Synthesis and SAR of 2-aryl pyrido[2,3-d]pyrimidines as potent mGlu5 receptor antagonists

Recent advances in the chemistry and biology of pyridopyrimidines

“…Wendt et al described a novel series of pyrido [2,3-d] pyrimidines mGlu5 receptor antagonists. The pharmacological activity of the lead compound 137 (Ar ¼ 3,5-diClC 6 H 3 , IC 50 ¼ 0.72 nM) was reported and showed positive effects on anxiety and pain in rodent models (Scheme 43) [46].…”

Microwave-Assisted Synthesis of Bioactive Six-Membered Heterocycles and Their Fused Analogues

“…For example, this system is present in AZD8055 (180), a selective ATP-competitive PI3KAkt-mTOR signaling pathway inhibitor [168], piritrexim (181), a lipid-soluble inhibitor of dihydrofolate reductase (DHFR) that displays high potency for the treatment of metastatic urothelial cancer [169], and pyrido[2,3-d]pyrimidine 182 that is a hepatitis C virus inhibitor [170] (Figure 12). Other pyridopyrimidine derivatives have also been reported for their potential use as anticardiovascular [171], anti-inflammatory [172,173], antibacterial [174,175], and anti-Parkinson agents [176]. In this context, novel series of pyridopyrimidines were synthesized by Basiri et al [177] through a one pot four-component MW-assisted reaction.…”

Synthesis and fungicidal activity of 2‐substituted‐3‐(4‐fluorophenyl)‐benzofuro [3,2‐d] pyrimidin‐4(3H)‐ones

“…Benzofuropyrimidinones are important heterocycles bearing remarkable biological activities. Some of them have shown good analgesic, anti‐inflammatory, and antimicrobial activities [1–3], whereas others exhibited good anticoccidial and blood sugar‐lowering activities [4, 5]. On the other hand, many examples have been demonstrated that incorporation of fluorine atom in molecular structure of heterocyclic compounds often resulted in the improvement of pharmacological properties of the compounds as compared to their non‐fluorine analogs [6, 7].…”