Synthesis of Novel 3-(Piperazin-1-yl)-1,2-benzothiazole Derivatives and Their Antibacterial Activity

Garlapati, Krishna Kanth; Srinivasu, N.; Kumar, K. Siva; Ganta, Ravi Kumar

doi:10.1134/s1070428022100220

Cited by 1 publication

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“…An example of a drug containing piperazine in its structure is ciprofloxacin, which is a fluoroquinolone antibiotic with a mechanism of action based on the inhibition of the bacterial enzyme DNA gyrase [ 23 ]. Our literature review of studies on the activity of piperazine derivatives indicates that many compounds from this group have antibacterial [ 24 , 25 , 26 , 27 , 28 ] and antifungal activity [ 29 ].…”

Section: Introductionmentioning

confidence: 99%

Synthesis and Antimicrobial Activity of New Mannich Bases with Piperazine Moiety

Janowska,

Andrzejczuk,

Gawryś

et al. 2023

Molecules

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A series of novel Mannich bases were designed, synthesized, and screened for their antimicrobial activity. The target compounds were synthesized from 4-(3-chlorophenyl)-5-(3-fluorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione and different piperazine derivatives. The structures of the products were confirmed by 1H and 13C NMR and elemental analysis. The activity of piperazine derivatives against bacteria (Gram-positive: Staphylococcus epidermidis, Staphylococcus aureus, Micrococcus luteus, Bacillus cereus, and Bacillus subtilis; Gram-negative: Escherichia coli, Pseudomonas aeruginosa, Klebsiella pneumoniae, and Proteus mirabilis) and yeasts (Candida glabrata, Candida krusei, and Candida parapsilosis) was determined by the minimum inhibitory concentration and minimum bactericidal concentration values. Significant activity was observed against Gram-positive bacteria, mainly staphylococci (PG7–PG8) and bacteria of the genes of Micrococcus and Bacillus (PG1-3), as well as selected strains of Gram-negative bacteria, including bacteria of the Enterobacteriaceae family (PG7), while all tested compounds showed high fungistatic activity against Candida spp. yeasts, especially C. parapsilosis, with MICs ranging from 0.49 µg/mL (PG7) to 0.98 µg/mL (PG8) and 62.5 µg/mL (PG1-3). In conclusion, the results obtained confirm the multidirectional antimicrobial activity of the newly synthesized piperazine derivatives. Furthermore, in silico studies suggest that the tested compounds are likely to have good oral bioavailability. The results obtained will provide valuable data for further research into this interesting group of compounds. The library of compounds obtained is still the subject of pharmacological research aimed at finding new interesting biologically active compounds.

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