Green Synthesis of Novel Pyridines via One-Pot Multicomponent Reaction and Their Anti-Inflammatory Evaluation

Abstract

A functional and environmentally green procedure for the design of novel pyridine 5a – h and 7a – d derivatives through two pathways is presented. The first pathway is via a one-pot, four-component reaction of p -formylphenyl-4-toluenesulfonate ( 1 ), ethyl cyanoacetate ( 2 ), acetophenone derivatives 3a–h or acetyl derivatives 6a – d , and ammonium acetate ( 4 ) under microwave irradiation in ethanol. The advantages of this method are an excellent yield (82%–94%), pure products, a short reaction time (2–7 min), and low-cost processing. The second pathway was obtained by the traditional method with treatment of the same mixture under refluxing in ethanol, which afforded the same products, 5a – h and 7a – d , in less yield (71%–88%) and over a longer reaction time (6–9 h). The constructions of the novel compounds were articulated via spectral and elemental analysis. Overall, the compounds have been designed, synthesized, and studied for their in vitro anti-inflammatory activity using diclofenac as a reference drug (5 mg/kg). The most potent four compounds, 5a , 5f , 5g , and 5h , showed promising anti-inflammatory activity.

Design and Synthesis of Pyridine and Thiazole Derivatives as Eco‐friendly Insecticidal to Control Olive Pests

“…Our study begins with the treatment of ethyl 2-cyano-3-(4-{[(4methylphenyl)sulfonyl] oxy}phenyl)acrylate [21] (2) with the respective active methylene such as malononitrile, ethyl acetoacetate, ethyl benzoyl acetate, m-acetyl thiophene, o-acetyl naphthalene, and ammonium acetate, in ratio (1 : 1: 2), respectively under microwave irradiation afforded excellent yields from pyridine derivatives (85-92 %) within short reaction time 5 min (Scheme 1).…”

“…The insecticidal activity of all the pyridine and thiazole derivatives was measured via leaf dip bioassay methods. [13][14][15][16][17][18][19][20][21][22]…”

Design, synthesis, biological and computational screening of novel pyridine-based thiadiazole derivatives as prospective anti-inflammatory agents

“…Furthermore, several research groups, such as Abd El-Lateef et al (2023) [ 30 ] and Bian et al (2021) [ 31 ], have recently highlighted the efficacy of pyridine derivatives, particularly in demonstrating potent anti-inflammatory properties ( Fig. 2 ).…”

Design, synthesis of novel Schiff bases as potential insecticidal agents against Spodoptera frugiperda (Lepidoptera: Noctuidae)

“…Crop yield and growth are constantly in jeopardy due to pest activity, particularly that of animals. The Food and Agriculture Organization (FAO) has released growing estimates of actual and projected losses, which are regularly reported [4,5], despite several interventions and advancements in crop protection. Pest resistance to pesticides has grown over time, affecting crop development and yield, and is one of the main causes [6].…”