Medicinal Chemistry

polar substituent groups to influence drug solubility and absorption can be manipulated under such circumstances to reduce the l ...

prion protein is predominantly in an α-helical conformation, it is nontoxic; when it is predominantly in a β-sheet conformation, ...

Viruses can exist and reproduce only as extreme cellular parasites because they do not possess a complete synthetic machinery fo ...

549 Table 9.1 Viruses Causing Disease in Humans Family agent Disease DNA viruses Adenovirus Human adenovirus Upper respiratory t ...

effective drugs for the treatment of human immunodeficiency virus. The dawning of the 21st century has brought new concerns abou ...

Assembly of new virus particles from nucleic acids and proteins (from steps 4 and 5) (blocked by rifampin (9.4)) Release and ex ...

the lip, keratitis of the cornea, and encephalitis. Its analog, Ara-C (9.6, cytarabine), is primarily an antineoplastic drug, bu ...

it is a viral DNA polymerase inhibitor but does not readily block the polymerase of the host cell. Therefore, acyclovir is a spe ...

antisense mechanism. It binds to target mRNA, resulting in inhibition of early protein synthesis within the virus-infected cell. ...

polymerase activities. The NNRTIs include nevirapine (9.22), delavirdine (9.23), and efavirenz (9.24). The third and most recent ...

9.3.3 Antivirals Targeting Other Mechanisms Amantadine (9.1, 1-aminoadamantane) and related compounds (e.g., rimantadine (9.30)) ...

EXOGENOUS PATHOGENS AND TOXINS 557 Zanamivir (9.31) and oseltamivir (9.32) are neuraminidase inhibitors. Neuraminidase is an ess ...

558 MEDICINAL CHEMISTRY Figure 9.2 Synthesis of Peramivir. The starting material, (−)-lactam, 1 , underwent hydroly- sis with me ...

cells against viral infection by altering the plasma membrane (i.e., in a nonspecific manner). It also activates an endonuclease ...

Gram-negative small rods (respiratory infections: pneumonia, whooping cough) Hemophilus influenzae Bordetella pertussis Gram-po ...

Bacterial cell wall targets Penicillins (bactericidal; inhibit cell wall crosslinking) e.g., benzylpenicillin, phenoyxmethylpen ...

Bacterial nucleic acid synthesis Sulfonamides (bacteriostatic; inhibit bacterial folic acid synthesis) Trimethoprim (bacteriost ...

563 Table 9.2 Sensitivities of Some Organisms to Commonly Used Antibiotics Drug 1234567891 01112131415161718 192021 Ampicillin/A ...

such as the penicillins and cephalosporins, after the bacterium has expended considerable biosynthetic energy. In contrast to th ...

The penicillins are produced by the molds Penicillium notatumandP. chrysogenum. Through the use of different culture media or bi ...