Synthesis and biological evaluation of some novel diastereoselective benzothiazole β-lactam conjugates

Three-component synthesis of chromeno β-lactam hybrids for inflammation and cancer screening

“…The 13 C NMR spectral data for compound 5b exhibited signals at δ 60.9 and δ 80.4 ppm for the C-2 and C-3 β-lactam ring protons, respectively, the aromatic carbons at appropriate shifts, the β-lactam carbonyl carbon at δ 161.4 ppm and the aldehyde carbonyl carbon at δ 190.5 ppm. The cis stereochemistry was confirmed from the vicinal coupling constants of the two β-lactam ring protons, H-2 and H-3 (J2,3 ≥4.0 Hz) [18]. X-Ray single crystal analysis done on β-lactam 5b confirmed the cis stereochemistry ( Fig.…”

“…In this study, β-lactams 5a-j were synthesized by a diastereoselective ketene-imine cycloaddition reaction (Scheme 1) [18,20]. The reaction of 4-hydroxybenzaldehyde (1) with bromoacetic acid (2) in DMF at 70 o C in the presence of solid K2CO3 afforded 2-(4formylphenoxy)acetic acid (3).…”

“…The commonly used bicyclic β-lactam antibiotics such as the penicillins and cephalosporins prevent bacterial transpeptidases from crosslinking the polysaccharide cell wall [13]. More recently, functionalized monocyclic β-lactams have been developed having a host of other pharmaceutical capabilities, such as anti-HIV [14], antifungal [15], anticancer [16,17] and antimalarial [18] (Figure 3), anti-inflammatory, or analgesic activities [19]. Thus, the β-lactam framework presents a rich source of diverse biological properties.…”

Silica‐supported Cu(II)–quinoline complex: Efficient and recyclable nanocatalyst for one‐pot synthesis of benzimidazolquinoline derivatives and 2H‐indazoles

“…Benzimidazole‐based compounds are a class of nitrogen‐based benzo‐fused heterocyclic products which possess several kinds of applications, particularly in coordination chemistry and catalysis. It has been shown that they play an important role in numerous pharmaceutical products with a wide range of biological activities including anticancer, antioxidant, antimicrobial, antihypertensive, anthelmintic, anti‐inflammatory, and so on (Figure ) . Benzimidazoles bearing quinolines are an excellent choice for producing many hybrid molecules with remarkable properties .…”

MIL‐101(Fe) hexagonal microspindle as a highly efficient, reusable and versatile catalyst for benzo‐fused heterocyclic nucleus synthesis

“…Benzo‐fused heterocyclic scaffolds have been extensively screened for the expansion of antihypertensive, antiviral, antimicrobial and antitumour activities. Moreover, these compounds are very significant intermediates in organic reactions. They have been also broadly surveyed due to their presence in various bioactive products including an anti‐inflammatory agent, an HIV reverse transcriptase inhibitor and anticoagulants .…”