The synthesis of two groups of structure hybrids comprising basically the antipyrine moiety attached to either polysubstituted thiazole or 2,5-disubstituted-1,3,4-thiadiazole counterparts through various linkages is described. Twelve out of the newly synthesized compounds were evaluated for their anti-inflammatory activity using two different screening protocols; namely, the formalin-induced paw edema and the turpentine oil-induced granuloma pouch bioassays, using diclofenac Na as a reference standard. The ulcerogenic effects and acute toxicity (ALD(50)) values of these compounds were also determined. Meanwhile, the analgesic activity of the same compounds was evaluated using the rat tail withdrawal technique. Additionally, the synthesized compounds were evaluated for their in vitro antimicrobial activity. In general, compounds belonging to the thiazolylantipyrine series exhibited better biological activities than their thiadiazolyl structure variants. Collectively, compounds 6, 10, 26, and 27 proved to display distinctive anti-inflammatory and analgesic profiles with a fast onset of action. All of the tested compounds revealed super GI safety profile and are well tolerated by the experimental animals with high safety margin (ALD(50)>3.0 g/kg). Meanwhile, compounds 7, 10, 11, and 23 are considered to be the most active broad spectrum antimicrobial members in this study. Compound 10 could be identified as the most biologically active member within this study with an interesting dual anti-inflammatory analgesic and antibacterial profile.

Download full-text PDF

Source
http://dx.doi.org/10.1016/j.bmc.2008.11.035DOI Listing

Publication Analysis

Top Keywords

anti-inflammatory analgesic
12
compounds evaluated
12
compounds
8
synthesized compounds
8
design synthesis
4
synthesis thiazolyl
4
thiazolyl thiadiazolyl
4
thiadiazolyl derivatives
4
derivatives antipyrine
4
antipyrine potential
4

Similar Publications

Aim: Tramadol (TRM), a widely used opioid analgesic for moderate to severe pain, is associated with liver and kidney toxicity at high doses or prolonged use. This study investigates the protective role of rosmarinic acid (RA), a natural phenolic compound known for its antioxidant, anti-inflammatory, and cell-protective properties, against TRM-induced hepatorenal toxicity.

Methods: Thirty-five male Wistar rats were divided into five groups: Control, TRM, RA, TRM+RA25, and TRM+RA50.

View Article and Find Full Text PDF

Oxycodone for analgesia in children undergoing endoscopic retrograde cholangiopancreatography: a randomized, double-blind, parallel study.

Front Pharmacol

January 2025

Department of Anesthesiology and Pediatric Clinical Pharmacology Laboratory, Shanghai Children's Medical Center, Affiliated to Shanghai Jiao Tong University School of Medicine, Shanghai, China.

Background: Postoperative visceral pain is a common complication after endoscopic retrograde cholangiopancreatography (ERCP). In this study, we compared the analgesic and anti-inflammatory effects of oxycodone and fentanyl in children undergoing ERCP.

Methods: A single-center, randomized, double-blind study was conducted at a tertiary care hospital affiliated with Shanghai Jiao Tong University.

View Article and Find Full Text PDF

Knee arthritis is a common degenerative joint disease, usually with joint swelling, chronic pain, and dysfunction as the main clinical manifestations. At present, the conservative treatment for knee arthritis is mostly using anti-inflammatory and analgesic drugs, but the effect is mostly temporary, and can not prevent its progress and surgery is usually the last treatment method. Total knee arthroplasty, also known as TKA, is one of the most effective treatments for osteoarthritis of the knee that has progressed to the end stage.

View Article and Find Full Text PDF

Astragalin inhibits neuronal excitability and activates neuronal autophagy in the ACC and LH of CFA mice to alleviate inflammatory pain and pain-related emotions.

Int Immunopharmacol

January 2025

Department of Anatomy, School of Basic Medical Sciences, Guangdong Pharmaceutical University, Guangzhou, China; Guangdong Key Laboratory of Pharmaceutical Bioactive Substances, Guangdong Pharmaceutical University, Guangzhou, China. Electronic address:

Astragalin (AST), a natural flavonoid, exhibits anti-inflammatory, anti-cancer, and antioxidant properties. However, its effects and molecular mechanisms in inflammatory pain remain unclear. Therefore, this study aims to investigate the impact of AST on a Complete Freund's Adjuvant (CFA)-induced inflammatory pain mouse model and to elucidate its potential mechanisms.

View Article and Find Full Text PDF

Chronic wounds, especially non-healing wounds, significantly affect patients' quality of life and raise the costs of therapy. Wound healing is a complicated process involving interdependent stages, which may be impaired and delayed by infections with multi-drug resistant pathogens. Current medical strategies for wound healing, especially the treatment of non-healing wounds, exert limited therapeutic effects, thus become a dramatic challenge for modern medicine.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!