The Hantzsch dihydropyridine synthesis is found to benefit from .

BACE-1 has been shown to be an attractive therapeutic target in Alzheimer's disease (AD). Using a 1,4-dihydropyridine (DHP) scaffold, we synthesized new inhibitors of BACE-1 by modifying the known BACE inhibitor 2 containing a hydroxyethylamine (HEA) motif. Using structure-based drug design based on computer-aided molecular docking, the isophthalamide ring of 2 was replaced with a 1,4-dihydropyridine ring as a brain-targeting strategy. Several of the new dihydropyridine derivatives were synthesized and their BACE-1-inhibitory activities were evaluated using a cell-based, reporter gene assay system that measures the cleavage of alkaline phosphatase (AP)-APP fusion protein by BACE-1. Most of the 1,4-DHP analogs showed BACE-1-inhibitory activities with IC50 values in the range 8-30 μM, suggesting that the 1,4-DHP skeleton may be utilized to develop brain-targeting BACE-1 inhibitors.

T1 - Synthesis of new 1,4-dihydropyridine derivatives containing thiazolyl substituents
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AB - A series of 4-[2-methyl (or aryl) thiazole-4-yl]-2,6-dimethyl-3,5-diacetyl (or dibenzoyl) 1,4-dihydropyridines were synthesized using a modified Hantzsch reaction involving the condensation of the corresponding aldehyde with acetyl acetone or benzoyl acetone. The preparation of the corresponding aldehydes (2-methylthiazole-4-carboxaldehyde and some 2-arylthiazole-4-carboxaldehydes) was achieved by a simplified protocol of the published synthesis.


A conventient one-step synthesis of spirodihydropyridines

Dihydropyridine synthesis - Organic chemistry
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N2 - A series of 4-[2-methyl (or aryl) thiazole-4-yl]-2,6-dimethyl-3,5-diacetyl (or dibenzoyl) 1,4-dihydropyridines were synthesized using a modified Hantzsch reaction involving the condensation of the corresponding aldehyde with acetyl acetone or benzoyl acetone. The preparation of the corresponding aldehydes (2-methylthiazole-4-carboxaldehyde and some 2-arylthiazole-4-carboxaldehydes) was achieved by a simplified protocol of the published synthesis.


Step 3: Formation of the dihydropyridine

The Hantzsch pyridine synthesis or Hantzsch dihydropyridine synthesis is a between an such as , 2 equivalents of a such as and a nitrogen donor such as or . The initial reaction product is a dihydropyridine which can be in a subsequent step to a . The driving force for this second reaction step is . This reaction was reported in 1881 by .

The new generation dihydropyridine type calcium ..

We have recently reported () that some multicompound 1, 4-dihydro pyridine derivatives with anti cancer aganist human cancer cell line (MCF-7, Hela and Hep) and (). In this study, we have reported newly synthesized multi compound 1, 4-dihydropyridine connected with 1, 3, 4-oxadiazoles and 1, 2, 4-triazole derivatives for improve the ability of anticancer and antimicrobal effects and with specified structural activity features with corresponding bilogical screnning.