Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents

Bekhit, Adnan A.; Farghaly, A. M.; Shafik, R. M.; El-Semary, Mona M.; Bekhit, Alaa El‐Din A.; Guemei, Aida A.; El-Shoukrofy, Mai S.; Ibrahim, Tamer M.

doi:10.1016/j.bioorg.2017.12.028

Cited by 29 publications

(10 citation statements)

References 41 publications

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“…Accordingly and as a continuation of our efforts to discover diverse chemotypes for potential antibacterial agents, 32 we aim at preparing new triazolo[1,5- a ]pyrimidine derivatives coupled with amino acids. The synthetic process comprises green conditions, e.g.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

et al. 2021

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Section: Introductionmentioning

confidence: 99%

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

et al. 2021

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“…These are prominent bioisosteres to purines and have turned out to be an eye-catching structural component in the advancement of pharmaceutical molecules. Owing to their broad array of applicability such as anticancer, 214,215 antiviral, 216 anti-inflammatory, [217][218][219] antimicrobial, 218,220 this scaffold has inspired various medicinal chemistry scientists for the synthesis of various thienopyrimidine scaffolds. 29 The thienopyrimidine nucleus is considered as a bioisostere of the quinazoline core and thus regarded to possess similar biological profiles.…”

Section: Thienopyrimidinementioning

confidence: 99%

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Laxmikeshav

Kumari

Shankaraiah

2021

Medicinal Research Reviews

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This review article proposes a comprehensive report of the design strategies engaged in the development of various sulfur-bearing cytotoxic agents. The outcomes of various studies depict that the sulfur heterocyclic framework is a fundamental structure in diverse synthetic analogs representing a myriad scope of therapeutic activities. A number of five-, six-and seven-membered sulfur-containing heterocyclic scaffolds, such as thiazoles, thiadiazoles, thiazolidinediones, thiophenes, thiopyrans, benzothiazoles, benzothiophenes, thienopyrimidines, simple and modified phenothiazines, and thiazepines have been discussed. The subsequent studies of the derivatives unveiled their cytotoxic effects through multiple mechanisms (viz. inhibition of tyrosine kinases, topoisomerase I and II, tubulin, COX, DNA synthesis, and PI3K/Akt and Raf/MEK/ERK signaling pathways), and several others. Thus, our concise illustration explains the design strategy and anticancer potential of these five-and six-membered sulfur-containing heterocyclic molecules along with a brief outline on seven-membered sulfur heterocycles. The thorough assessment of antiproliferative activities with the reference drug allows a proficient assessment of the structure-activity relationships (SARs) of the diversely synthesized molecules of the series.

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“…Unfortunately, few drugs possessed these two activities in a single compound. Therefore, there are continuous trails to develop a monotherapy against inflammation due to microbial infection (dual antimicrobial/ anti-inflammatory agent) with minimal adverse effects and high safety margin [3].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: multi-target compounds with dual antimicrobial and anti-inflammatory activities

et al. 2020

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Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were assessed for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound 7g was identified to be the most potent antibacterial candidate against strains of MRSA, E. coli, K. pneumoniae, P. aeruginosa, and A. baumannii, respectively, with safe therapeutic dose. Compounds 7a-k, 8a-c, and 9a-c showed good antiinflammatory activity with excessive selectivity towards COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds 9a-c were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds 7b, 7h, and 7i into COX-2 active site was correlated with the results of in vitro COX-2 inhibition assays.

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Synthesis, biological evaluation and molecular modeling of novel thienopyrimidinone and triazolothienopyrimidinone derivatives as dual anti-inflammatory antimicrobial agents

Cited by 29 publications

References 41 publications

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-a]pyrimidines bearing amino acid moiety

Expedition of sulfur‐containing heterocyclic derivatives as cytotoxic agents in medicinal chemistry: A decade update

Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: multi-target compounds with dual antimicrobial and anti-inflammatory activities

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