71834-42-9

Upstream product

• 100-52-7 benzaldehyde 
• 99-91-2 para-chloroacetophenone 
• 22966-22-9 (E)-1-(4-chlorophenyl)-3-phenyl-2-propen-1-one 
• 17356-08-0 thiourea 
• 66443-36-5 4-(4-chloro-phenyl)-6-phenyl-1⁽³⁾H-pyrimidine-2-thione 
• 1147550-11-5 ammonium thiocyanate 

Downstream Products

• 511309-26-5 C₁₈H₁₃ClN₂OS 

Relevant academic research and scientific papers

Novel potent and selective DPP-4 inhibitors: Design, synthesis and molecular docking study of dihydropyrimidine phthalimide hybrids

Background: Dipeptidyl peptidase-4 (DPP-4) inhibitors have emerged as antihyperglycemic agents that improve glycemic control in type 2 diabetic patients, either as monotherapy or in combination with other antidiabetic drugs. Methods: A novel series of dihydropyrimidine phthalimide hybrids was synthesized and evaluated for their in vitro and in vivo DPP-4 inhibition activity and selectivity using alogliptin as reference. Oral glucose tolerance test was assessed in type 2 diabetic rats after chronic treatment with the synthesized hybrids ± metformin. Cytotoxicity and antioxidant assays were performed. Additionally, molecular docking study with DPP-4 and structure activity relationship of the novel hybrids were also studied. Results: Among the synthesized hybrids, 10g, 10i, 10e, 10d and 10b had stronger in vitro DPP-4 inhibitory activity than alogliptin. Moreover, an in vivo DPP-4 inhibition assay revealed that 10g and 10i have the strongest and the most extended blood DPP-4 inhibitory activity compared to alogliptin. In type 2 diabetic rats, hybrids 10g, 10i and 10e exhibited better glycemic control than alogliptin, an effect that further supported by metformin combination. Finally, 10j, 10e, 10h and 10d had the highest radical scavenging activity in DPPH assay. Conclusions: Hybrids 10g, 10i and 10e are potent DPP-4 inhibitors which may be beneficial for T2DM treatment.

Efficient ionic liquid-catalysed synthesis and antimicrobial studies of 4,6-diaryl- and 4,5-fused pyrimidine-2-thiones

One-pot three-component condensation of aromatic ketones (1-tetralones, acetophenones, indane-1,3-dione), substituted aromatic aldehydes and thiourea in the presence of N-methylpyridinium tosylate under solvent free conditions at 100-110 °C for 2-4 h afforded tetrahydrobenzo[h]quinazoline-2-thiones, pyridimidine-2-thiones and indeno-pyrimidine-2-thiones in excellent yields. All synthesised thiones were screened for their antimicrobial activities.

Behaviour of 4,6-diaryl-2(1H) pyrimidine-2-thiones towards some electrophiles and nucleophiles

4,6-DIARYl-1,2-dihydro-2(1H)-pyrimidine-2-thiones (1a,b) were ....used for the synthesis of several new pyrimidine derivatives. They were further subjected to hetero ring anellation affording isoxazolo [4,5-d] thiazolo [2,3-A] pyrimidine (5,6) and isoxazolo [4,5-d] thiazino [2,3-A] pyrimidines (11,12). Biological evaluation of some of the prepared compounds revealed promising antimicrobial activity.