In vitro antimicrobial activities of capuramycin analogues against non-tuberculous mycobacteria

Dubuisson, Tia; Bogatcheva, Elena; Krishnan, Manju Y.; Collins, Michael T.; Einck, Leo; Nacy, Carol A.; Reddy, Venkata M.

doi:10.1093/jac/dkq372

Cited by 41 publications

(30 citation statements)

References 24 publications

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“…Drug combinations having synergistic interactions are generally considered as more effective and, therefore, preferable [28]. Incidentally, EFNTE is proved to have synergistic effects with tylosin against S. typhimurium .…”

Section: Discussionmentioning

confidence: 99%

Synergistic Effect and Antiquorum Sensing Activity ofNymphaea tetragona(Water Lily) Extract

Hossain

Park

Kim

et al. 2014

BioMed Research International

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Salmonellosis is a common and widely distributed food borne disease where Salmonella typhimurium is one of the most important etiologic agents. The purpose of this study was to investigate the antimicrobial activity of Nymphaea tetragona alone and in combination with antibiotics against S. typhimurium. It also aimed to assess the plant for quorum sensing inhibition (QSI) activity and to identify the bioactive compounds. The antibacterial activities of the extract were assessed using broth microdilution method. Disk agar diffusion method was employed to determine the QSI and bioactive compounds were identified by GC-MS analysis. Ethyl acetate fraction of N. tetragona extract (EFNTE) demonstrated good antimicrobial activity (MIC 781 μg/mL) against 4 strains out of 5. FIC index ranged from 0.375 to 1.031 between EFNTE/tylosin and 0.515 to 1.250 between EFNTE/streptomycin against S. typhimurium. Among all extracts, EFNTE and butanol fraction more significantly inhibited pigment production of C. violaceum. Polyphenols were identified as major compound of EFNTE and butanol fraction. These results indicate that combination among N. tetragona extract and antibiotics could be useful to combat drug-resistance Salmonella infections and polyphenols are promising new components from N. tetragona that warrant further investigation as a candidate anti-Salmonella agent and quorum sensing inhibitor.

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Section: Discussionmentioning

confidence: 99%

Synergistic Effect and Antiquorum Sensing Activity ofNymphaea tetragona(Water Lily) Extract

Hossain

Park

Kim

et al. 2014

BioMed Research International

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“…Despite the number of new drugs being studied in pre-clinical and clinical trials for TB, they are being studied in combination drug regimens with other broad-spectrum antibiotics. Furthermore, these drugs, including DC-159a, 22 SQ-641, 23 CPZEN-45, 24 BTZ043, 25 bedaquiline, 26 and pretomanid 27 , lack bactericidal activity against many NTM species. The development of narrow-spectrum anti-mycobacterial drugs could revolutionize the treatment of both TB and NTM.…”

Section: 1 - Introductionmentioning

confidence: 99%

Design, synthesis and evaluation of indole-2-carboxamides with pan anti-mycobacterial activity

Franz

Belardinelli

Kaminski

et al. 2017

Bioorganic & Medicinal Chemistry

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Current treatment regimens for non-tuberculous mycobacteria (NTM) and tuberculosis (TB) generally require long duration of therapy with multiple drugs, some of which are broad spectrum antibiotics. Despite some advances in antimicrobial compounds, there remains a need in therapy for antibiotics with specific mycobacterial targets. It has been shown that MmpL3 is an essential transporter required for the translocation of mycolic acids to the mycobacterial cell envelope. Here, we synthesized a series of indole-2-carboxamides that inhibit MmpL3 and have potent pan-activity against mycobacterial species. The compounds were tested against several fast and slow-growing Mycobacterium species, including M. abscessus, M. massiliense, M. bolletii, M. chelonae, M. tuberculosis, M. avium, M. xenopi and M. smegmatis. The target of these indole compounds makes them selective for mycobacteria, while showing no clinically relevant bactericidal activity against S. aureus or P. aeruginosa. These compounds were tested against THP-1, a human-cell line, and showed minimal in vitro cytotoxicity and good selectivity indices. The data shown and discussed suggest that lead indole-2-carboxamides are strong contenders for further preclinical testing as NTM therapeutics.

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“…SQ-641 was shown to be bactericidal against different NTMs tested, with a minimum bactericidal concentration/MIC ratio ranging from 1 to 8 and killed all mycobacteria faster than positive control drugs for each strain, including clarithromycin, rifampicin, amikacin and streptomycin. In chequerboard titrations, SQ-641 was synergistic with ethambutol against both M. avium complex and Mycobacterium smegmatis, and was synergistic with streptomycin and rifabutin against M. abscessus (Dubuisson et al, 2010). Standard broth microdilution assay, as well as the agar dilution method, were performed to determine MICs for all strains.…”

Section: Sq-641mentioning

confidence: 99%

Challenges facing the drug discovery pipeline for non-tuberculous mycobacteria

Soni

Groote

Dasgupta

et al. 2016

Journal of Medical Microbiology

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In vitro antimicrobial activities of capuramycin analogues against non-tuberculous mycobacteria

Abstract: In vitro, SQ641 was the most potent of the capuramycin analogues against all NTM tested, both laboratory and clinical strains.

Cited by 41 publications

References 24 publications

Synergistic Effect and Antiquorum Sensing Activity ofNymphaea tetragona(Water Lily) Extract

Synergistic Effect and Antiquorum Sensing Activity ofNymphaea tetragona(Water Lily) Extract

Design, synthesis and evaluation of indole-2-carboxamides with pan anti-mycobacterial activity

Challenges facing the drug discovery pipeline for non-tuberculous mycobacteria

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