Nifedipine chemistry

Beaune, P.H., Kremers, P., Wolff, T. and Waxman, W.J. (1986) Characterization of rat and human liver microsomal cytochrome P-450 forms involved in nifedipine oxidation, a prototype for genetic polymorphism in oxidative drug metabolism. The Journal of Biological Chemistry, 261, 5051-5060. 

Theoretically it should be possible to classify the slow channel blockers according to whether or not they affect the kinetics of slow channel transport. In this way we could readily separate the nifedipine type of drugs from those that are more like verapamil. Alternatively can these drugs be subgrouped according to their chemistry This possibility seems to be remote. Thus diltiazem is a benzothiazepine derivative (Figure 1 nifedipine is derived from dihydropyridine whilst verapamil has some structural features in common with papaverine. 

Blood Chemistry. Results of biochemical measurement in blood are shown in Table I. Nifedipine treatment had no effect on plasma cholesterol levels of rabbits maintained on standard diet or 2% cholesterol diet. 

Pharmaceutical chemists, too, have evinced a keen interest in DHA chemistry, particularly the 4-aryldihydropyridines, which exhibit powerful vasodilating activities via the blocking of calcium channels and modifying movement of Ca2+ into and within the cell. The explosion in activity in this area of heterocyclic synthesis has produced an exponential growth in patent applications and papers and has led to the marketing of a new drug, nifedipine (4).6 Other active 4-aryldihydropyridine derivatives, such as nimodipine and nicardipine (cerebral vasodilators) and nitrendipine (antihypertensive), are presently under clinical trials.7 An excellent list of other practical applications of dihydropyridines has been collected by Kuthan and Kurfiirst.2... 

This reaction produces symmetrical dihydropyridines whose chemistry can be traced back to the late 1800s, biochemistry shortly thereafter, and pharmacology relevant to the present indication to the early 1970s. ( though its precursor nifedipine suffered from too short a half-life, if anything, 20 may now have too long a half-life, and T3 ratios can vary in the natural hormone. 

Peng HM, Auchus RJ (2014) Two surfaces of cytochrome 65 with major and minor contributions to CYP3A4-catalyzed steroid and nifedipine oxygenation chemistries. Arch Biochem Biophys 541 53-60... 

CYP3A4-catalyzed steroid and nifedipine oxygenation chemistries. Arch Biochem Biophys 541 53-60... 

Nifedipine (Procardia and Adalat) belongs to a class of drugs called calcium channel blockers and is effective in the treatment of various types of angina, including that induced by exercise. Show how nifedipine can be synthesized from 2-nitrobenzaldehyde, methyl acetoacetate, and ammonia. Hint Review the chemistry of your answers to Problems 19.43 and 19.54 and then combine that chemistry to solve this problem.)... 

Abstract Some innovative S3mthetic methods in organic chemistry are concisely presented, multicomponent reactions, specifically the Ugi multicomponent reaction, parallel syntheses and combinatorial chemistry, mechanochemically promoted organic reactions, organic reactions promoted by microwave irradiation and syntheses in ionic liquids. Examples of chemoselective or as3mimetric syntheses completed by one of the presented specific methods are presented for the antihy-pertensive drug nifedipine, the alkaloid tropinone, the local anesthetic xylocaine and the HIV inhibitor tipranavir. 

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