Synthesis of pyrazolo-enaminones, bipyrazoles and pyrazolopyrimidines and evaluation of antioxidant and antimicrobial properties

Akhramez, Soufiane; Oumessaoud, Asmaa; Hibot, Achraf; Talbi, Soumaya; Hamri, Salha; Ketatni, El Mostafa; Ouchetto, Hajiba; Hafid, Abderrafia; Ayad, Houda; Abbadi, Noureddine El; Zanane, Chorouk; Latrache, Hassan; Khouili, Mostafà; Pujol, Maria Dolors

doi:10.1016/j.arabjc.2021.103527

Cited by 8 publications

(1 citation statement)

References 32 publications

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“…Several pharmacological agents contain pyrazole moiety including antimicrobials, hypoglycemic, and anti-inflammatory agents, due to their proven biological properties that lead to analgesic, anti-inflammatory, and anti-depressant effect [16]. Among pyrazoles, bipyrazoles have also shown beneficial therapeutic effects for treatment of infectious diseases, inflammatory conditions and some cancers [17].…”

Section: Introductionmentioning

confidence: 99%

New Treatment for Type 2 Diabetes Mellitus Using a Novel Bipyrazole Compound

Alqudah

Qnais

Wedyan

et al. 2023

Cells

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2′,3,3,5′-Tetramethyl-4′-nitro-2′H-1,3′-bipyrazole (TMNB) is a novel bipyrazole compound with unknown therapeutic potential in diabetes mellitus. This study aims to investigate the anti-diabetic effects of TMNB in a high-fat diet and streptozotocin-(HFD/STZ)-induced rat model of type 2 diabetes mellitus (T2D). Rats were fed HFD, followed by a single low dose of STZ (40 mg/kg). HFD/STZ diabetic rats were treated orally with TMNB (10 mg/kg) or (200 mg/kg) metformin for 10 days before terminating the experiment and collecting plasma, soleus muscle, adipose tissue, and liver for further downstream analysis. TMNB reduced the elevated levels of serum glucose in diabetic rats compared to the vehicle control group (p < 0.001). TMNB abrogated the increase in serum insulin in the treated diabetic group compared to the vehicle control rats (p < 0.001). The homeostasis model assessment of insulin resistance (HOMA-IR) was decreased in the diabetic rats treated with TMNB compared to the vehicle controls. The skeletal muscle and adipose tissue protein contents of GLUT4 and AMPK were upregulated following treatment with TMNB (p < 0.001, < 0.01, respectively). TMNB was able to upregulate GLUT2 and AMPK protein expression in liver (p < 0.001, < 0.001, respectively). LDL, triglyceride, and cholesterol were reduced in diabetic rats treated with TMNB compared to the vehicle controls (p < 0.001, 0.01, respectively). TMNB reduced MDA and IL-6 levels (p < 0.001), and increased GSH level (p < 0.05) in diabetic rats compared to the vehicle controls. Conclusion: TMNB ameliorates insulin resistance, oxidative stress, and inflammation in a T2D model. TMNB could represent a promising therapeutic agent to treat T2D.

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Section: Introductionmentioning

confidence: 99%