in combination with macrolides and inhibitors of dihydrofolate reductase against Pneumocystis carinii

1998 ◽  
Vol 42 (4) ◽  
pp. 445-451 ◽  
Author(s):  
O. Cirioni ◽  
A. Giacometti ◽  
F. Barchiesi ◽  
G. Scalise
Keyword(s):  
Dihydrofolate Reductase ◽  
Pneumocystis Carinii ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Lytic Peptides

scholarly journals Enhanced In Vitro Activity of Dihydrofolate Reductase and Dihydropteroase Synthase Inhibitors in Combination against Nocardia spp

2003 ◽  
Vol 47 (3) ◽  
pp. 1174-1174 ◽  
Author(s):  
Deborah M. Thielking ◽  
Michelle S. Destefano ◽  
Michael H. Cynamon ◽  
Anthony E. T. Yeo
Keyword(s):  
Dihydrofolate Reductase ◽  
Vitro Activity ◽  
In Vitro Activity

scholarly journals In Vitro Activity of a Novel Diaminopyrimidine Compound, Iclaprim, against Chlamydia trachomatis and C. pneumoniae

2004 ◽  
Vol 48 (5) ◽  
pp. 1885-1886 ◽  
Author(s):  
S. A. Kohlhoff ◽  
P. M. Roblin ◽  
T. Reznik ◽  
S. Hawser ◽  
K. Islam ◽  
...  
Keyword(s):  
Chlamydia Trachomatis ◽  
Dihydrofolate Reductase ◽  
Reductase Inhibitor ◽  
Chlamydia Pneumoniae ◽  
Vitro Activity ◽  
Minimal Bactericidal Concentration ◽  
In Vitro Activity

ABSTRACT The in vitro activities of iclaprim, a novel dihydrofolate reductase inhibitor, azithromycin, and levofloxacin were tested against 10 strains of Chlamydia trachomatis and 10 isolates of Chlamydia pneumoniae. For C. trachomatis and C. pneumoniae, the iclaprim MIC and minimal bactericidal concentration at which 90% of isolates were inhibited (MIC90 and MBC90) were 0.5 μg/ml, compared to an azithromycin MIC90 and MBC90 of 0.125 μg/ml and levofloxacin MIC90s and MBC90s of 1 μg/ml for C. trachomatis and 0.5 μg/ml for C. pneumoniae.

scholarly journals Enhanced in vitro activity of WR99210 in combination with dapsone against Mycobacterium avium complex.

1996 ◽  
Vol 40 (11) ◽  
pp. 2644-2645 ◽  
Author(s):  
L M Shah ◽  
M S DeStefano ◽  
M H Cynamon
Keyword(s):  
Dihydrofolate Reductase ◽  
Mycobacterium Avium ◽  
Mycobacterium Avium Complex ◽  
Reductase Inhibitor ◽  
Vitro Activity ◽  
Dilution Method ◽  
In Vitro Activity ◽  
Fixed Concentration ◽  
Broth Dilution

WR99210, a dihydrofolate reductase inhibitor, has promising in vitro activity against Mycobacterium avium complex (MAC). The in vitro activities of WR99210 alone and in combination with a fixed concentration of dapsone (0.5 microgram/ml) were evaluated against 35 clinical MAC isolates by a broth dilution method. The MIC at which 50% of isolates were inhibited (MIC50) and MIC90 of WR99210 alone were 2 and 8 micrograms/ml, respectively. The MIC50 and MIC90 of WR99210 in combination with dapsone were 0.25 and 4 micrograms/ml, respectively. Overall, 75% of the MAC isolates displayed enhanced susceptibility to the combination.

scholarly journals In-vitro activity of topoisomerase inhibitors against Pneumocystis carinii

1997 ◽  
Vol 40 (4) ◽  
pp. 583-586 ◽  
Author(s):  
O. Cirioni ◽  
A. Giacometti ◽  
M. Quarta ◽  
G. Scalise
Keyword(s):  
Pneumocystis Carinii ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Topoisomerase Inhibitors

scholarly journals In-vitro activity of polycationic peptides against Cryptosporidium parvum, Pneumocystis carinii and yeast clinical isolates

1999 ◽  
Vol 44 (3) ◽  
pp. 403-406 ◽  
Author(s):  
Andrea Giacometti ◽  
Oscar Cirioni ◽  
Francesco Barchiesi ◽  
Francesca Caselli ◽  
Giorgio Scalise
Keyword(s):  
Cryptosporidium Parvum ◽  
Pneumocystis Carinii ◽  
Vitro Activity ◽  
Clinical Isolates ◽  
In Vitro Activity

scholarly journals Antimycobacterial Activities of 2,4-Diamino-5-Deazapteridine Derivatives and Effects on Mycobacterial Dihydrofolate Reductase

2000 ◽  
Vol 44 (10) ◽  
pp. 2784-2793 ◽  
Author(s):  
William J. Suling ◽  
Lainne E. Seitz ◽  
Vibha Pathak ◽  
Louise Westbrook ◽  
Esther W. Barrow ◽  
...  
Keyword(s):  
Dihydrofolate Reductase ◽  
Vitro Activity ◽  
Synthetic Approach ◽  
In Vitro Activity ◽  
Monocytic Cell ◽  
Aryl Group ◽  
Monocytic Cell Line ◽  
Immunodeficiency Virus ◽  
Pteridine Derivatives

ABSTRACT Development of new antimycobacterial agents for Mycobacterium avium complex (MAC) infections is important particularly for persons coinfected with human immunodeficiency virus. The objectives of this study were to evaluate the in vitro activity of 2,4-diamino-5-methyl-5-deazapteridines (DMDPs) against MAC and to assess their activities against MAC dihydrofolate reductase recombinant enzyme (rDHFR). Seventy-seven DMDP derivatives were evaluated initially for in vitro activity against one to three strains of MAC (NJ168, NJ211, and/or NJ3404). MICs were determined with 10-fold dilutions of drug and a colorimetric (Alamar Blue) microdilution broth assay. MAC rDHFR 50% inhibitory concentrations versus those of human rDHFR were also determined. Substitutions at position 5 of the pteridine moiety included -CH3, -CH2CH3, and -CH2OCH3 groups. Additionally, different substituted and unsubstituted aryl groups were linked at position 6 through a two-atom bridge of either -CH2NH, -CH2N(CH3), -CH2CH2, or -CH2S. All but 4 of the 77 derivatives were active against MAC NJ168 at concentrations of ≤13 μg/ml. Depending on the MAC strain used, 81 to 87% had MICs of ≤1.3 μg/ml. Twenty-one derivatives were >100-fold more active against MAC rDHFR than against human rDHFR. In general, selectivity was dependent on the composition of the two-atom bridge at position 6 and the attached aryl group with substitutions at the 2′ and 5′ positions on the phenyl ring. Using this assessment, a rational synthetic approach was implemented that resulted in a DMDP derivative that had significant intracellular activity against a MAC-infected Mono Mac 6 monocytic cell line. These results demonstrate that it is possible to synthesize pteridine derivatives that have selective activity against MAC.

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