scholarly journals Anti-Toxoplasma gondii Activities and Structure-Activity Relationships of Novel Fluoroquinolones Related to Trovafloxacin

1999 ◽  
Vol 43 (7) ◽  
pp. 1783-1787 ◽  
Author(s):  
Anis A. Khan ◽  
Fausto G. Araujo ◽  
Katherine E. Brighty ◽  
Thomas D. Gootz ◽  
Jack S. Remington
Keyword(s):  
Toxoplasma Gondii ◽  
Inhibitory Concentration ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Increased Activity

ABSTRACT Eleven novel fluoroquinolones closely related to trovafloxacin were evaluated for their in vitro activity against Toxoplasma gondii, and their structure-activity relationships were examined. The 50% inhibitory concentration (IC50) of trovafloxacin against T. gondii was 2.93 μM; the IC50 of the 11 analogs ranged from 0.53 to 14.09 μM. Six analogs had IC50s lower than that of trovafloxacin. Examination of the structure-activity relationships of the compounds revealed that addition of a -CH3 at C-5 of the 1,8-naphthyridone ring, at C-2 of the azabicyclohexane ring, or on the -NH2 at the 6 position of the azabicyclohexane ring resulted in a four- to sixfold increase in activity. Moreover, replacement of 2,4-difluorophenyl by cyclopropyl at N-1 of the 1,8-naphthyridone ring increased activity twofold, and moving the -NH2 one atom further away from the azabicyclohexane ring decreased activity. There was no difference between the naphthyridone and quinolone analogs. These results indicate that structure-activity studies of compounds related to drugs active against T. gondii may be useful in producing compounds with more potent activities against the parasite.

scholarly journals Novel Azolylalkyloxy Compounds with Antipicornaviral Activity

1995 ◽  
Vol 6 (4) ◽  
pp. 245-254 ◽  
Author(s):  
M. D. Abel ◽  
A. D. Cameron ◽  
C. M. Ha ◽  
C. A. Koski ◽  
H. T. Luu ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Optimal Length ◽  
Structure Activity Relationships ◽  
Structure Activity ◽  
Wide Range ◽  
Highly Effective ◽  
Qualitative Structure

A novel series of azolylalkyloxy compounds was designed, synthesized and evaluated for antipicornaviral activity. Several of the compounds exhibited in vitro activity comparable to that of Disoxarll. An investigation of qualitative structure-activity relationships indicated that the optimal length of the alkyI chain is six or seven carbon atoms, with seven being marginally superior. The effect of different azole moieties on activity was relatively small, with 3-methylisoxazole and 4-methylthiazole being most effective. The nature of the oxy substituent was found to be extremely important for antipicornaviral activity. The 2-dibenzofuryl group proved to be the most effective oxy substituent for this class of compounds. Compounds 11 and 22, combining dibenzofuran with 3-methylisoxazole and 4-methylthiazole, respectively, were highly effective in vitro against a wide range of human rhinoviruses as well as several enteroviruses.

Synthesis and structure–activity relationships of novel IKK-β inhibitors. Part 2: Improvement of in vitro activity

2004 ◽  
Vol 14 (15) ◽  
pp. 4013-4017 ◽  
Author(s):  
Toshiki Murata ◽  
Mitsuyuki Shimada ◽  
Hiroshi Kadono ◽  
Sachiko Sakakibara ◽  
Takashi Yoshino ◽  
...  
Keyword(s):  
Vitro Activity ◽  
In Vitro Activity ◽  
Structure Activity Relationships ◽  
Structure Activity

Comparison of the in Vitro Activity of Daptomycin and four other Antimicrobial Agents against Staphylococci Associated with CAPD Peritonitis

1988 ◽  
Vol 8 (4) ◽  
pp. 277-279
Author(s):  
Wendy L. Vaudry ◽  
Claudia Gratton ◽  
Kinga Kowalewska ◽  
Wanda M. Wenman
Keyword(s):  
Peritoneal Dialysis ◽  
Minimum Inhibitory Concentration ◽  
Continuous Ambulatory Peritoneal Dialysis ◽  
Antimicrobial Agents ◽  
Inhibitory Concentration ◽  
Vitro Activity ◽  
In Vitro Activity ◽  
Coagulase Negative Staphylococci ◽  
Vancomycin Resistant

The minimum inhibitory concentration (MIC) of daptomycin was compared with that of four other antimicrobial agents against clinically relevant staphylococci. Sixtyfive isolates were obtained from patients on continuous ambulatory peritoneal dialysis (CAPD) who contracted peritonitis. These isolates comprised 29 S. Sureus strains (all sensitive to oxacillin); 25 S. epidermidis strains (14 sensitive and 9 resistant to oxacillin); and 11 unspeciated coagulase-negative staphylococci (2 sensitive and 11 resistant to oxacillin). All of the oxacillin susceptible strains were inhibited by ≤2 mg/L of the five antibiotics tested. The oxacillin resistant staphylococci were also resistant to cefuroxime and variably resistant to cefamandole, but were uniformly susceptible to both vancomycin and daptomycin. Daptomycin possesses equivalent in vitro activity to vancomycin against strains of S. Sureus and coagulase negative staphylococci associated with CAPD peritonitis. If vancomycin resistance becomes a significant problem in these patients, and daptomycin is shown to be active against vancomycin resistant organisms, then it would have potential usefulness as an alternative to vancomycin in the treatment of peritonitis caused by multiply -resistant staphylococci.

New naphthoquinones and an alkaloid with in vitro activity against Toxoplasma gondii RH and EGS strains

2012 ◽  
Vol 132 (4) ◽  
pp. 450-457 ◽  
Author(s):  
Ronize Andréia Ferreira ◽  
Alaide Braga de Oliveira ◽  
Simone Andrade Gualberto ◽  
José M. Miguel Del Corral ◽  
Ricardo Toshio Fujiwara ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Vitro Activity ◽  
In Vitro Activity

In vitro activity of N-Phenyl-1,10-phenanthroline-2-amines against tachyzoites and bradyzoites of Toxoplasma gondii

2021 ◽  
pp. 116467
Author(s):  
Erica S. Martins-Duarte ◽  
Juliana de Araujo Portes ◽  
Ramon Borges da Silva ◽  
Hugo Silva Pires ◽  
Simon J. Garden ◽  
...  
Keyword(s):  
Toxoplasma Gondii ◽  
Vitro Activity ◽  
In Vitro Activity

scholarly journals In Vitro Activity of Oxazolidinone against Nontuberculous Mycobacteria, Including Macrolide-Resistant Clinical Isolates

2021 ◽  
Author(s):  
Dae Hun Kim ◽  
Su-Young Kim ◽  
Won-Jung Koh ◽  
Byung Woo Jhun
Keyword(s):  
Minimum Inhibitory Concentration ◽  
Inhibitory Concentration ◽  
Minimum Bactericidal Concentration ◽  
Nontuberculous Mycobacteria ◽  
Macrolide Resistance ◽  
Vitro Activity ◽  
Clinical Isolates ◽  
In Vitro Activity

We evaluated the in vitro activities of oxazolidinone antibiotics including linezolid, sutezolid, and delpazolid against clinical nontuberculous mycobacteria isolates. Regardless of macrolide resistance, for M. avium, M. intracellulare, and M. kansasii, sutezolid showed the lowest minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) value among oxazolidinone antibiotics. However, for M. abscessus, M. massiliense, the MIC and MBC values for all oxazolidinone antibiotics showed similar values. Oxazolidinone antibiotics warrant further investigation as potential antibiotics.

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