Abstract
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).
Highlights
The field of drug discovery has conventionally been a dynamic, innovation-driven and highly prosperous sector of the global industry
Multicomponent reactions (MCRs) are considered to be very important and powerful reactions in combinatorial and medicinal chemistry [57] because of the benefits they offer in terms of the synthesis of diverse structures that will lead to an increase in the economy of organic synthesis [58,59] by shortening the time span [60]
The reaction between amines or ammonia heterocyclic proton-containing chemist, Carl Mannich, in 1912, the synthesis of atropine glucoside pharmacophores is known as afor
Summary
The field of drug discovery has conventionally been a dynamic, innovation-driven and highly prosperous sector of the global industry. Revolutionary advancements in health disciplines and technology have helped researchers in the discovery and development of numerous drugs, which play a significant role in the pharmacotherapy of a range of ailments and diseases [1]. Innovations in medicinal chemistry are responsible for the discovery of many breakthrough remedies that have improved the life and health of human beings over the past century. The human body produces free radicals in the form of reactive oxygen species (ROS), which regulate cellular processes, i.e., angiogenesis, platelet aggregation, signal transduction, etc. Free radicals can impose a harmful and deleterious impact on cellular components, i.e., Molecules 2020, 25, 2710; doi:10.3390/molecules25112710 www.mdpi.com/journal/molecules
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