medchem

which is the least common drug target for commercial drugs?

carbohydrates

carbohydrates play critical roles in many biological processes, including

cell-cell communication and cell signaling

common drug targets for the development of commercial drugs

Enzymes, receptors, membrane transport proteins, and DNA

Enzymes catalyze

biochemical reactions

Enzymes can be targeted to

either activate or inhibit biochemical reactions activity.

Receptors are

proteins that bind to specific molecules,

Receptors are proteins that bind to specific molecules, such as

hormones, neurotransmitters, or drugs,

Receptors initiate a

signal transduction pathway.

Membrane transport proteins regulate

the transport of substances across cell membranes.

DNA can be targeted by drugs that

interfere with DNA replication or transcription,

DNA can be targeted by drugs that interfere with DNA replication or transcription, which can be used to treat

cancer and other diseases.

Which effect does an antagonistic drug have?

An antagonistic drug inhibits the signaling of a receptor.

Antagonistic drugs bind to

the same receptor as an agonist,

an agonist is a molecule that

activates the receptor,

but Antagonistic drugs do not activate the receptor. Instead, antagonists

block or reduce the activity of the receptor,

antagonists block or reduce the activity of the receptor, thereby inhibiting the ? response

physiological

antagonists block or reduce the activity of the receptor, thereby inhibiting the physiological response that would have been

initiated by the agonist.

Antagonistic drugs are commonly used in pharmacology to treat a variety of conditions, including

hypertension, asthma, and anxiety disorders.

Which bond is the strongest?

A covalent bond

Van der Waals, hydrogen, dipole-dipole, and ion-dipole bonds are all

intermolecular forces that hold molecules together

covalent bonds are

intramolecular forces that hold atoms together within a molecule.

Covalent bonds involve

the sharing of electrons between atoms,

Covalent bonds involve the sharing of electrons between atoms, resulting in a

strong, stable bond.

Covalent bond is formed when

two atoms share a pair of electrons in their outermost shell.

Covalent bonds are typically stronger than the other types of bonds listed because they involve

the sharing of electrons between atoms, Covalent bonds are typically stronger than the other types of bonds listed because they involve the sharing of electrons between atoms, resulting in a stronger electrostatic attraction between the atoms.

SAR studies involve modifying

the chemical structure of a drug molecule

SAR studies involve measuring its

biological activity

SAR studies involve measuring its biological activity to determine

how specific structural features contribute to the drug's activity.

The goal of SAR studies is to

identify the key structural features that are responsible for the drug's activity,

the information of SAR studies is used to

design and optimize new drug candidates

the information of SAR studies is used to design and optimize new drug candidates with

improved potency, selectivity, and pharmacokinetic properties.

SAR studies are a critical step in drug discovery and development, as they provide insights into

the molecular mechanisms of drug action

SAR studies help guide

the design of new drugs with improved therapeutic properties.

What does the D in the abbreviation ADMET properties of drugs stand for?

Distribution.

ADMET

absorption, distribution, metabolism, excretion, and toxicity.

absorption, distribution, metabolism, excretion, and toxicity are the key factors that determine

the pharmacokinetic and pharmacodynamic properties of drugs in the body.

Distribution refers to the process by which a drug is

transported from the bloodstream to its site of action, and also to other tissues in the body.

the distribution process is influenced by various factors, such as

the drug's chemical properties, binding to plasma proteins, and its ability to cross cell membranes.

Understanding a drug's distribution properties is important for

optimizing its therapeutic efficacy, minimizing toxicity, and determining appropriate dosing regimens.

arrange atom (bromine, chloride, fluorine, hydrogen, and nitrogen) in order of increasing electronegativity?

H, Br, Cl, N, F

Electronegativity is a measure of

the tendency of an atom to attract electrons towards itself in a covalent bond.

the most electronegative element

Fluorine

the least electronegative element

hydrogen

What technique is mainly used for solution conformational studies of lead compounds?

NMR (nuclear magnetic resonance)

NMR

nuclear magnetic resonance

NMR spectroscopy is a powerful tool for studying

the conformational properties of organic molecules in solution

In NMR, the sample is subjected to

a strong magnetic field,

In NMR, the sample is subjected to a strong magnetic field, which causes

the nuclei of certain atoms to absorb and re-emit electromagnetic radiation at characteristic frequencies.

By analyzing these characteristic frequencies, NMR can provide detailed information about

the molecular structure and conformation of the sample.

NMR is particularly useful for studying the conformational properties of lead compounds, as it can reveal important information about

the interactions between the lead compound and its target receptor or enzyme.

NMR information can be used to

guide the design and optimization of new drug candidates with improved potency and selectivity.

Which is a false statement regarding non-competitive enzyme inhibitor? (a) It binds to an allosteric site of the enzyme (b) It does not compete with the natural substrate for binding to the active site of the enzyme (c) Its binding to the enzyme can induce a conformational change of the enzyme (d) It can be used in combination therapies with a competitive inhibitor (e) It usually is a mimic of the natural enzyme substrate

(e) It usually is a mimic of the natural enzyme substrate.

Non-competitive enzyme inhibitors bind to

an allosteric site of the enzyme,

an allosteric site of the enzyme, is a different site from the active site. Once bound, they induce a

conformational change of the enzyme

an allosteric site of the enzyme, is a different site from the active site. Once bound, they induce a conformational change of the enzyme that

reduces its catalytic activity towards the substrate.

Non-competitive inhibitors bind to

an allosteric site of the enzyme,

Non-competitive inhibitors bind to an allosteric site of the enzyme, rather than

the active site,

Non-competitive inhibitors do not

compete with the natural substrate for binding.

Binding of a non-competitive inhibitor to the enzyme can induce

a conformational change in the enzyme

Binding of a non-competitive inhibitor to the enzyme can induce a conformational change in the enzyme, leading to

a decrease in its catalytic activity towards the substrate.

Non-competitive inhibitors can be used in

combination therapies

Non-competitive inhibitors can be used in combination therapies with a

competitive inhibitor

Non-competitive inhibitors can be used in combination therapies with a competitive inhibitor to

enhance the overall efficacy of the treatment.

What is a correct statement regarding the preferred metabolism of a drug? (a) There should be no metabolism at all (b) The metabolism should be very fast (c) The metabolism should take place in the kidneys (d) The metabolites should not be toxic (e) The metabolites should be excreted through exhalation

(d) The metabolites should not be toxic.

Drug metabolism refers to

the chemical reactions that occur in the body to convert a drug into other compounds (metabolites) that can be eliminated from the body.

Ideally, the metabolites should be

non-toxic and easily eliminated from the body

Ideally, the metabolites should be non-toxic and easily eliminated from the body to

prevent harmful effects.

Cell membranes are ? in nature.

fluid and dynamic

Cell membranes - The phospholipid bilayer provides a

flexible barrier

Cell membranes - The phospholipid bilayer allows for

various membrane-associated processes to occur.

Proteins play a key role in cell membrane function, including

transport of molecules and signaling.

The basic structure of a cell membrane is

a phospholipid bilayer, with hydrophilic heads facing the exterior and interior of the membrane and hydrophobic tails facing each other.

The basic structure of a cell membrane is a phospholipid bilayer, with hydrophilic heads facing

the exterior and interior of the membrane

The basic structure of a cell membrane is a phospholipid bilayer, with hydrophobic tails facing

each other.

The interior of a membrane is

lipophilic, or hydrophobic,

The interior of a membrane is lipophilic, or hydrophobic, due to

the presence of the nonpolar fatty acid tails of the phospholipids.

The exterior of a membrane is

hydrophilic, or polar,

The exterior of a membrane is hydrophilic, or polar, due to

the presence of the polar head groups of the phospholipids and other polar molecules.

Proteins are an integral part of the ? of cell membranes.

structure and function

An inhibitor has a Ki of 0.1 uM in its interaction with an enzyme. What then are the Ka and Kd values of the same interaction?

The Lipinski's rule of five includes the following four characteristics for oral drugs:

(a) Molecular weight (MW) less than or equal to 500 daltons. (b) No more than 5 hydrogen bond donors (nitrogen or oxygen atoms with a hydrogen atom attached). (c) No more than 10 hydrogen bond acceptors (nitrogen or oxygen atoms). (d) Octanol-water partition coefficient (log P) less than or equal to 5.

Hydrogen bond donors are

atoms with a hydrogen atom attached to an electronegative atom,

hydrogen bond donor examples

nitrogen (N), oxygen (O), or fluorine (F).

In a molecule, hydrogen bond donors can be identified by

looking for the presence of these electronegative atoms that are bonded to a hydrogen atom.

in water (H2O), the ? atom is an hydrogen bond acceptor,

oxygen

in water (H2O) the ? atoms are hydrogen bond donors.

two hydrogen

in ammonia (NH3), the ? atom is a hydrogen bond acceptor,

nitrogen

in ammonia (NH3), the ? atoms are hydrogen bond donors.

three hydrogen

a molecule with ? hydrogen bond donors is less likely to pass Lipinski's rule of five for oral drugs.

more than five

steps To find the molecular weight of a compound,

1.Determine the chemical formula of the compound, which tells you the types and numbers of atoms in the molecule. 2. Look up the atomic weight of each element in the periodic table. 3. Multiply the atomic weight of each element by the number of atoms of that element in the molecule. 4. Add up the results from step 3 to get the molecular weight.

Which is a false statement regarding solid-phase synthesis? (a) It simplifies removal of solvents (b) It simplifies automation of reactions (c) It simplifies monitoring of reactions (d) It simplifies reproducibility of reactions (e) It simplifies removal of soluble reagents

(e) It simplifies removal of soluble reagents.

Solid-phase synthesis simplifies

the removal of solvents and soluble by-products,

In solid-phase synthesis, the reactants are typically

immobilized on a solid support,

In solid-phase synthesis, The use of solid support also simplifies

automation, monitoring, and reproducibility of reactions.

What effect does an agonistic drug have?

It promotes the signalling of a receptor

which is the most common drug target for commercial drugs?

enzymes

What does the E in the abbreviation ADMET properties of drugs stand for?

excretion

What is the purpose of structure-activity-relationship (SAR) studies?

To determine which atoms or functional groups are important to the activity of a drug.

The A in the abbreviation ADMET properties of drugs stands for

Absorption.

arrange atoms (bromine, chloride, fluorine, hydrogen, and nitrogen) in order of increasing electronegativity?

Br, H, Cl, F, N.