Angiotensin I converting enzyme ACE inhibitors

Inhibitors of the angiotensin I-converting enzyme (ACE-inhibitors) have been introduced into cardiovascular medicine, in particular for the treatment of hypertension and congestive heart failure (CHE). 

Wijesekara, I. and Kim, S. K. (2010). Angiotensin-i-converting enzyme (ace) inhibitors from marine resources Prospects in the pharmaceutical industry. Mar. Drugs 8,1080-1093. 

Je, J. Y., Park, J. Y., Jung, W. K., Park, P. J., and Kim, S. K. (2005a). Isolation of angiotensin I converting enzyme (ACE) inhibitor from fermented oyster sauce, Crassostrea gigas. Food Chem. 90, 809-814. 

Lisinopril is an angiotensin I-converting enzyme (ACE) inhibitor. It competitively inhibits ACE, prevents angiotensin I conversion to angiotensin II, and is a potent vasoconstrictor that also stimnlates aldosterone secretion. Results are a decrease in sodinm and fluid retention, a decrease in BP, and increase in dinresis. It is indicated in the treatment of hypertension treatment of heart failure not responding to dinretics and digitalis and treatment of acute MI within 24 honrs in hemodynamically stable patients. 

Peptidyl-dipeptidase A (angiotensin-I converting enzyme, ACE, EC 3.4.15.1) plays a pivotal role in the control of blood pressure [80]. It has been established that its active site contains an essential Zn-atom that functions like that of carboxypeptidase A [2], ACE is inhibited by peptides having a proline or aromatic amino acid at the C-terminal position. These observations as well as the similarities with the active site of carboxypeptidase A have allowed a rational design of effective inhibitors of ACE (e.g., captopril (3.4) and enalapril (3.5)) used in the treatment of hypertension [81]. 

Synthetic peptide inhibitors have been developed for a variety of proteases [199-204]. Peptide inhibitors of the metalloprotease angiotensin I converting enzyme (ACE) are of major importance as hypertensive agents [13, 31]. A variety of peptides derived from protease-catalyzed hydrolysis of com cc-zein [202-203] or of wheat germ protein [199, 204] inhibit ACE (Table 6). The most potent of such plant-derived ACE inhibitory peptides is Ile-Val-Tyr (IVY) (Ki 0.1 xM) [199, 204], Further plant-derived peptide ACE inhibitors include the tripeptide glutathione [73, 82], the glutathione -related peptide Y-L-glutamyl-(+)-allyl-L-cysteine sulphoxide [73, 82, 200, 201] and the tripeptide His-His-Leu (HHL) from fermented soybean [201] (Table 6). 

The angiotensin I-converting enzyme (ACE) participates in regulating blood pressure in the renin-angiotensin system. The inhibitors such as captopril (Suetsuna and Chen, 2001) and enalapril (Sawayama et ah, 1990) have been used as antih)/pertensive drugs. The ACE-inhibitory activity of various source have studied, and it was found that some ACE-inhibitory peptides were produced by enzymatic digestion of various marine food proteins, including tuna muscle (Kohama et al., 1991 Qndetti, 1977), sardine muscle (Suetsima et al., 1991), dried bonito (Yokoyama et ah, 1992), dried-salted fish (Astawan et ah, 1995), fish sauce (Okamoto et al, 1995), and fish water-soluble protein (Wako et ah, 1999). 

The only other application of hydroformylation applied to the synthesis of a pharmaceutical intermediate on a commercial scale has recently been reported. The synthesis of (S)-allysine ethylene acetal, an intermediate in the manufacmre of angiotensin I-converting enzyme (ACE) and neutral endopeptidase (NEP) inhibitors, was reported by researchers at Dr. Reddy s and Chirotech using a combination of... 

Friedman, D. I. and G. L. Amidon. Passive and carrier-mediated intestinal absorption components of two angiotensin converting enzyme (ACE) inhibitor prodrugs in rats enalapril and fosinopril. Pharm. Res. 1989, 6, 1043-1047. 

Chemical Class-. Angiotensin-converting enzyme (ACE) inhibitor, nonsulfhydryl I Clinical Pharmacology ... 

Hyperkalaemia, not surprisingly, is the most important side effect of these drugs and can be dangerous in patients who are taking K-i- supplements or other K-i--sparing diuretics. Concomitant use of angiotensin-converting enzyme (ACE) inhibitors and NSAIDs can also exacerbate hyperkalaemia. 

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