Module 1.4: Medicinal Chemistry Flashcards by Robea May Martin

SAR adrenergic Agonist: Substitution at R2

Increase in alpha 2 activity

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SAR adrenergic Agonist: Substitution at R2

Increases B-activity
Increase CNS & Oral activity
Decrease degradation by MAO

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SAR adrenergic Agonist: Aromatic Substitution

3-OH is for Alpha activity
* 4-OH is for Beta activity
* 3&4-OH – both

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SAR adrenergic Agonist: Aromatic Substitution
3-OH is for
* 4-OH is for
* 3&4-OH – both

3-OH is for Alpha activity
* 4-OH is for Beta activity
* 3&4-OH – both

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SAR adrenergic Agonist: aromatic substitution at3 and 4
___, ____ oral activity

Polar, decreases oral activity

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SAR adrenergic Agonist: aromatic sustitution: Metabolized by ___ leading to Shorter DOA

COMT

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SAR adrenergic Agonist: aromatic sustitution: Metabolized by COMT leading to _____

Shorter DOA

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Adrenergic agonist means

Sympathomimetic activity

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SAR of Adrenergoc Agonist:
Lack of 1 OH –__
▪ Absence of both OH – __

resistance to COMT
indirect activity

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Adrenergic agonist means

Fight or flight response: Sympathomimetic

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SAR adrenergic Agonist: Aromatic Substitution
3-OH replacement by ___ 3-OH replacement by _________ will
→increase Beta activity
→ decrease degradation by COMT

Methanol

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SAR adrenergic Agonist: Aromatic Substitution Moving 4-OH to 5-OH will
___
____

→increase B2 activity
→ decrease degradation by COMT

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SAR adrenergic Agonist: Aromatic Substitution
Moving____ will
→increase B2 activity
→ decrease degradation by COMT

4-OH to 5-OH

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SAR of Adrenergoc Agonist:
____ – resistance to COMT
_____- indirect activity

Lack of 1 OH
Absence of both OH –

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
pharmacopore

Quinazoline

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SAR of Adrenergoc ANTAGONIST: ____

Sympatholitic

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
Prototype

Prazosin

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SAvR of Adrenergoc ANTAGONIST: Alpha blocker
____ is essential for the activity

4-amino group

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
__ 2nd position of quinazoline

Piperazine

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
Positions __, __, __, __ can be varied

5,6,7,8

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
Can be any heterocyclic ring

Piperazine

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SAR of Adrenergoc ANTAGONIST: Alpha blocker
examples

Piperazine and piperadine

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SAR of Adrenergoc ANTAGONIST: BETA blocker
Pharmacopore

Aryloxopropanol

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SAR of Adrenergoc ANTAGONIST: BETA blocker
Prototype

Propranolol

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SAR of Adrenergoc ANTAGONIST: BETA blocker ____ can be varied with other heteroaromatic ring

Aryl ring

SAR of Adrenergoc ANTAGONIST: BETA blocker __, and __ both beneficial to activity

Branching & extension

SAR of Cholinergic agonists: ___

parasympathomimetic

SAR of Cholinergic agonists: Direct Acting Pharmacopore

Acetylcholine

SAR of Cholinergic agonists: Direct Acting Prototype

Acetylcholine

SAR of Cholinergic agonists: Direct Acting Acetylcholine components Functional group

- Acetoxy/Ester Portion * Ethylene Bridge * Quaternary Nitrogen All are essential for the activity – overall size of the molecule should not be altered

SAR of Cholinergic agonists: Direct Acting Acetylcholine components Functional group All are essential for the activity – overall size of the molecule ___ be altered

should not

SAR of Cholinergic agonists: Direct Acting _____ * The methyl group cannot be extended but may be replaced with NH2 (Carbamate) * Not easily hydrolyzed * Longer DOA

Acetoxy/Ester Portion

SAR of Cholinergic agonists: Direct Acting Acetoxy/Ester Portion * ____ cannot be extended but may be replaced with NH2

The methyl group

SAR of Cholinergic agonists: Direct Acting _____ cannot be altered

Ammonium group

SAR of Cholinergic agonists: Direct Acting Acetoxy/Ester Portion Not easily ____ Longer ___

hydrolyzed DOA

SAR of Cholinergic agonists: Direct Acting ___: Addition of methyl increase muscarinic selectivity; longer duration of action

choline/ ethylene bridge

SAR of Cholinergic agonists: INDIRECT Acting - Prototype: Physostigmine * Equivalent to the ester of acetylcholine (recognize by AChE but not easily hydrolyzed by the enzyme

Carbamate

SAR of Cholinergic agonists: Direct Acting choline/ ethylene bridge : Addition of ___ increase muscarinic selectivity; longer duration of action

methyl

SAR of Cholinergic agonists: INDIRECT Acting Prototype of Carbamate

Physostigmine

SAR of Cholinergic agonists: INDIRECT Acting Carbamate: Equivalent to the ____ (recognize by AChE but not easily hydrolyzed by the enzyme)

ester of acetylcholine

SAR of Cholinergic agonists: INDIRECT Acting Carbamate: has a ___ group

amino group

SAR of Cholinergic agonists: INDIRECT Acting Carbamate: has an amine group to prevent ____

hydrolysis

SAR of Cholinergic ANTAGONIST: _____ Prototype drug: Atropine Contains Tropane ring system

Amino Alcohols Esters SAR

SAR of Cholinergic ANTAGONIST: Amino Alcohols Esters SAR Prototype drug: ___ Contains Tropane ring system

Atropine

SAR of Cholinergic ANTAGONIST: Amino Alcohols Esters SAR Prototype drug: Atropine Contains _____system

Tropane ring

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine MOA: Increase ______________ of opening of GABA-gated Chloride Channel

SAR of Anxiolytics, Sedative, and Hypnotic agents __ C=O – is essential for the activity * Fused triazole or Imidazole ring at positions 1 and 2 – increases activity * Fused ring – Imidazole = Midazolam

Benzodiazepine

SAR of Anxiolytics, Sedative, and Hypnotic agents ____ MOA: Increase frequency of opening of GABA-gated Chloride Channel

Benzodiazepine

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine MOA: Increase frequency of opening of ____

GABA-gated Chloride Channel

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine MOA: Increase ______________ of opening of GABA-gated Chloride Channel

Frequency

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine ___ – is essential for the activity * Fused triazole or Imidazole ring at positions 1 and 2 – increases activity * Fused ring – Imidazole = Midazolam

C=O Carboxyl

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine C=O – is essential for the activity _____ or Imidazole ring at positions 1 and 2 – increases activity * Fused ring – Imidazole = Midazolam

* Fused triazole

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine C=O – is essential for the activity * Fused triazole or ____ at positions 1 and 2 – increases activity * Fused ring – Imidazole = Midazolam

Imidazole ring

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine C=O – is essential for the activity * Fused triazole or Imidazole ring at positions ____ – increases activity * Fused ring – Imidazole = Midazolam

1 and 2

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine C=O – is essential for the activity * Fused triazole or Imidazole ring at positions 1 and 2– _____ * Fused ring – Imidazole = Midazolam

increases activity

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine C=O – is essential for the activity * Fused triazole or Imidazole ring at positions 1 and 2– increases activity *______ – Imidazole = Midazolam

Fused ring

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine ______ substitution with EWG increases the activity= increases CNS Activity

X - Carbon7

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine X: substitution with EWG increases the activity= _______

increases CNS Activity

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= _____ group – increases the activity * Prime numbering in the aromatic ring indicates the possible attachment of substituents * 2’ or 2’ and 6’ – substitution with EWG will increase the drug activity * 4’ substitution – will decrease the activity

5-phenyl

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= 5-phenyl group – ___ * Prime numbering in the aromatic ring indicates the possible attachment of substituents * 2’ or 2’ and 6’ – substitution with EWG will increase the drug activity * 4’ substitution – will decrease the activity

increases the activity

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= 5-phenyl group – increases the activity * ______ numbering in the aromatic ring indicates the possible attachment of substituents * 2’ or 2’ and 6’ – substitution with EWG will increase the drug activity * 4’ substitution – will decrease the activity

Prime

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= 5-phenyl group – increases the activity * Prime numbering in the aromatic ring indicates the possible attachment of substituents *______ – substitution with EWG will increase the drug activity * 4’ substitution – will decrease the activity

2’ or 2’ and 6’

SAR of Anxiolytics, Sedative, and Hypnotic agents BenSAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= 5-phenyl group – increases the activity * Prime numbering in the aromatic ring indicates the possible attachment of substituents * 2’ or 2’ and 6’ – substitution with EWG will increase the drug activity *______ – will decrease the activityzodiazepine= 5-phenyl group – increases the activity

4’ substitution

SAR of Anxiolytics, Sedative, and Hypnotic agents Benzodiazepine= 5-phenyl group – increases the activity * Prime numbering in the aromatic ring indicates the possible attachment of substituents * 2’ or 2’ and 6’ – substitution with EWG will increase the drug activity * 4’ substitution – will ____ the activity

decrease

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates MOA: Increase duration of ____

opening of GABA-gated Chloride Channel

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates MOA: Increase _____________ of opening of GABA-gated Chloride Channel

duration

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates _______ * Increase lipophilicity * Quick Onset and Short DOA

R1 Alkyl substitution

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates R1 Alkyl substitution *___ * Quick Onset and Short DOA

Increase lipophilicity

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates R1 Alkyl substitution * Increase lipophilicity * Quick Onset and ___

Short DOA

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates ______ * Increase lipophilicity * Ultra-short acting effect

Replacing oxygen w/ sulfur

SAR of Anxiolytics, Sedative, and Hypnotic agents Barbiturates R5 Alkyl or Aryl (Aromatic ring) substitution * Increase ____

lipophilicity

SAR of antipsychotic and antidepressant drug Antipsychotic : _______ * Increases the potency

R2 EWG substitution

SAR of antipsychotic and antidepressant drug Antipsychotic : R2 EWG substitution * _____

Increases the potency

SAR of antipsychotic and antidepressant drug Antipsychotic : 3 degree Amine * ____ must have a N-containing side chain on the ring N and must be separated by at least 3C! * Essential for the activity

R-group

SAR of antipsychotic and antidepressant drug Antipsychotic : 3 degree Amine * R-group must have a ___ side chain on the ring N and must be separated by at least 3C! * Essential for the activity

N-containing

SAR of antipsychotic and antidepressant drug Antipsychotic : 3 degree Amine * R-group must have a N-containing side chain on the ring N and must be separated by at least ___ * Essential for the activity

3C!

SAR of antipsychotic and antidepressant drug Antipsychotic : 3 degree Amine * R-group must have a N-containing side chain on the ring N and must be separated by at least 3C! * ______

Essential for the activity

SAR of antipsychotic and antidepressant drug ______ SAR is somehow related to antipsychotic

Antidepressants:

SAR of antipsychotic and antidepressant drug Antipsychotic : Tertiary amine is essential for the activity of___, and ___

antihistamine and anticholinergic

SAR of antipsychotic and antidepressant drug _____ The ring side and side chain Nitrogen is separated by 3C

Antidepressants

SAR of antipsychotic and antidepressant drug ___ The Central Ring System makes the two aromatic rings “skewed” which is required for the activity

Antidepressants

Isolated from Papaver somniferum

SAR of Opiod Analgesic

What is the pharmacopore of SAR of Opiod Analgesic

aromatic ring Phenol tertiary amine

Opiod Analgesic SAR: It is the aromatic ring

Ring A

Opiod Analgesic SAR: ___ + 3-OH is the phenol

Ring A

Opiod Analgesic SAR: contains the tertiary amine

Ring D

Opiod Anlagesic: Addition of ___ to 3C will result to Codeine

Methyl

Opiod Anlagesic: Addition of methyl to 3C will result to _____

Codeine

Opiod Anlagesic: Addition of methyl to 3C will result to codeine Addition of either ___or ___ will decrease the activity

methyl

Opioid Analgesic SAR: ▪______ removal of a particular part of the molecule and observe its effect to the activity

Drug dissection:

Opioid Analgesic SAR: Drug dissection: removal of a 6-OH or Alkene at position 7 or 8= _____

Retained activity

Opioid Analgesic SAR: Drug dissection: removal of ring D= ____

Decreased activity

Opioid Analgesic SAR: Drug dissection: removal of ring E * retained activity * Will result to ___ such as Levorphanol which are more potent and longer acting than Morphine

morphinans

Opioid Analgesic SAR: Drug dissection: removal of ring E * _____ * Will result to morphinans such as Levorphanol which are more potent and longer acting than Morphine

Retained activity

Opioid Analgesic SAR: Drug dissection: ______ * Retained activity * Will result to morphinans such as Levorphanol which are more potent and longer acting than Morphine

removal of ring E

Opiod Analgesic: Drug dissection: removal of ring ___ * Retained activity * Will result to Benzomorphans such as Pentazocine

C and D also E

Opiod Analgesic: Drug dissection: removal of ring C and D * _____ * Will result to Benzomorphans such as Pentazocine

Retained activity

Opiod Analgesic: Drug dissection: removal of ring C and D * Retained activity * Will result to ___ such as Pentazocine

Benzomorphans

Opiod Analgesic: Drug dissection: removal of ring __, __, and __ * Retained activity * Will result to 4 phenylpiperidines such as Fentanyl (more flexible molecules)

B, C and E

Opiod Analgesic: Drug dissection: removal of ring C and D * Retained activity * Will result to Benzomorphans such as ___

Pentazocine

Opiod Analgesic: Drug dissection: removal of ring B, C and E * ___ * Will result to 4 phenylpiperidines such as Fentanyl (more flexible molecules)

Retained activity

Opiod Analgesic: Drug dissection: removal of ring B, C and E * Retained activity * Will result to 4 ___ such as Fentanyl (more flexible molecules)

phenylpiperidines

Opiod Analgesic: Drug dissection: removal of ring B, C and E * Retained activity * Will result to 4 phenylpiperidines such as __ (more flexible molecules)

Fentanyl

It is more potent than benzodiazepines

Barbiturates

it is 100x more potent than morphine

fentanyl

Pharmacopore of what Lipophilic ring that may be substituted * A linker (ester or amide) * Amine group that is usually tertiary amine

SAR of Local anesthetic:

SAR of Local anesthetic: What Functional group is the linker

A linker is an ester and amide

SAR of Local anesthetic: __ group that is usually tertiary amine

amine group

Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

Polyenes

this MOA: Binds with ergosterol and acts as false membrane component causing membrane disruption belongs to

Antifungal agents: Polyenes

Polyenes Contain a system of ___ in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

conjugated double bonds

Polyenes Contain a system of conjugated double bonds in ___. They differ from erythromycin in that they are larger and contain the conjugated –ene system of double bonds

macrocyclic lactone rings

Polyenes Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from _____ in that they are larger and contain the conjugated –ene system of double bonds

erythromycin

Polyenes Contain a system of conjugated double bonds in macrocyclic lactone rings. They differ from erythromycin in that they are larger and contain the ___ of double bonds

conjugated –ene system

Polyenes: 26-membered ring-polyenes: ___

natamycin

Polyenes: 38-membered ring-polyenes: ____, ____

nystatin, and amphotericin B

Polyenes: MOA: Binds with ___ and acts as false membrane component causing membrane disruption

ergosterol

Source of Amphotericin B

Streptomyces nodosus

Antifungal agents that is Indicated for the treatment of severe life-threatening infections; systemic mycoses

Amphotericin

amphotericin B is indicated for the txt of severe life-threatening infections; systemic mycoses

Amphotericin B

It is a antifungal agents that is Not absorbed systemically when given orally and is too toxic to be given parenterally. Hence, is administered topically

Nystatin

Source of nystatin is ___

Streptomyces noursei

Antifungal agents: Azole: Synthetic antifungal agents that can achieve ____ for the infecting fungus over host

selectivity

Polyenes is similar to ____ (Macrolides)

Erythromycin

Antifungal agents thatmust not br given IM

Amphotericin B

In griseofulvin, when there is increase in fats = ____ in absorption

increase

Antifungal agents MOA ofAllylamine and related compounds

MOA: Inhibits ergosterol synthesis via inhibiting squalene epoxidase.

aNTIFUNGAL AGENT that is not absorbed systematically weh given orally and is toxic ____

not absorbedsystematically - orally toxic - parenterally

Antifungal agents: Azole: ___ functionality confers high lipophilicity except Fluconazole

Non-polar

Antifungal agents: ___ Isolated from Penicillum griseofulvum

griseofulvin

Griseofulvin oral bioavailability is ____

poor

Antifungal agents: Used for ringworm infections

Griseofulvin

Antifungal agents: ______ MOA : Inhibits ergosterol synthesis via inhibiting squalene epoxidase

Allylamine and related compounds

wha is the MOA of griseofulvin

Mitotic spindle poison

Antifungal agents MOA: Mitotic spindle poison

Griseovulfin

Antifungal agents Example of Allylamine and related compounds

Examples: Naftiline, Terbinafine, Tolnaftate (not an allylamine)

Antifungal agents: ____ ▪ MOA: Inhibits lanosterol 14-a-demethylase * High Conc: Fungicidal * Low Conc: Fungistatic

Azole

Antifungal agents: Azole ▪ MOA: _____ * High Conc: Fungicidal * Low Conc: Fungistatic

Inhibits lanosterol 14-alpha demethylase

Antifungal agents: Azole ▪ MOA: Inhibits lanosterol 14-a-demethylase * High Conc: _____ * Low Conc: ____

Fungicidal Fungistatic

Antifungal agents: ______ ▪ MOA: Inhibits lanosterol 14-a-demethylase

Azole

Antifungal agents: ____Synthetic antifungal agents that can achieve selectivity for the infecting fungus over host

Azole

Antifungal agents: _____: Must contain weakly basic imidazole or triazole ring bonded by a nitrogen-carbon linkage to the rest of the structure

Azole

Antifungal agents: Azole: Must contain _______ or triazole ring bonded by a nitrogen-carbon linkage to the rest of the structure

weakly basic imidazole

Antifungal agents: Azole: The most potent antifungal azoles possess ____ with at least one of which is halogen substitute

two or three aromatic rings

Antifungal agents: Azole: Halogen atom that yields most potency is ____

fluorine

Antifungal agents: Azole: Non-polar functionality confers ___ except Fluconazole

high lipophilicity

Antifungal agents: Azole: Presumably, the large non polar portion of these molecules mimics the non-polar steroidal part of ___

lanosterol 14-a-demethylase

Antifungal agents: Azole: ▪ Substitution at other positions of the ring yields ____

inactive compounds.

Antifungal agents: Azole: Non-polar functionality confers high lipophilicity except ___

Fluconazole

Antifungal agents: Azole: Presumably, the large non polar portion of these molecules mimics the ___part of lanosterol 14-a-demethylase

non-polar steroidal

Azole SAR: Imidazole Examples

COMET-K Clotrimazole Oxiconazole Miconazole Econazole Tioconazole - Ketoconazole

Azole SAR: TRIAZOLE, Examples

FITVIP Fluconazole Itraconazole Terconazole Voriconazole Isavuconazole Posaconazole

Nucleoside Flucytosine MOA: Taken up by ___ and is converted to 5-fluorouracil which inhibits thymidylate synthase.

fungi

Nucleoside ____ MOA: Taken up by fungi and is converted to 5-fluorouracil which inhibits thymidylate synthase.

Flucytosine

It is an antifungal agent that is Taken with_____ to decrease its resistance.

Nucleoside Flucytosine MOA: Taken up by fungi and is converted to ____ which inhibits thymidylate synthase.

5-fluorouracil

Nucleoside ____ MOA: Taken up by fungi and is converted to 5-fluorouracil which inhibits ____

thymidylate synthase.

It is an antifungal agent that is Taken with_____ to decrease its resistance.

Amphotericin B

__ Generalities: Have one common structural features – a quinoline ring or a quinoline with an additional benzene added (an acridine ring)

Antimalarial agents

Antimalarial agents Generalities: Have one common structural features – a _____ring or a ____ with an additional benzene added (an acridine ring)

quinoline

Antimalarial agents Generalities: Have one common structural features – a quinoline ring or a quinoline with an additional ____ added (an acridine ring)

benzene

Used against the Plasmodium species

Antimalarial agents

Antimalarial agents: is used as____ species

Plasmodium species

Antimalarial agents Cinchona Alkaloid ______ Quinine’s spectrum of activity is considered to narrow for prophylactic use relative to the synthetic agents.

Quinine and Quinidine

Quinine and Quinidine of activity is considered to narrow for prophylactic use relative to the synthetic agents.

Quinine’s spectrum

Antimalarial agents Quinine and Quinidine Quinine’s spectrum of activity is considered to narrow for ____ relative to the synthetic agents.

prophylactic use

Antimalarial agents Cinchona Alkaloid: Is still indicated for malaria caused by ___ to other agents like chloroquine

P.falciparum resistant

Antimalarial agents Side effects of Cinchona Alkaloid

Cinchonism (nausea, vomiting, tinnitus, and vertigo)

Antimalarial agents Cinchona Alkaloid: Is still indicated for malaria caused by P.falciparum resistant to other agents lwhat is the ike____

chloroquine

What is the manifestation of Cinchonism

nausea, vomiting, tinnitus, and vertigo

antimalarial agents Are the closest of the anti-malarial that are based on the quinine structure.

4-aminoquinolines

Antimalarial agents This group is substituted at the same position 4 as quinine and have an asymmetric carbon equivalent to quinine’s C-9 position

4-aminoquinolines

Just as with quinine, both isomers are active and the 4-aminoquinoline racemic mixtures are used

4-aminoquinolines

considered the prototype of anti-malaria

Chloroquine & Chloroquine PO4

Antimalarial agents Chloroquine & Chloroquine PO4 considered the prototype of anti-malarial HCl- ____ PO4- ____

HCl – parenteral PO4 – oral

DOC for erythrocytic malaria; also used in SLE and RA

4-aminoquinolines

4-aminoquinolines is a DOC for ___, ___, and ____.

DOC for erythrocytic malaria; also used in SLE and RA

____ – the only drug effective against the exoerythrocytic stages of malaria

Primaquine: antimalarial agents

Primaquine: the only drug effective against the ____ stages of malaria

exoerythrocytic

What should be watch out for (WOF) 8-aminoquinolines

WOF: hemolytic anemia – G6PD px

G6PD stands for

Glucose 6 phosphate deficiency

what should be watch out for (WOF) 4-aminoquinolines

▪ WOF: QT Prolongation- affects the heart

Antimalarial agents: Polycyclic Drugs ___ – newest of the anti-malarial drug from the natural source of Artemisia annua

Artemisinin

Antimalarial agents: Polycyclic Drugs Artemisinin – newest of the anti-malarial drug from the natural source of ____

Artemisia annua

Used in DMARD (Demodifying anti-rheumatic drug) and also anti-malarial drug

Hydroxychloroquine

BEQ: What drug has Gemtocidal activity (Vs Vivax, Ovale, Malariae)

Quinine Choloquine

BEQ: drugs that have an activity to Gametocidal (vs. all plasmodium spp.)

Primaquine, Artremisinin

BEQ: drugs that have an activity to tissues schizonticide

Primaquine

BEQ: drugs that have an activity as radical cure

Primaquine

BEQ: drugs that have an activity as prevention of relapse

Primaquine

Module 1.4: Medicinal Chemistry Flashcards

Oraganic Medicinal Chemistry