Pyridoimidazolyl Sulfonamide Compound 2: A Superior Dual-Acting Drug Candidate with Potent

A dataset describing the synthesis and evaluation of 40 novel pyridoimidazolyl sulfonamide derivatives as potential gout therapeutics. The data was authored by Xiaoyu Shi and last updated on 2026-05-26. It focuses on a lead compound, designated '2', which demonstrated potent URAT1 inhibition and anti-inflammatory activity in preclinical models.

Use Cases

• Modeling structure-activity relationships based on the synthesis of 40 novel derivatives.
• Analyzing in vivo efficacy based on serum uric acid reduction percentages in mice and rats.
• Evaluating pharmacokinetic properties based on reported half-life and oral bioavailability.
• Assessing dual-action drug candidates based on combined URAT1 and IL-1β inhibition IC50 values.

Strengths

• Contains specific potency metrics, including a URAT1 IC50 of 0.19 μM and an IL-1β IC50 of 3.39 μM.
• Reports concrete in vivo efficacy results, showing 96.8% and 91.9% serum uric acid reduction in hyperuricemic mice and rats.
• Includes key pharmacokinetic and safety parameters: a 6.3-hour half-life, 20.1% oral bioavailability, and an MTD > 1000 mg/kg.

Limitations

• Row count is unknown, which may limit suitability assessment.
• Column-level documentation is absent; field semantics must be inferred after download.
• The dataset is very small at 3.7 KB, indicating limited scope.

Provenance

Source

figshare

Collection Method

Likely contains experimental results from the synthesis and biological evaluation of chemical compounds.

Freshness

Last updated 2026-05-26 21:06:28; freshness should be verified.