Biological and Pharmacological Activity of Thiophene and its Derivatives

Blicke, F. F.

doi:10.1002/9780470186527.ch2

Cited by 3 publications

(2 citation statements)

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“…In this process, a precursor analogue has to be fed to the producing microorganism to produce a new product (Kennedy 2007). Previously, propargyl-premonensin was produced with the addition of propargyl-malonyl-N-acetyl-cysteamine to fermentation broth of Streptomyces cinnamonensis A495 (Blicke 1952). There are some known biologically active and medicinally useful heterocyclic molecules which act as precursors in PCB for the synthesis of new drugs (Kennedy 2007;Tran et al 2012).…”

Section: Introductionmentioning

confidence: 99%

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Precursor-directed combinatorial biosynthesis of cephalosporin analogue by endolithic actinobacterium Streptomyces sp. AL51 by utilizing thiophene derivative

et al. 2017

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Natural products or their derivatives provide a reliable resource for new drugs. The multi-step chemical reaction to produce new drug is not only expensive but also release pollutants. The precursor-based combinatorial biosynthesis (PCB) is, however, a better option to produce novel natural products with potential pharmaceutical applications. The present work is an attempt to synthesize an antibacterial compound by transforming thiophene precursor using endolithic sp. AL51. The sp. AL51 was isolated from a granite rock sample collected from Mylliem, Meghalaya, India. The isolate was identified as sp. based on its cultural, morphological, biochemical and molecular characteristics. The bioactive compound CAx1 was extracted from the fermentation broth. The compound was characterized by bioactivity-guided fractionation and identified by infrared, UV-visible, nuclear magnetic resonance and mass spectrometry data and identified as 7-[1-(thiophene-5-yl)-1-formamido]-3-propylenyl-3-cephem-4-carboxylic acid with molecular formula CHNOS. The purified compound showed considerable in vitro antibacterial activity against both Gram-positive and Gram-negative bacteria showing its broad spectrum property. The obtained results provide promising baseline information for the potential use of endolithic actinobacterium for semisynthetic drug discovery. This is the first report on PCB of broad range antibacterial compound by endolithic strain.

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Section: Introductionmentioning

confidence: 99%

“…These thiophene derivatives are well known for therapeutic application (Mabkhot et al 2016). It has been found that some thiophene derivatives can also act as precursors in the biosynthesis of antibiotics when they are supplemented to the fermentation medium (Blicke 1952).…”

Section: Introductionmentioning

confidence: 99%