Design, synthesis, and antimicrobial evaluation of novel 2-arylbenzothiazole analogs bearing fluorine and piperazine moieties

Al-Harthy, Thuraya; Zoghaib, Wajdi M.; Stoll, Raphael; Abdel‐Jalil, Raid J.

doi:10.1007/s00706-017-2088-4

Cited by 9 publications

(5 citation statements)

References 26 publications

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“…The novel class was reported and screened against different bacteria and fungi strains. The molecule bearing electron withdrawing moiety by induction e.g., fluoro in compound 26 has a role in enhancing antibacterial activity in comparison to the non-fluorinated derivatives [ 140 ].…”

Section: Benzazolesmentioning

confidence: 99%

Importance of Fluorine in Benzazole Compounds

2020

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Fluorine-containing heterocycles continue to receive considerable attention due to their unique properties. In medicinal chemistry, the incorporation of fluorine in small molecules imparts a significant enhancement their biological activities compared to non-fluorinated molecules. In this short review, we will highlight the importance of incorporating fluorine as a basic appendage in benzothiazole and benzimidazole skeletons. The chemistry and pharmacological activities of heterocycles containing fluorine during the past years are compiled and discussed.

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Section: Benzazolesmentioning

confidence: 99%

Importance of Fluorine in Benzazole Compounds

2020

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“…In addition, a new series from the same intermediate ( 15) was proposed with the same research team of 5-fluoro-6-(4 methylpiperazin-1-yl)-substitutedphenylbenzo[d]thiazoles and screened against different bacteria and fungi strains. Among, two compounds, (17 and 18) show potent bacterial growth inhibition against Gram-positive bacteria S. aureus with MIC 32 μg/cm 3 compared to 10 μg/cm 3 for tamoxifen used as a positive cytotoxicity standard (Figure 4) [61].…”

Section: Benzothiazole Containing Piperazinementioning

confidence: 99%

The Impact of Incorporating Piperazine on Biological Activities of Benzazoles

Al-Harthy,

Zoghaib,

Abdel-Jalil

2024

Heterocyclic Chemistry - New Perspectives [Working Title]

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Heterocycles are widely distributed compounds in natural products and are involved in many biological processes. Its uses have been extended to different fields, including industry, medicine, and agriculture sectors. Benzazole is one of the popular heterocycle scaffolds known as a privilege structure which is commonly found in many pharmaceutical agents. Another outstanding scaffold is piperazine that is known as a distinguishable motif in drug design with a wide range of biological activities. One of the fruitful approaches in the drug design is a hybridization of privilege structures in one skeleton which are believed to grant a characteristic feature with improved or more selective biological activities than the two scaffolds. The effect that piperazine imparted while introduced into a benzazole has drawn attention since first used in the nineteenth century. Numerous research has been performed discussing the synthesis and biological activities of benzazoles containing piperazine. In this chapter, we will highlight a general introduction about chemistry and structure of piperazine, and its importance in medicinal chemistry and benzazole as well. Next, several studies will be discussed that highlight the importance of incorporating piperazine in benzazole skeletons, benzimidazole, benzothiazole, and benzoxazole, and biological activity inherited from this combination.

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“…Moreover, only compound 90b showed the best inhibitory potency against the fungal strain C. neoformans with 103.06% growth inhibition. 96 Jauhari et al described the 6-uorobenzoxazole derivative 64 (Fig. 37 above) as an antimicrobial agent using the disc diffusion method at a concentration of 10 mg mL −1 .…”

Section: Antimicrobial Activity Of Uorinated Benzazolesmentioning

confidence: 99%

“…Moreover, only compound 90b showed the best inhibitory potency against the fungal strain C. neoformans with 103.06% growth inhibition. 96 …”

Section: Antimicrobial Activity Of Fluorinated Heterocyclesmentioning

confidence: 99%