Inhibitors structural formulas

Therapeutic Function Tyrosine hydroxylase Inhibitor Chetnicel Name tt-Methyl-L-tyrosine Common Name Metirosine Structural Formula ... 

Fig. 9.5 Structural formula of the 17a-hydroxylase-17,20-lyase inhibitor MH61.

Figure 7.1, Structural formulae of some monoamine oxidase inhibitors (moclobemide, pirlindole and toloxatone) and alpha2 adrenoceptor antagonists [S-...

Figure 7.3. Structural formulae of the noradrenaline (norepinephrine)/dopamine reuptake inhibitor amfebutamone (bupropion) and some nonselective noradrenaline and serotonin (5-hydroxytr3 tamine 5-HT) reuptake inhibitors (venlafaxine, and...

Phenols and derivatives are the main aromatic compounds of plants, whose structural formulas contain at least one benzene ring. They serve as odors, fungicidals, or germination inhibitors. Coumarins are especially common in grasses, orchids, citrus fruits, and legumes. Plants containing phenols with anticancer properties include the following ... 

Therapeutic Function Cardiotonic, Platelet aggregation inhibitor Chemical Name lH-Imidazole-4-carboxamide, 5-amino-l(5-D-ribofuranosyl-Common Name Acadesine AICA riboside Arasine Structural Formula ... 

Therapeutic Function Aromatase inhibitor Chemical Name Androsta-l,4-diene-3,17-dione, 1-methyl-Common Name Atamestane Structural Formula ... 

Therapeutic Function Carbonic anhydrase inhibitor. Antiglaucoma Chemical Name 4,5-Dichloro-m-benzenedisulfonamide Common Name Diclofenamid Structural Formula ... 

Therapeutic Function Antidepressant, Monoamine oxidase inhibitor Chemical Name 4-Pyridinecarboxylic acid 2-(l-methylethyl)hydrazide Common Name -Structural Formula ... 

Therapeutic Function Cholinesterase inhibitor, Cognition activator Chemical Name 1-Acridinol, 9-amino-l,2,3,4-tetrahydro-, maleate (1 1) Common Name Velnacrine maleate Structural Formula ... 

Therapeutic Function Acetylcholinesterase inhibitor Chemical Name Ethanone, 2,2,2-trifluoro-l-(3-(trimethylsilyl)phenyl)-Common Name Zifrosilone Structural Formula ... 

The proton pump inhibitor nepaprazole is a racemate. Draw the structural formulae of both -configured isomers. 

The vasopeptidase inhibitor omapatrilat is a pure stereoisomer and its systematic name is (4S,7S,10aS)-5-oxo-4- [(2S)-3-phenyl-2-sulfanylpropan-oyl]amino octahydropyrido[2,l-fo] [ 1,3]thiazepine-7-carboxylic acid. Draw the structural formula of this compound with complete specification of the... 

Similar substituent effects are observed for the anti-MAO activity of / -carbolines and pargyline derivatives (47). In Equation 25, E 6 8 is the sum of values of the 6 and 8 substituents, and o-4b is the o- value of substituents to the 4b position. In Equation 26, E84 corresponds to the para substituent and o-2 to the ortho position of the side chain. The coincidence in the stereoelectronic effects of substituents on the MAO inhibition is surprisingly good for these three classes of inhibitors. On the structural formulas shown above, the arrows indicate positions where the a values are directed, and the shaded circles show sterically limited positions. Thus, the individual correlations are substantiated, and physicochemical significance is proved by similar biological correlations. 

The commercial use of some organophosphates and carbamates as systemic insecticides has resulted in the synthesis of a large number of these anticholinesterases. Structural formulae and some data for these inhibitors are given in the reviews of Usdin (Ul), Aldridge and Reiner (A12), and Main (M4). Compounds which structurally resemble substrates are usually very good inhibitors of plasma cholinesterase. Thus, organophosphorus compounds modeled on acetylcholine are powerful inhibitors of the enzyme (Table 20). Quaternary aminophenylphosphates... 

Figure 5.1. Structural formula of the Abl inhibitor STI-571 (panel 1) and the variant (panel 2) [Refs in 225],...

Fig. 34.9. X-Ray crystallographically determined binding site of Protox [15], including the co-crystallized inhibitor INH (for structural formula see Fig. 34.10) and a part of the co-factor FAD. Highlighted is Arg98 at the entrance of the binding site cavity, interacting with INH and almost all...

Previous editions of Selective Toxicity have been well received, and translated into German, Italian, Japanese, and Russian. This new edition, which reviews the literature up to September 1984, has been thoroughly revised to reflect current awareness of the subject. Many additions have been made, some of them quite substantial, but all blended into the original framework. There are new sections on drugs that influence the immune process, on inhibitors based on the transition state of the molecule, and on IMBIs, which are the irreversible mechanism-based inhibitors. There are new taxonomic tables of bacteria and protozoa, and an index of the 650 structural formulae used in the text. A new section (17.4) provides help in searching for the physical and biological properties of drugs, whether in compilations (books) or in computerized databanks. 

Following are structural formulas for three other angiotensin-converting enzyme (ACE) inhibitors, all members of the pril" family. Which are chiral For each that is chiral, determine the number of stereoisomers possible for it. List the similarities in structure among each of these four drugs. 

Comparison of Acetyl-CoA-Carboxylase (ACC) Inhibitors with Acetolactate Synthase (ALS) Inhibitors The response patterns from four chemically-unrelated herbicides are compared in Figure 4 The structural formulas of the compounds are given in Figure 6 These treatments have been carried out with different amounts of the active ingredients Therefore, one should not look at the bars too quantitatively the increase or decrease of metabolites is what is important ... 

Fig. 7.6 Structural formulas of complexes of enzyme ( receptor ) part (R) and neutral inhibitors with atom numbering. Asterisks exhibit different parts of molecules treated at the different levels of theory. (Reproduced with permission from Ref [77]. Copyright 2011 Elsevier)...

Below two structural formulas of potent, orally active, long-acting morpholine acetal human NK-1 receptor antagonists 195,196, are given. These compounds are tested as efficient drugs for the treatment of the Alzheimer disease [169]. The fluorine-containing biaryl-triazolopyridine 197 is tried as a potent and selective p38a inhibitor for stress relief [170]. 

Flo. 8. Structural formulas of some inhibitors of microsomal drug metabolism. (Conney and Bunts, Advances in Pharmacology, 1, 31, 1962.)... 

Fig. 2. Structural formula for inhibitors, substrate and transition state analogs, and reaction products bound to ribonucleases. Only polar hydrogen atoms are indicated, (cont.)...

Since a knowledge of the correct tautomeric form of the pyrimidines is a requisite for understanding the mode of binding to active sites, as well as nucleic acid structure and modification, the formulae of the conventionally-named 2- and 4-hydroxypyrimidines are presented in the correct lactam, or pyrimidone, form in this chapter. Other physical properties of the pyrimidines, such as dissociation constants, protonation sites, and distribution coefficients, are presented in cases where there is a known relation to drug activity. Biogenesis and enzyme control mechanisms are discussed where they relate to an understanding of inhibitor action. 

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