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ASP2151, a novel helicase–primase inhibitor
ASP2151, a novel helicase–primase inhibitor

... complex as a new class of anti-herpesvirus agents. Our medicinal chemistry process was initiated based upon a 2-amino thiazole-containing HSV HPI23 to create more potent virusspecific agents with broader spectra and we consequently selected ASP2151 as a candidate for a novel anti-herpes agent. ASP21 ...
Review on Prodrugs
Review on Prodrugs

... to release the active parent drug, which can then elicit its desired pharmacological effect in the body. In most cases, prodrugs are simple chemical derivatives that are only one or two chemical or enzymatic steps away from the active parent drug. However, some prodrugs lack an obvious carrier or pr ...
Supplementing for Joint Health
Supplementing for Joint Health

effects of cytochrome p450 enzyme inhibitors on the
effects of cytochrome p450 enzyme inhibitors on the

Martindale: The Complete Drug Reference
Martindale: The Complete Drug Reference

View eBook - Absorption Systems
View eBook - Absorption Systems

The Dopamine Transporter and Cocaine Medication Development
The Dopamine Transporter and Cocaine Medication Development

... use of nonhuman subjects that are anatomically and physiologically similar to humans have allowed for the development of a clear and clinically relevant characterization of medication effectiveness in subjects with a documented history of drug use under well controlled laboratory conditions. The pro ...
Prodrugs—from Serendipity to Rational Design
Prodrugs—from Serendipity to Rational Design

... to release the active parent drug, which can then elicit its desired pharmacological effect in the body. In most cases, prodrugs are simple chemical derivatives that are only one or two chemical or enzymatic steps away from the active parent drug. However, some prodrugs lack an obvious carrier or pr ...
The challenge of selecting protein kinase assays
The challenge of selecting protein kinase assays

Product Monograph
Product Monograph

OpioidAnalgesics_2
OpioidAnalgesics_2

Meropenem-Clavulanic Acid Has High In Vitro Activity against Multidrug-Resistant Mycobacterium tuberculosis
Meropenem-Clavulanic Acid Has High In Vitro Activity against Multidrug-Resistant Mycobacterium tuberculosis

  GLYCYRRHIZA GLABRA Review Article LAKSHMI T
  GLYCYRRHIZA GLABRA Review Article LAKSHMI T

... Glycyrrhizinic  acid,  a  major  component  of  licorice,  has  antiulcer  effect  by  raising  the  local  concentration  of  prostaglandins  that  promote  mucous  secretion  and  cell  proliferation  in  the  stomach.  In  vitro  activity  of  Extractum  liquiritiae  (EL),  glycyrrhizic  acid  (G ...
Potent inhibition of human cytochrome P450 3A isoforms
Potent inhibition of human cytochrome P450 3A isoforms

Neurochemical Neutralization of Methamphetamine With High
Neurochemical Neutralization of Methamphetamine With High

... on both dopaminergic and serotonergic nerves requires the transport of METH into the nerve terminals (Seiden et al., 1993). Thus, transport of METH into nerve terminals is the crucial first step in the production of METH-associated pharmacological and toxicological effects. Compounds that bind to bi ...
Morphine Glucuronidation and Glucosidation Represent
Morphine Glucuronidation and Glucosidation Represent

... 12 rpm for 4 hours. Control experiments were also performed with phosphate buffer or HLM (0.5 mg/ml) and BSA (2% w/v) on both sides of the dialysis cells at low and high concentrations of morphine to ensure that equilibrium was attained. A 200-ml aliquot was collected from each compartment, treated ...
Chemical, pharmacokinetic and pharmacodynamic properties of
Chemical, pharmacokinetic and pharmacodynamic properties of

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PhD thesis

patrick_tb_ch22
patrick_tb_ch22

Captopril Ameliorates Myocarditis in Acute
Captopril Ameliorates Myocarditis in Acute

Uptake of Methotrexate, Aminopterin, and
Uptake of Methotrexate, Aminopterin, and

... which have recently been described, the 3 drugs are stoichiometrically equivalent in potency between 0 and 80% inhibition ofenzyme activity (17). Enzyme Assay. Folate reductase in intestinal supernatants from untreated mice was titrated with drugs in a manner similar to that described by Werkheiser3 ...
www.chembio.umich.edu
www.chembio.umich.edu

... Statistical analysis. For comparisons of treatment groups, a one-way ANOVA followed by Bonferroni post hoc analysis using GraphPad Prism Software (version 4.01) was done. Statistical significance was achieved when P < 0.05. ...
Evaluation of the use of static and dynamic models to predict drug
Evaluation of the use of static and dynamic models to predict drug

low-dose diuretics for first-line and combined treatment of
low-dose diuretics for first-line and combined treatment of

... with a reduced risk of CHD in the clinical trials. There are also other possible explanations. Hyperglycemia It has been known for decades that thiazide diuretics are associated with an increased risk of the development of diabetes. At lower doses of chlorthalidone (12.5-25 mg/day), this effect is m ...
okf"kZd izfrosnu@Annual Report 2014-15
okf"kZd izfrosnu@Annual Report 2014-15

< 1 ... 3 4 5 6 7 8 9 10 11 ... 70 >

Discovery and development of ACE inhibitors



The discovery of an orally inactive peptide from snake venom established the important role of angiotensin converting enzyme (ACE) inhibitors in regulating blood pressure. This led to the development of Captopril, the first ACE inhibitor. When the adverse effects of Captopril became apparent new derivates were designed. Then after the discovery of two active sites of ACE: N-domain and C-domain, the development of domain-specific ACE inhibitors began.
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