Medicinal Chemistry
were that simple, more and better drugs would already be available. Medicinal chemistry is a science unto itself, a central scie ...
of ways of identifying a potential lead compound, including rational drug design, random high throughput screening, and focused ...
human biochemistry and pathology to drive the design of drug-like molecules engineered to fit precisely into targets of drug act ...
Most drugs are molecules, but most molecules are not drugs. Every year, millions of new molecules are prepared, but only a very ...
A drug molecule possesses one or more functional groups positioned in three-dimensional space on a structural framework that hol ...
the drug entering the bloodstream and being distributed throughout the entirety of the body, or “locally,” which involves site-s ...
the stomach at which point it is subjected to a pH of 1.8–2.2, as well as to a variety of pepsin enzymes. Under such acidic cond ...
phospholipase, ribonuclease, and deoxyribonuclease. The drug designer must consider these environments of varying pH combined wi ...
14 Table 1.2 Ionization Constants of Common Drugs Weak acids pKa Weak bases pKa Acetaminophen 9.5 Alprenolol 9.6 Acetazolamide 7 ...
DRUG MOLECULES: STRUCTURE AND PROPERTIES 15 active at an oral dose of 0.1 mg, then fillers are necessary to ensure that the pill ...
16 MEDICINAL CHEMISTRY Table 1.3 Percentage Protein Binding for Common Drugs 99% 95–99% 90–95% 50–90% <50% Levothyroxine Amit ...
the blood–brain barrier and most drugs designed to enter the brain will likewise traverse the maternal–placental barrier. 1.1.2. ...
18 Table 1.4 Half-Lives of Selected Drugs in Patients (with Normal Renal Function) <1 h 1–4 h 4–12 h 12–24 h 1–2 days >2 d ...
1.1.3 Structural Fragments of a Drug Molecule: Pharmacophore, Toxicophore, Metabophore As previously defined, a drug molecule co ...
arrangement of atoms in a drug molecule that are responsible for the metabolic properties. Since functional groups are responsib ...
1.1.4 Structural Fragments of Drug Molecules: Interchangeable Bioisosteres A drug molecule may be conceptualized as a collection ...
22 Classical bioisosteres Monovalent atoms or groups: OH SH Br I NH PH -Pr 2 2 i CH 3 CI F H CH 2 COCH R 2 CONHR NH O S CO R 2 ...
These properties dictate the therapeutic, toxic, and metabolic characteristics of the over- all drug molecule. These properties ...
difficult to predict and to engineer with insight into a molecule. Accordingly, extensive use is now made of quantum mechanics a ...
1.2.1 Role and Structure of Water: Influence on Drug Structure Life is based on water, the major constituent of living organisms ...
«
1
2
3
4
5
6
7
8
9
10
»
Free download pdf