In the design of H2 antagonist, the polar guanidine group was proposed to interact with the antagonist binding region by two hydrogen bonds. Compound A is designed based on modification of compound B and has higher antagonist activity compared to compound B. H2N NH NH2 NH HN Guanidine Guanidine HN What drug design strategy has been used here? O Rigidification O Simplification O Substituent variation O Chain Extension

In the design of H2 antagonist, the polar guanidine group was proposed to interact with the antagonist binding region by two hydrogen bonds. Compound A is designed based on modification of compound B and has higher antagonist activity compared to compound B. H2N NH NH2 NH HN Guanidine Guanidine HN What drug design strategy has been used here? O Rigidification O Simplification O Substituent variation O Chain Extension

Organic Chemistry

8th Edition

ISBN:9781305580350

Author:William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Publisher:William H. Brown, Brent L. Iverson, Eric Anslyn, Christopher S. Foote

Chapter22: Reactions Of Benzene And Its Derivatives

Section: Chapter Questions

Problem 22.53P

See similar textbooks

Similar questions

Which one of the following sentences, regarding the compounds shown below, is incorrect? CI HO Compound I Compound II O Piperazine nitrogens, in compound II, have different pKa values O The binding affinity of compound I to H' receptor is stronger than that of compound I O Compound can form intramolecular ionic interactions, in blood pH, while compound II does not O The major form of compound I, at gastric pH, is a monocation O Compound I is selective to H' receptor while compound II is selective to H? receptor
A drug which has high affinity for muscarinic receptors not nicotinic receptors and is an antagonist not an agonist: Norepinephrine (LEVOPHED) O Atracurium (TRACURIUM) Echothiophate (PHOSPHOLINE) Ipratropium (ATROVENT) Norepinephrine (LEVOPHED) nint)
Drugs called COX-2 inhibitors (e.g., Vioxx, Bextra, andCelebrex) were thought to relieve the pain and inflammation ofosteoarthritis without the stomach bleeding and ulcers non-steroidal anti-inflammatory drugs (NSAIDs) cause. In a 12-month trial, Vioxx caused fewer gastrointestinal side effectsthan the NSAID ibuprofen. However, a study of the recurrenceof colon polyps after three years of Vioxx found an increasedrisk for heart attack and stroke beginning after 18 months oftreatment. As a result, Vioxx was withdrawn from the market,and an FDA panel concluded that COX-2 inhibitors as a classhave increased cardiovascular risk that varies by drug anddose. The FDA then caused the withdrawal of Bextra and re-quired a warning label on Celebrex. Based on this information,list (a) an observation, (b) a hypothesis, (c) an experiment, and(d) a theory.
(4 pts) a) a) Name these compounds Amines w HCI H₂N none properly: bon 29e soluble HCO, Na b) pts) Which of the following would give a positive coe b) acetone d) cyclopentanone H₂C CH3 aqu NH CH3 datioase term is use phenyl an efter b) basic hydrolysis of an ester nide For each of the above label it as a 1° 2° or 3º ami
) The potency of antagonists is frequently defined in terms of either their IC50, ortheir Ki. Explain what these two terms mean.
† 14.) A reversible inhibitor that is unable to bind to the ES complex A) always binds in the active site D) is always a noncompetitive inhibitor B) may be an uncompetitive inhibitor E) results in a decreased Kmapp C) results in an increased Vmax PP F) results in an unaltered Vmax pp † 15.) On a Lineweaver-Burk plot, a changing y-intercept upon addition of increasing concentration of inhibitor means C) the slope is increasing F) the Vmax PP is unchanged A) the inhibitor can bind to the free enzyme D) the inhibitor can bind to the ES complex B) the KmaPP is decreasing E) the Km PP is unchanged app 16.) Vn represents the rate of reaction for an enzyme-substrate pairing under what conditions? A) when [S] = ∞ E) for all [S]> Km max B) when [S] = Km F) for all [S] Km
Several compounds have been found to inhibit -lactamase, and drugs based on these compounds can be taken in combination with penicillins and cephalosporins to restore their effectiveness when resistance is known to be a problem. The commonly prescribed formulation called Augmentin is a combination of the -lactamase inhibitor shown below with amoxicillin (shown above). It is used to treat childhood ear infections when resistance is suspected, and many kids know it as the white liquid that tastes like bananas. Which of the statements below are true statements? 1. The stereochemistry of the fusion between the four-and five-membered rings in the inhibitor and amoxicillin are different. 2. The inhibitor possesses enol ether and allylic alcohol functional groups while the antibiotic possesses a phenol and a secondary amide functional group. 3. Neither the inhibitor nor the antibiotic contains strained rings. 4. Both 1 and 2 are true.
AvapH dT T(V, – Vi) dP AvapH _ AvapH _ AvapH TV -P RT2 RT AvapH For a change of state, ApapS Tvap P Deduce the relationship between In- and AvapH, AvapS, and T.
Which of the following systems has been associated to the Salvinorin-A's mechanism of action? Glutamate Serotonin Opioid GABA
Suggest all the possible interactions that metoclopramide can interact with in physiological pH. CI N. H. H2N O.
X 10 (select) v molecules of penicillin
If the EC50 of an agonist is 3 x 10-7 mol/L and the presence of antagonist changes this EC50 to 3 x 10-6 mol/L where the Emax stays unaffected. Pertaining to the agonist - antagonist interaction, which of the following statement(s) do you think are correct? Group of answer choices A.competitive reversible; log (rA-1) = 0.95 B.competitive irreversible; log (rA-1) = 0.95 C.non-competitive irreversible; log (rA-1) = 0.95 D.competitive reversible; log (rA-1) = 10 E.competitive reversible; log (rA-1) = 9.5