Isoxazole/Isoxazoline Skeleton in the Structural Modification of Natural Products: A Review

Abstract

Isoxazoles and isoxazolines are five-membered heterocyclic molecules containing nitrogen and oxygen. Isoxazole and isoxazoline are the most popular heterocyclic compounds for developing novel drug candidates. Over 80 molecules with a broad range of bioactivities, including antitumor, antibacterial, anti-inflammatory, antidiabetic, cardiovascular, and other activities, were reviewed. A review of recent studies on the use of isoxazoles and isoxazolines moiety derivative activities for natural products is presented here, focusing on the parameters that affect the bioactivity of these compounds.

An Efficient Synthesis, Antimicrobial Evaluation and In Silico Studies of 1,2,3‐Triazolyl‐isoxazolyl‐ethanol Derivatives

“…They also provide a tool for the optimization of the ADMET properties. [15][16][17][18] The clubbed azole and azolyl ethanol scaffolds played a dynamic role in the design and development of the new lead and drug molecules. [19][20][21][22][23] These combinations have been extensively employed in the design and development of numerous drugs such as fluconazole, ravuconazole, isavuconazole, voriconazole, itraconazole, broxaterol, etc.…”

“…[24][25][26][27] 1,2,3-Triazole-containing compounds received more attention due to their varied biological activities such as antifungal, [28][29][30][31][32][33][34] antimicrobial, [35,36] antivirals, [37,38] antimalarial, [39,40] anticancer [41][42][43] and anti-inflammatory activities. [44,45] The isoxazole containing natural and synthetic compounds reported for a wide range of biological activities such as antimicrobial, [46,47] antibacterial, [48][49][50] antifungal, [51,52] antitubercular, [16,[53][54][55] antiviral, [56,57] anticancer, [58][59][60] and anti-inflammatory. [61][62][63] Some of the FDA-approved and commercialized drugs containing isoxazole and triazole pharmacophore are shown in Figure 1 1) The hybrids of 1,2,4-triazole drugs by clubbing with azole or structural modifications of the fluconazole, isavuconazole, ravuconazole and albaconazole were reported for potential antifungal activity.…”

“…The azole pharmacophores displayed a significant role in the development and discovery of drugs. They also provide a tool for the optimization of the ADMET properties [15–18] . The clubbed azole and azolyl ethanol scaffolds played a dynamic role in the design and development of the new lead and drug molecules [19–23] .…”

“…1,2,3‐Triazole‐containing compounds received more attention due to their varied biological activities such as antifungal, [28–34] antimicrobial, [35,36] antivirals, [37,38] antimalarial, [39,40] anticancer [41–43] and anti‐inflammatory activities [44,45] . The isoxazole containing natural and synthetic compounds reported for a wide range of biological activities such as antimicrobial, [46,47] antibacterial, [48–50] antifungal, [51,52] antitubercular, [16,53–55] antiviral, [56,57] anticancer, [58–60] and anti‐inflammatory [61–63] …”

Antioxidant activity of novel nitrogen scaffold with docking investigation and correlation of DFT stimulation

“…[22][23][24][25][26] The iso-oxazolines exhibit antibacterial, antifungal, anticancer, and anti-inammatory properties. 27 Furthermore, S-containing heterocyclic compounds are used in dyes, medicines, and agrochemicals as well as being key components of primary (cystine and methionine amino acids) and secondary metabolites (biotin and thiamine). 28,29 Benzothiazepines are recognized for their impact on cardiovascular functioning by acting as calcium channel inhibitors, and they have also been found to exhibit anticonvulsant and anticancer properties.…”