Synthesis and medicinal chemistry of selected antitubercular natural products and natural product derivatives

Mahajan, Aman; Hans, Renate; Chibale, Kelly; Kumar, Vipan

doi:10.1039/c3ra46124f

Cited by 5 publications

(3 citation statements)

References 318 publications

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“…A Case Study -Antitubercular Agents A particular area in which natural product isolation and synthesis has remained both popular and productive is in the discovery of antitubercular agents, [136,137] and while terpenoid [138] and coumarin [139] systems are well known, newer structures continue to be found (Figures 3 and 4).…”

Section: Aureus Infection[135]mentioning

confidence: 99%

Natural Products as a Source for Novel Antibiotics

Moloney

2016

Trends in Pharmacological Sciences

238

163

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Natural products have historically been of crucial importance in the identification and development of antibacterial agents. Interest in these systems has waned in recent years, but the rapid emergence of resistant bacterial strains has forced their re-evaluation as a route to identify novel chemical skeletons with antibacterial activity for elaboration in drug development. This overview examines the current situation, highlights new natural product systems which have been found, together with re-examination of some old ones, and new technologies for their identification. While natural products certainly have the potential to re-emerge as a key start-point in antibacterial drug discovery, reports of new or reinvestigated structures need to be supported with sufficient quality chemical (solubility, stability), biochemical (including toxicity in particular, along with target information) and microbiological [minimum inhibitory concentration (MIC) and resistance frequency] validation data to assist in the identification of promising hit structures and to avoid wasted effort from trawling over already cultivated territory. This is particularly important in a resource-limited research environment.

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Section: Aureus Infection[135]mentioning

confidence: 99%

Natural Products as a Source for Novel Antibiotics

Moloney

2016

Trends in Pharmacological Sciences

238

163

View full text Add to dashboard Cite

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“…To combat this trend, the discovery, development and remodeling of drugs against multi-drug-resistant bacterial strains is desperately needed. 2,3 The type II fatty acid synthase (FAS II) pathway of lipid biosynthesis is an attractive antibacterial target because it involves essential processes for bacterial proliferation that are distinct from the FAS pathway present in mammalian cells. 4 The iterative cycles of condensation, reduction and dehydration in the FAS II pathway have been extensively studied in bacteria and many of their conserved proteins have been previously targeted with antibacterial agents such as cerulenin 5 , isoniazid 6 or triclosan 7 (Figure 1).…”

Section: Introductionmentioning

confidence: 99%

“…The crucial biotransformation towards 4 is a series of oxidations catalyzed by TtmP, which selectively oxidizes the terminal methyl group of 2 three times to synthesize thiotetromycin carboxylic acid (3). The carboxylic acid substrate 3 is further transformed into 4 by amidotransferase TtmN in the presence of ATP, L-glutamine and Mg 2+ (Figure 1).…”

Section: Introductionmentioning

confidence: 99%