On drug discovery against infectious diseases and academic medicinal chemistry contributions

• Yves L. Janin

Beilstein J. Org. Chem. 2022, 18, 1355–1378, doi:10.3762/bjoc.18.141

• effects such as metronidazole (21), which is still used to treat anaerobic infections [151]. In any case, pretomanid (18), first mentioned in 1996 and reported [152] for its effect on mycobacteria growth in 2000, was developed by the TB alliance and approved for use in human in 2019. Again, this was the

Synthesis and antimicrobial activity of 1H-1,2,3-triazole and carboxylate analogues of metronidazole

• Satya Kumar Avula,
• Syed Raza Shah,
• Khdija Al-Hosni,
• Muhammad U. Anwar,
• Rene Csuk,
• Biswanath Das and
• Ahmed Al-Harrasi

Beilstein J. Org. Chem. 2021, 17, 2377–2384, doi:10.3762/bjoc.17.154

• -Wittenberg, Kurt-Mothes-Str. 2, d-06120, Halle (Saale), Germany 10.3762/bjoc.17.154 Abstract Herein, a series of novel 1H-1,2,3-triazole and carboxylate derivatives of metronidazole (5a–i and 7a–e) were synthesized and evaluated for their antimicrobial activity in vitro. All the newly synthesized compounds

• metronidazole derivatives. The antimicrobial (antifungal and antibacterial) activity of the prepared compounds was studied. All compounds (except 2 and 3) showed a potent inhibition rate of fungal growth as compared to control and metronidazole. The synthetic compounds also showed higher bacterial growth

• inhibiting effects compared to the activity of the parent compound. Amongst the tested compounds 5b, 5c, 5e, 7b and 7e displayed excellent potent antimicrobial activity. The current study has demonstrated the usefulness of the 1H-1,2,3-triazole moiety in the metronidazole skeleton. Keywords: antimicrobial

Michael-type addition of azoles of broad-scale acidity to methyl acrylate

• Sławomir Boncel,
• Kinga Saletra,
• Barbara Hefczyc and
• Krzysztof Z. Walczak

Beilstein J. Org. Chem. 2011, 7, 173–178, doi:10.3762/bjoc.7.24

• , pyrazole and 1,2,4-triazole moieties, constitute building blocks for a variety of therapeutic agents (Figure 1). 1,2-Arylimidazole derivatives, e.g., 2-(3-chloro-4-methylphenyl)-1-phenyl-4-(trifluoro-methyl)imidazole (I) are selective cyclooxygenase (COX-2) inhibitors [1]. Metronidazole (2-(2-methyl-5