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PMY2106 > Drug Classes According To Pharmacophore > Flashcards

Drug Classes According To Pharmacophore Flashcards

1
Q

mechanisms of antibacterial agents

A
  • inhibiting cell metabolism
  • inhibiting cell wall synthesis
  • interacting with plasma membrane
  • disrupting protein synthesis
  • inhibition of nucleic acid transport and replication
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2
Q

drug class that inhibits cell metabolism

A

sulfanilamide

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3
Q

sulfanilamide SAR (structure, activity relation)

A
  • para amino group essential
  • aromatic and sulfonamide essential
  • aromatic ring must have para substitutions
  • sulfonamide nitrogen must be primary or secondary
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4
Q

fanisdar

A

combination of sulfadoxine and pyrimethamine

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5
Q

fanisdar MOA

A
  • blocks synthesis of tetrahydrofolate
  • which is an enzyme cofactor that provides one carbon units for synthesis of pyrimidine nucleic acid bases
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6
Q

fanisdar conditions to treat

A
  • malaria
  • uti’s
  • gut infections
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7
Q

drug class that inhibits cell wall synthesis

A

penicillins

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8
Q

penicillin SAR

A
  • beta-lactam essential
  • free COOH essential
  • bicyclic system important
  • acylamino side chain essential
  • sulfur usual but not essential
  • cis stereochemistry important with respect to acylamino side chain (bold wedge)
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9
Q

drug class that interacts with plasma membrane

A

ion-conducting antibiotics

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10
Q

examples of ion-conducting antibiotics

A

vancomycin, gramicidin A and polymyxin B

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11
Q

SAR of ion-conducting antibiotics

A
  • they are massive structures
  • active for G- bacteria
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12
Q

drug class that disrupts protein synthesis

A
  • aminoglycosides
  • tetracyclines
  • macrolides
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13
Q

drug class that inhibits nucleic acid transportation and replication

A
  • quinolones
  • fluoroquinolones
  • work by stabilising complex formed between DNA and topoisomerases
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14
Q

SAR of quinolones

A
  • bicyclic ring
  • pyridine
  • piperazinyl ring at position 7 beneficial
  • cyclopropyl substituent at position 1 increased broad spectrum activity
  • replacement of nitrogen at position 8 reduced adverse reactions
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15
Q

drugs that inhibit transcription phase (antiviral agents)

A
  • Efavirenz
  • Didanosine
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16
Q

drug that inhibits post transcription phase (antiviral agents)

A

idinavir

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17
Q

idinavir

A
  • relatively larger molecule
  • no weird representations
  • not as massive as vancomycin
18
Q

drugs that are ion channel disruptors (antiviral agent)

A
  • adamantanes
  • look like a little hat
  • contain NH3+ Cl-
19
Q

inhibitors of neuraminidase (antiviral agent)

A
  • zanamivir
  • tamiflu
  • both transition state inhibitors
20
Q

antidiabetic agents

A
  • insulinotropic agents
  • insulin-sensitising agents
21
Q

insulinotropic agents

A
  • sulfonylureas
  • act by closing membrane bound ATP sensitive potassium channels
22
Q

SAR of sulfonylureas

A
  • Sulfur atom double bonded to two oxygens
23
Q

insulin-sensitising agents

A
  • biguanides
  • thiazolidinediones
24
Q

SAR of biguanides

A
  • has a double bonded NH side chain
25
Q

common features in thiazolidinedione agonists

A
  • pentagon structure with NH and S and two double bonded oxygens
  • PPARy agonists
  • treat diabetes by lowering serum glucose without increasing insulin secretion
26
Q

PPARy

A
  • nuclear receptor
  • regulates fatty acid storage and glucose metabolism
27
Q

alpha-glucosidase inhibitors

A
  • numerous benzene rings attached to each other with lots of phenol groups
  • delays digestion of dietary carbohydrate in the form of starch and sucrose into monosaccharides
  • delaying absorption lowers blood glucose
28
Q

classes of antineoplastics (anti-tumor)

A
  • alkylating agents
  • antimetabolites (acting on enzymes
  • inhibitors of signaling pathways
  • antimitotics
  • topoisomerase II inhibitors
29
Q

central nervous system agents

A

opioids

30
Q

SAR of opioids

A
  • 3 benzene rings
  • alkene or 6-hydroy groups not essential
  • phenol group is important
  • tertiary amine is important
31
Q

point to consider with opioids

A

analgesic activity not only related to presence of important function groups, but to their relative position with respect to each other

32
Q

psychoactive drugs (hypnotics)

A
  • benzodiazepines
  • enhance effect of GABA at GABAa receptor, resulting in sedative, hypnotic, anxilytic, anticonvulsant and muscle relaxant properties
33
Q

SAR of benzodiazepines

A
  • benzene ring and 7-member diazepine ring
  • activity decreased with substitutions on nitrogen larger than methyl
  • activity decreased by substituents at benzene ring positions other that C7
  • activity increased by electron withdrawing groups on C7
34
Q

another psychoactive drug (hypnotics)

A
  • barbiturates
35
Q

SAR of barbiturates

A
  • benzene ring with nitrogen substitutions in meta-substitution
  • double bonded oxygens in ortho position
  • hypnotic activity increases with lipid solubility until number of C atoms at both C-5 substituents is between 6 and 10
  • unsaturated alkyl, alkenyl and alkynyl derivatives more hypnotic than saturated analogues
  • polar substituents at position 5 decreases lipid solubility and potency
  • replacement of oxygen at C-2 by sulfur results in faster onset but shorter duration of activity
36
Q

drugs of alzheimers

A
  • neostigmine
  • donepezil
  • rivastigmine
  • galantamine
37
Q

SAR of alzheimer’s drugs

A
  • benzene ring attached to ester group
  • ester attached to Me2N
38
Q

SAR of drugs for parkinson’s disease

A
  • based on L-DOPA, the precursor to dopamine, NA and A
  • single benzene ring with two phenol groups at the meta and para positions
  • R in dopamine = Me2NH2
  • R in NA = CH(OH)CH2NH2
  • R in A = CH(OH)CH2NHCH3
39
Q

respiratory agents

A
  • based on ephedrine
  • salbutamol and salmeterol
40
Q

SAR of respiratory agents

A
  • N-alkyl substitution increases potency for beta-adrenergic receptor
  • phenol group important
  • alpha-methyl substitution increases potency for alpha-adrenergic receptor
  • salbutamol has a hydroxymethylene group on meta position
  • salmeterol is simply a longer molecule
41
Q

why does salmeterol have a long duration of action compared to salbutamol?

A

because it is more lipophilic, so it can cross the BBB more easily

PMY2106 (15 decks)

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