Synthesis and Antimicrobial Evaluation of a New Series of N‐1,3‐Benzothiazol‐2‐ylbenzamides

Abstract

Enterococcus faecalisis a Gram-positive commensal inhabitant of the intestinal tract of humans, animals, and insects. However, it is also an opportunistic pathogen and has emerged as a leading cause of hospital-acquired extraintestinal infections. Fluoroquinolones have been frequently used to treatE. faecalisinfections, and the emergence of fluoroquinolone-resistantE. faecalisstrains has recently been reported in several countries. Thus, the identifications of new antibiotics specifically directed toE. faecalismay be envisaged. In this paper, a new series ofN-1,3-benzothiazol-2-ylbenzamides have been designed, synthesized, and evaluated for theirin vitroantimicrobial activities. Among the tested compounds,3iwas active againstE. faecalis.

Antiproliferative Activity Evaluation of a Series ofN-1,3-Benzothiazol-2-ylbenzamides as Novel Apoptosis Inducers

“…Chemistry. Compounds 1a-l and 2b-e were previously reported by this group [18]. Compounds 1m,n and 2a were prepared as reported in Schemes 1 and 2, respectively.…”

“…Furthermore, it has been reported that antimicrobials often induce cytotoxicity via apoptotic mechanism, thus making themselves candidates as new tools for anticancer therapy. In the last decade, our research group was interested in the design, synthesis, and biological evaluation of novel benzothiazole derivatives as antimicrobial agents [8,10,18]. Thus, to further investigate the panel of activity for this class of compounds, we decided to study some of them as potential anticancer agents.…”

“…Thus, to further investigate the panel of activity for this class of compounds, we decided to study some of them as potential anticancer agents. Based on the results obtained by Wang et al [16] on a series of benzothiazole derivatives that exhibited antiproliferative activity against the human hepatocellular carcinoma cell line, HepG2, and the human mammary carcinoma cell line, MCF-7, we selected a small series of compounds among the previously synthesized benzothiazoles [18] for biological evaluation as potential apoptosis inducers. The selected compounds belong to two small series (1 and 2, Figure 1).…”

Auxin-like effect of derivatives of Pyrimidine, Pyrazole, Isoflavones, Pyridine, Oxazolopyrimidine and Oxazole on acceleration of Vegetative growth of Flax

“…In recent years the considerable attention is focused on practical application in the agriculture of different classes of low molecular weight heterocyclic compounds, derivatives of pyrimidine, pyrazole, isoflavones, pyridine, oxazole, oxazolopyrimidine as effective substitutes of traditional plant growth regulators, herbicides, fungicides and antimicrobial agents [14][15][16][17][18][19][20][21][22][23][24][25][26] . Testing of different classes of chemical low molecular weight heterocyclic compounds on human and animal cells indicated their activity against cancer, viral, bacterial, fungal, infectious, inflammatory and nervous diseases [27][28][29][30][31] .…”

1,3-Benzothiazoles as Antimicrobial Agents

“…We recently studied two different series of 1,3‐benzothiazoles both as antifungals against Candida spp . and antibacterials, in particular against Enterococcus faecalis . In the last year, we determined for the first time the X‐ray crystallographic structure of E .…”