Study on N-(pyridin-4-Yl) Salicylamides as Antimycobacterial Agents

A series of N-(pyridin-4-yl) salicylamides derivatives were prepared through acylation of the corresponding acetylsalicyloyl chlorides with substituted 4-amino-pyridines. These compounds were evaluated in vitro for antimycobacterial activities against Mycobacterium tuberculosis (TB) and Mycobacterium avium (A) by the minimum inhibitory concentrations (MIC) values. Eight of the compounds exhibited lower MIC against A than isoniazide (INH). Meanwhile, four of the compounds exhibited good anti-TB activity, when they were compared with INH. Antimycobacterial activities of N-(pyridin-4-yl) salicylamides were influenced by the balance between hydrophobicity and electron-withdrawing substituent effect on the phenyl and pyridine ring. These studies show that these compounds might serve as prospective wide-spectrum antimycobacterial substances.

Download Full-text

The efficacy of the disinfection of bronchoscopes contaminated in vitro with Mycobacterium tuberculosis and Mycobacterium avium-intracellulare in sputum: a comparison of Sactimed-I-Sinald and glutaraldehyde

Journal of Hospital Infection ◽

10.1016/0195-6701(95)90272-4 ◽

1995 ◽

Vol 29 (4) ◽

pp. 257-264 ◽

Cited By ~ 15

Author(s):

G. Nicholson ◽

R.A. Hudson ◽

M.V. Chadwick ◽

H. Gaya

Keyword(s):

Mycobacterium Tuberculosis ◽

Mycobacterium Avium ◽

Mycobacterium Avium Intracellulare

Download Full-text

SYNTHESIS AND ANTITUBERCULAR ACTIVITY OF PIPERIDINE AND MORPHOLINE 1, 8 NAPHTHYRIDINE ANALOGUES

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2016v8i12.13503 ◽

2016 ◽

Vol 8 (12) ◽

pp. 252 ◽

Cited By ~ 2

Author(s):

Muwaffag Badawneh ◽

Jalal Aljamal

Keyword(s):

Mycobacterium Tuberculosis ◽

Inhibitory Concentration ◽

Antitubercular Activity ◽

Antimycobacterial Activity ◽

Significant Activity ◽

Reference Drug ◽

Novel Drugs ◽

Elemental Analyses ◽

Antimycobacterial Agents

Objective: The search for new, potentially useful antimycobacterial agents. In continuation with our previous screening for the discovery of novel drugs for tuberculosis, a new series of 1,8-naphthyridines derivatives were synthesized and evaluated in vitro for antimycobacterial activity against Mycobacterium tuberculosis H37Rv.Methods: Several 4-morpholinomethyl-1.8-naphthyridine derivatives have been synthesized in excellent yields. The synthesized compounds were characterized by spectroscopic methods as well as elemental analyses. They were screened for their antimycobacterial activity. The growth was monitored radiometrically in 7H12 broth with the BACTEC 460 TB system. The minimum inhibitory concentration (MIC) was determined for compounds that demonstrated ≥ 90% growth inhibition in the primary screening.Results: The obtained data suggested that all compounds showed significant activity against Mycobacterium tuberculosis H37Rv compared to the standard reference drug. Analogues (6-11) having heterocyclic groups in position 7 were the most potent of those we tested.Conclusion: These findings clearly identify the 1,8-naphthyridine analogue (10) with a 6-amino-2-(4'-methoxy benzylamine-4-morpholinomethyl-7-morpholino-substituent as promising anti-tubercular agents possessing significant activity against Mycobacterium tuberculosis H37Rv

Download Full-text

Antimycobacterial activity of 1-deaza-7,8-dihydropteridine derivatives against Mycobacterium tuberculosis and Mycobacterium avium complex in vitro

Journal of Antimicrobial Chemotherapy ◽

10.1093/jac/47.4.451 ◽

2001 ◽

Vol 47 (4) ◽

pp. 451-454 ◽

Cited By ~ 14

Author(s):

W. J. Suling

Keyword(s):

Mycobacterium Tuberculosis ◽

Mycobacterium Avium ◽

Mycobacterium Avium Complex ◽

Antimycobacterial Activity

Download Full-text

Determination of in vitro susceptibility of Mycobacterium avium complex isolates to antimycobacterial agents by various methods.

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.31.11.1697 ◽

1987 ◽

Vol 31 (11) ◽

pp. 1697-1702 ◽

Cited By ~ 50

Author(s):

C B Inderlied ◽

L S Young ◽

J K Yamada

Keyword(s):

Mycobacterium Avium ◽

Mycobacterium Avium Complex ◽

In Vitro Susceptibility ◽

Antimycobacterial Agents

Download Full-text

Bioluminescence screening in vitro (Bio-Siv) assays for high-volume antimycobacterial drug discovery.

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.40.6.1536 ◽

1996 ◽

Vol 40 (6) ◽

pp. 1536-1541 ◽

Cited By ~ 40

Author(s):

T M Arain ◽

A E Resconi ◽

M J Hickey ◽

C K Stover

Keyword(s):

Mycobacterium Tuberculosis ◽

Drug Discovery ◽

High Volume ◽

Luciferase Gene ◽

Direct Identification ◽

Mycobacterium Intracellulare ◽

Large Numbers ◽

Antimycobacterial Agents ◽

Screening In Vitro

Bioluminescence-based assays to indicate antimicrobial susceptibility have been developed and validated for recombinant strains of Mycobacterium tuberculosis, Mycobacterium bovis BCG, Mycobacterium avium, and Mycobacterium intracellulare expressing an integrated eukaryotic luciferase gene. MICs determined with these bioluminescence assays for several antimycobacterial agents, including isoniazid, ethambutol, rifampin, amikacin, streptomycin, ciprofloxacin, and clarithromycin, compared favorably with traditional BACTEC methods and visual estimations of the inhibitory end point. Assay methodology has been optimized for the analysis of large numbers of novel compounds and is simple, inexpensive, and labor efficient. The availability of these four recombinant mycobacteria has permitted a strategy for drug discovery employing the nonpathogenic BCG strain for mass screening purposes with subsequent confirmation of activity against the pathogenic mycobacteria. Furthermore, evidence suggests that the BCG-based screen may allow the direct identification of bactericidal agents.

Download Full-text

Differential Gene Expression in Response to Exposure to Antimycobacterial Agents and Other Stress Conditions among Seven Mycobacterium tuberculosis whiB-Like Genes

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.00295-06 ◽

2006 ◽

Vol 50 (8) ◽

pp. 2836-2841 ◽

Cited By ~ 131

Author(s):

Deborah E. Geiman ◽

Tirumalai R. Raghunand ◽

Nisheeth Agarwal ◽

William R. Bishai

Keyword(s):

Mycobacterium Tuberculosis ◽

Stress Conditions ◽

Pcr Analysis ◽

Reverse Transcription Pcr ◽

Small Proteins ◽

Antimycobacterial Agents ◽

Differential Gene ◽

Biochemical Analyses ◽

In Vitro Stress

ABSTRACT The seven Mycobacterium tuberculosis whiB-like genes encode small proteins postulated to be transcriptional regulators. A systematic real-time reverse transcription-PCR analysis following exposure to antibiotics and a variety of growth and in vitro stress conditions indicates differential, and in some cases dramatic, transcription modulations for the different M. tuberculosis whiB family members. This information together with biochemical analyses of the whiB1 to whiB7 gene products will be important for understanding the biology of this novel family of proteins in mycobacteria and related actinomycetes.

Download Full-text

Comparative antimycobacterial activities of rifampin, rifapentine, and KRM-1648 against a collection of rifampin-resistant Mycobacterium tuberculosis isolates with known rpoB mutations.

Antimicrobial Agents and Chemotherapy ◽

10.1128/aac.40.11.2655 ◽

1996 ◽

Vol 40 (11) ◽

pp. 2655-2657 ◽

Cited By ~ 69

Author(s):

S L Moghazeh ◽

X Pan ◽

T Arain ◽

C K Stover ◽

J M Musser ◽

...

Keyword(s):

Mycobacterium Tuberculosis ◽

Rna Polymerase ◽

Gene Mutations ◽

Rpob Gene ◽

Genetic Alterations ◽

Beta Subunit ◽

Polymerase Beta ◽

Antimycobacterial Agents ◽

Rifampin Resistance

A collection of 24 rifampin-resistant clinical isolates of Mycobacterium tuberculosis with characterized RNA polymerase beta-subunit (rpoB) gene mutations was tested against the antimycobacterial agents rifampin, rifapentine, and KRM-1648 to correlate levels of resistance with specific rpoB genotypes. The results indicate that KRM-1648 is more active in vitro than rifampin and rifapentine, and its ability to overcome rifampin resistance in strains with four different genetic alterations may prove to be useful in understanding structure-function relationships.

Download Full-text