4-Thiazolidinones: novel inhibitors of the bacterial enzyme murB

Andres, C. J.; Bronson, Joanne J.; D’Andrea, Stanley V.; Deshpande, Milind; Falk, Paul; Grant-Young, Katharine A.; Harte, William E.; Ho, Hsu Tso; Misco, Peter F.; Robertson, James G.; Stock, David A.; Sun, Yaxiong; Walsh, Ann W.

doi:10.1016/s0960-894x(00)00073-1

Cited by 212 publications

(90 citation statements)

References 13 publications

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“…Phosphinate transition-state analogs of the MurC to -F enzymes were synthesized by various groups in the 1990s, and some of these showed potent enzyme inhibition (at low nanomolar levels for some, illustrating druggability of the targets) but no antibacterial activity, presumably due to a lack of cell entry (127,254,310,362,403). A number of inhibitors of MurB, -C, -D, and -F, found via screens for enzyme inhibition or binding, had micromolar (in some cases, low micromolar) 50% inhibitory concentrations (IC 50 s) and no (or weak in one case [370]) antibacterial activity (11,30,103,141,364,370).…”

Section: Murb To Murf Enzymes As Antibacterial Targetsmentioning

confidence: 99%

Challenges of Antibacterial Discovery

Silver¹

2011

Clin Microbiol Rev

1,155

961

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SUMMARY The discovery of novel small-molecule antibacterial drugs has been stalled for many years. The purpose of this review is to underscore and illustrate those scientific problems unique to the discovery and optimization of novel antibacterial agents that have adversely affected the output of the effort. The major challenges fall into two areas: (i) proper target selection, particularly the necessity of pursuing molecular targets that are not prone to rapid resistance development, and (ii) improvement of chemical libraries to overcome limitations of diversity, especially that which is necessary to overcome barriers to bacterial entry and proclivity to be effluxed, especially in Gram-negative organisms. Failure to address these problems has led to a great deal of misdirected effort.

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Section: Murb To Murf Enzymes As Antibacterial Targetsmentioning

confidence: 99%

Challenges of Antibacterial Discovery

Silver¹

2011

Clin Microbiol Rev

1,155

961

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“…4-Thiazolidinone derivatives among heterocyclic ring systems have been reported to possess various biological properties such as anticancer (18), anti-inflammatory (19,20), antibacterial (21,22), antioxidant (23), anticonvulsant (24), antiviral (25), antimicrobial (26) and antifungal activities (27). The following 1,3-thiazolidin-4-on derivatives are used in medicine: ralitoline (anticonvulsant), piprozolin (choleretic), etozolin, ozolinone (diuretic), dexetozolin (antihypertensive), mezolidon (antiulcer) (28)(29)(30).…”

Section: Introductionmentioning

confidence: 99%

Tiyoüreler, açiltiyoüreler ve 4-tiyazolidinonların sentezi, karakterizasyonu ve antikanser ve antiviral etkilerinin değerlendirilmesi

Kulabaş¹,

Özakpınar²,

Özsavcı³

et al. 2017

Marmara Pharmaceutical Journal

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In this study, thiourea derivatives [1][2][3][4] were synthesized by using 2-amino-4-substituted pyridine compounds and these compounds have been used as the starting materials for synthesis of 2-imino-1,3-thiazolidin-4-one ring [5,6]. Two different procedures for 4-thiazolidinone ring closure and synthesis method were optimized. The synthesized compounds were identified by the help of elemental analysis, IR, 1 H-NMR, 13 C-NMR and mass spectral data while the purities of them were proved with TLC. Synthesized compounds were evaluated for their antiviral and anticancer activity. Antiviral activity against Murine norovirus, Yellow fever, Enterovirus and Chikungunya strains of the test compounds were investigated and EC 50 values of these compounds were determined higher than 0,3 µM. Cytotoxicity of test compounds was examined on NIH3T3 cell line. When the anticancer activity of test compounds was examined against PC-3, A549, HeLa, HT-29, MCF-7, SJSA1 and K562 cell lines, the percent proliferation values of these compounds were observed over 61% for all cell lines.

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“…In this study, we extend these earlier investigations to thiazolidines, a class of derivatives which have been reported to possess a wide range of biological activities including antibacterial, antitumor, and anti-inflammatory activity [13][14][15][16] . In the present study, we have purified human CA I and II from fresh blood and examined the in vitro inhibition effects of some thiazolidin derivative compounds mentioned above on these enzymes, using the esterase activity of hCA I and hCA II, with 4-nitrophenyl acetate as substrate.…”

Section: Introductionmentioning

confidence: 84%