Synthesis and biological evaluation of ciprofloxacin – 1,2,3-triazole hybrids as antitumor, antibacterial, and antioxidant agents

Al-Taweel, Samir; Al-Saraireh, Yousef; Al-Trawneh, Salah; Alshahateet, Solhe; Al- Tarawneh, Rakan; Ayed, Nadaa; Alkhojah, Mohammad; AL-Khaboori, Wisam; Zereini, Wael; Al-Qaralleh, Omar

doi:10.1016/j.heliyon.2023.e22592

Cited by 10 publications

(1 citation statement)

References 45 publications

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“…Researchers are interested in lead compounds made of 1,2,3-triazoles with heterocycles because they have a variety of biological properties, including being antibacterial, antifungal, anticonvulsant, antimalarial, antitubercular, anticancer, antiviral, anti-diabetic, anti-HIV, anti-inflammatory, analgesic, and dipole-dipole bonds with various enzymes, proteins, and receptors. [20][21][22][23][24][25][26][27] 1,2,3triazoles as heterocyclic compounds with excellent yield, and this reaction is valuable because azides and acetylacetone are simple to assemble into a single structure is demonstrated by its use in various fields of material and life sciences, such as drug discovery, DNA labeling, and oligonucleotide synthesis (Scheme 1). [28] Decaprenyl phosphoryl-β-D-ribose oxidase (DprE1) and DprE2 are highly involved in the synthesis of arabinogalactan, an essential constituent of the Mtb cell wall biosynthesis.…”

Section: Introductionmentioning

confidence: 99%

Design, Synthesis and In vitro Antitubercular Effect of New Chalcone Derivatives Coupled with 1,2,3‐Triazoles: A Computational Docking Techniques

Sadineni,

Reddy Basireddy,

Rao Allaka

et al. 2024

Chemistry & Biodiversity

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A very interesting foundation for this study is the creation of new methods for modifying compounds with a 1,2,3‒triazole and chalcones, as these compounds are significant in organic synthesis as bioactive organic compounds. To contribute to the development of an efficient method for the conversion of antimicrobial and anti‐TB drugs, a novel series of cyclohepta pyridinone fused 1,2,3–triazolyl chalcones were designed and synthesized. All the newly prepared scaffolds were characterized by IR, NMR (1H & 13C) and mass spectrometry. Among the tested compounds, hybrids 8b, 8d, and 8f exhibited exceptional antibacterial susceptibilities with zone of inhibition 27, 32, and 38 mm against the tested E. faecalis bacteria, whereas 8d had better antitubercular potency against M. tuberculosis H37Rv strain with MIC value 5.25 µg/mL. All the synthesized compounds were initially assessed in silico against the targeted protein i.e., DprE1 that indicated compound 8d, 8f and 8h along with several other 1,2,3‐triazole compounds as possible inhibitors. Based on docking results, 8d showed that the amino acids His74(A), Lys76(A), Cys332(A), Asp331(A), Val307(A), Tyr357(A), ect., exhibited highly stable binding to DprE1 receptor of M. tuberculosis (4G3U). Moreover, these scaffolds physicochemical characteristics, filtration molecular properties, assessment of toxicity, and bioactivity scores were assessed.

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