- Novel peptidomimetic peptide deformylase (PDF) inhibitors of Mycobacterium tuberculosis
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Emergence of MDR-TB and XDR-TB led to the failure of available anti-tubercular drugs. In order to explore, identify and develop new anti-tubercular drugs, novel peptidomimetic series of Mtb–peptide deformylase (PDF) inhibitors was designed and synthesized. In vitro antimycobacterial potential of compounds was established by screening of compounds against Mycobacterium tuberculosis H37Rv strain using MABA. Among them, ester series of compounds 4a, 4b, 4c, 4d, and 4e were found most active, with compound 4c being highly active and exhibiting minimum inhibitory concentration of 6.25?μg/ml against M.?tb H37Rv strain. Additionally, the compounds were docked to determine the probable binding interactions and understand the mechanism of action of most active molecules on Mtb-peptide deformylase (PDF), which is involved in the mycobacterium protein synthesis.
- Gokhale, Kunal M.,Telvekar, Vikas N.
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p. 148 - 156
(2020/08/26)
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- NOVEL CEPHEM DERIVATIVE
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Provided is a cephem compound which has a wide antimicrobial spectrum, and in particular exhibit potent antimicrobial activity against beta-lactamase producing Gram negative bacteria, and pharmaceutical composition comprising the same. A Compound of the f
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Paragraph 0307
(2013/04/24)
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- A new facile method for preparation of heterocyclic α-iminonitriles and α-oxoacetic acid from heterocyclic aldehydes, p-aminophenol, and sodium cyanide
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Very efficient, simple, and high yield procedures for the transformation of heterocyclic aldehydes into heterocyclic methylidene-p-hydroxyanilines, heterocyclic α-iminonitriles, and finally into heterocyclic α-oxoacetic acids were described. Considering that many of these compounds have biological activity, the synthetic methodology was optimized using readily available, inexpensive starting materials, and the purification of the product involved only simple crystallization.
- Jursic, Branko S.,Douelle, Frederic,Bowdy, Katherine,Stevens, Edwin D.
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p. 5361 - 5365
(2007/10/03)
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- Tetracyclic spiro-hydantoin aldose reductase inhibitors and compositions
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Novel biologically-active tetracyclic spiro-hydantoin derivatives which are potent inhibitors of aldose reductase and useful in treating diabetic complications are disclosed. Pharmaceutical compositions containing the novel compounds and a method of treat
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