Mankind has always suffered from multiple diseases. Therefore, there has been a rigorous need in the field of medicinal chemistry for the design and discovery of new and potent molecular entities. In this work, thirteen tetrahydroquinoline derivatives were synthesized and evaluated biologically for their antioxidant, α-amylase enzyme inhibitory, anti-proliferative and anti-inflammatory activities. SF8 showed the lowest IC₅₀ of 29.19 ± 0.25 µg/mL by scavenging DPPH free radicals. SF5 showed significant antioxidant activity in total antioxidant capacity (TAC) and total reducing power (TRP) assays. SF5 and SF9 showed the maximum inhibition of α-amylase enzyme i.e., 97.47% and 89.93%, respectively, at 200 µg/mL concentration. Five compounds were shortlisted to determine their anti-proliferative potential against Hep-2C cells. The study was conducted for 24, 48 and 72 h. SF8 showed significant results, having an IC₅₀ value of 11.9 ± 1.04 µM at 72 h when compared with standard cisplatin (IC₅₀ value of 14.6 ± 1.01 µM). An in vitro nitric oxide (NO) assay was performed to select compounds for in vivo anti-inflammatory activity evaluation. SF13 scavenged the NO level to a maximum of 85% at 50 µM concentration, followed by SF1 and SF2. Based on the NO scavenging assay results, in vivo anti-inflammatory studies were also performed and the results showed significant activity compared to the standard, acetylsalicylic acid (ASA).

Ynamides are N-alkyne compounds bearing an electron withdrawing group at the nitrogen atom. They offer unique pathways for the construction of versatile building blocks owing to their exceptional balance between reactivity and stability. Recently several studies have been reported that explore and illustrate the synthetic potential of ynamides and ynamide-derived advanced intermediates in cycloadditions with different reaction partners to yield heterocyclic cycloadducts of synthetic and pharmaceutical value. Cycloaddition reactions of ynamides are the facile and preferable routes for the construction of structural motifs having striking importance in synthetic, medicinal chemistry, and advanced materials. In this systematic review, we highlighted the recently reported novel transformations and synthetic applications that involved the cycloaddition reaction of ynamides. The scope along with the limitations of the transformations are discussed in detail.