Synthesis of (2S,4S)-2-Substituted-3- (3-Sulfanylpropanoyl)-6- Oxohexahydropyrimidine-4-Carboxylic  Acids as Potential Antihypertensive Drugs

Еrshov, A. Yu.; Nasledov, D. G.; Lagoda, I. V.; Шаманин, В. В.

doi:10.4236/msce.2015.36002

Cited by 1 publication

(2 citation statements)

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“…Moreover, the presence of Pyro Glu at the N-terminus renders teprotide refractory to amino peptidases; this confers further stability and effectiveness in vivo. Nevertheless, teprotide has a relatively short duration of action and must be given parentally to be effective [11]. The optimum pH of angiotensin converting enzyme was found to vary with the substrate employed and to be influenced by the presence or absence of chloride ion.…”

Section: Chemistrymentioning

confidence: 99%

“…In 1970, Ferreira and Greene [10] isolated and characterized the first peptide, a bradykinin-potentiating pentapeptide that they called BPP5a; it also inhibited ACE and transiently lowered blood pressure in animal models. The significance of ACE in the pathogenesis of hypertension was not fully appreciated until 1977's, when Ondetti [11] first isolated and then synthesized the naturally occurring nonpeptide, teprotide. He proposed a hypothetical model of the active site of ACE and used it to predict and design compounds that would occupy the carboxy-terminal binding site of the enzyme [12].…”

Section: Introduction 11 Angiotensin Converting Enzymementioning

confidence: 99%

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Interaction Studies of ACE Inhibitors with Antidiabetic Drugs

Sattar¹,

Sadia²

2021

Metformin - Pharmacology and Drug Interactions

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Angiotensin converting enzyme (ACE)-inhibitors are effective in patients with mild to moderately severe hypertension, collagen vascular and cardiovascular disease. They are also used in the prevention and treatment of myocardial infarction and in the management of cardiac arrhythmias. Patients with cardiovascular diseases are generally on multiple medicines that’s why it is imperative to study drug–drug interactions of medicines which are commonly taken together in any given case, as combined administration of different medicines can significantly influence the availability of drugs. In the present study we investigated the “in vitro” interactions of ACE inhibitors (enalapril, captopril and lisinopril) with frequently prescribed and co-administered drugs in simulated human body environments. These interactions were monitored by means of UV spectrophotometry and separation technique as RP-HPLC. Prior to start of actual drug interactions, the method of analysis of each drug was established and its various parameters validated for considering its use in testing of drug in vitro as well as in human serum. For this purpose, an attempt was made to develop a number of new HPLC methods for determination of ACE inhibitors (enalapril, captopril and lisinopril) and simultaneously with interacting drugs. These methods were optimized, validated and then successfully employed for the quantitation of enalapril, captopril and lisinopril and selected drugs in interactions studies. As a result, new methods for the quantitation of individual as well as multiple drugs were developed. The interacting drugs selected were antidiabetic drugs (metformin, glibenclamide, glimepride and pioglitazone. Interaction consequences revealed that the availability of enalapril was not affected in presence of antidiabetic drugss whereas the availability of captopril and lisinopril were altered in presence of NIDDMs.

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Section: Chemistrymentioning

confidence: 99%

Section: Introduction 11 Angiotensin Converting Enzymementioning

confidence: 99%