Design and synthesis of ibuprofen-quinoline conjugates as potential anti-inflammatory and analgesic drug candidates

Synthesis of New 1,2,3,4-Tetrahydroquinoline Hybrid of Ibuprofen and Its Biological Evaluation

“…Ibuprofen, on the other hand, is maybe the most popular non-steroidal anti-inflammatory drug, used in the treatment of many musculoskeletal disorders [11], and is the safest traditional choice for utilization during chronic neuroinflammation such as in Alzheimer's [12], Parkinson's [13], and Machado-Joseph disease [14]. Hybrids of ibuprofen with quinoline are interesting [11] in order to study their potential biological Likewise, the 1,2,3,4-tetrahydroquinoline skeleton is prevalent in many pharmacologically active synthetic and natural products [9]. Another interesting example is the 2,4,6trisubstituted tetrahydroquinoline 6 (Figure 3 Discovered in 1934 by H. Andersag chloroquine is a drug primarily used to treat malaria.…”

“…Ibuprofen, on the other hand, is maybe the most popular non-steroidal anti-inflammatory drug, used in the treatment of many musculoskeletal disorders [11], and is the safest traditional choice for utilization during chronic neuroinflammation such as in Alzheimer's [12], Parkinson's [13], and Machado-Joseph disease [14]. Hybrids of ibuprofen with quinoline are interesting [11] in order to study their potential biological Many tetrahydroquinolines owing various simple or complex substituents have interesting biochemical activity; some are potential pharmaceutical agents. Thus, a very simple derivative, 2-methyl-5-hydroxy-1,2,3,4-tetrahydroquinoline, exhibits analgesic activity oneeighth as potent as morphine.…”

“…Ibuprofen, on the other hand, is maybe the most popular non-steroidal anti-inflammatory drug, used in the treatment of many musculoskeletal disorders [11], and is the safest traditional choice for utilization during chronic neuroinflammation such as in Alzheimer's [12], Parkinson's [13], and Machado-Joseph disease [14]. Hybrids of ibuprofen with quinoline are interesting [11] in order to study their potential biological activity, and to answer the question of whether they will combine the properties of both parent molecules or not, as we know the carboxylic functional group is not required for the anti-inflammatory properties of profens [15] but for causing gastric toxicity.…”

Recent advances in functionalized quinoline scaffolds and hybrids—Exceptional pharmacophore in therapeutic medicine

“…Quinoline hybrids have been synthesized in recent years and reported to have improved activity when compared to standard drugs used. Examples shown in Figure 3 are the Quinoline-coumarin hybrid (Taheri et al, 2019), the Quinolinebenzothiadiazole hybrid (Medeiros et al, 2021), the Quinolinethiazole hybrid (Eissa et al, 2021), Quinoline-triazine hybrid (Ghanim et al, 2022), amongst others. This review focuses on the synthesis, pharmacological activity, Structure-Activity Relationship (SAR), and ADMET studies of quinoline derivatives including quinoline hybrids to uncover their drug-likeness and the activities responsible for the novel pharmacological activity.…”

Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates

“…Physico-chemical properties (descriptors) can determine the correlation between the biological/antimicrobial properties and chemical entities quantitatively in mathematical equations expressed in the QSAR model, which can determine the most important features needed for the antimicrobial properties [31,32].…”