103295-96-1

Upstream product

• 1694-31-1 tert-butyl acetoacetate 
• 99-61-6 3-nitro-benzaldehyde 

Downstream Products

• 108931-51-7 1,4-dihydro-2-methoxy-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid,1,1-dimethylethyl ester 
• 108932-39-4 1,4-dihydro-2-[[(4-methoxyphenyl)methyl]thio]-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, 1,1-dimethylethyl ester 
• 108956-94-1 1,4-Dihydro-2-[[(4-methoxyphenyl)methyl]thio]-6-methyl-4-(3-nitrophenyl)-5-pyrimidinecarboxylic acid, 1,1-dimethylethyl ester, monohydrochloride 
• 112080-28-1 tert-butyl 6-methyl-4-(3-nitrophenyl)-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate 
• 103521-70-6 (+/-)-Mebudipine 

Relevant academic research and scientific papers

Synthesis and biological activity of two new calcium-channel blockers, mebudipine and dibudipine

Dihydropyridine derivative calcium-channel blockers are widely used in the therapy of hypertension, angina pectoris and other cardiovascular diseases. Because the prototype of dihydropyridine derivatives, nifedipine, does not have the optimum pharmacokinetic and pharmacodynamic characteristics, attempts have been made to synthesize other drugs in this class with improved properties. The synthesis and biological activity of two new calcium-channel blockers, non-symmetrical (mebudipine) and symmetrical (dibudipine) analogues of nifedipine, is described herein. The pharmacological potencies of the compounds were evaluated by studying their effects on the contractions of isolated guinea-pig ileum and rat aortic rings. Results were compared with those obtained from nifedipine. The new analogues and nifedipine inhibited the contractile response of guinea-pig ileum to electrical stimulation and the pIC50 value of the compounds did not differ significantly from each other. The compounds also antagonized the contractile responses of K+ -depolarized guinea-pig ileum to cumulative concentrations of calcium. The inhibitory effect of mebudipine was significantly higher than that of nifedipine whereas the inhibitory effects of dibudipine and nifedipine were not different. All three compounds relaxed KC1 (40 mM)-treated isolated aortic rings; the pIC50 values for relaxation were: mebudipine > nifedipine > dibudipine. It is concluded that these new dihydropyridine derivatives are potent relaxants of vascular and ileal smooth muscles and therefore have high potential for use as antihypertensive and anti-anginal agents.

Design and synthesis of 4-alkyl-2-amino(acetamino)-6-aryl-1,3-thiazine derivatives as influenza neuraminidase inhibitors

With a convenient and economical method, two series of 1,3-thiazine derivatives 1 and 2 were synthesized, and their neuraminidase (NA) inhibitory activities were evaluated. The pharmacological results showed that most of the compounds have potent NA inhibitory activity. Especially, 1g exhibited the best activity against influenza virus A (H1N1) NA (IC50 = 29.06 μg/mL), and its crystal structure was determined by single-crystal X-ray diffraction. The preliminary biological assay indicated that 1,3-thiazine could be used as a core structure to design novel influenza NA inhibitors. Two series of novel 1,3-thiazine analogs were synthesized and their neuraminidase (NA) inhibitory activities were evaluated. Most of the compounds have potent NA inhibitory activity. Compound 1g exhibited the best activity against influenza virus A (H1N1) NA with an IC50 of 29.06 μg/mL, and its crystal structure was determined by single-crystal X-ray diffraction.

Dihydropyrazolopyrimidine Inhibitors of KV1.5 (IKur)

A series of dihydropyrazolopyrimidine inhibitors of KV1.5 (IKur) have been identified. The synthesis, structure-activity relationships and selectivity against several other ion channels are described.