Medicinal Chemistry

Penicillins and Mechanisms of Bacterial Resistance. The most serious threat to antibiotic therapy, and to the use of β-lactam an ...

It is formed by acylases that cleave off the side chain of the penicillins, and can also be obtained by the selective chemical c ...

Since cephalosporin C is only one-thousandth as active as benzylpenicillin, its use is very limited. However, it is remarkably r ...

it is very unstable and therefore unlikely to be of use in its native form. The N-formimidyl derivative overcomes this problem. ...

to the other, releasing the ion on the other side. A channel former simply provides a polar tunnel that allows the migration of ...

Many hypotheses explaining the channel formation induced by gramicidin A have been put forth over the years. For example, two mo ...

soaps. Moreover, since fentichlor has a low oral toxicity, it can be used internally for skin infections. Inhibition of the meta ...

9.4.3.1 Antibacterials Targeting the Ribosomal 30S Subunit: Tetracyclines The tetracyclines are closely related to the anthracyc ...

9.4.3.2 Antibacterials Targeting the Ribosomal 30S Subunit: Aminoglycosides Clinically useful aminoglycosides contain a highly s ...

tobramycin (9.79), and netilmycin (9.80). Amikacin (9.81), a semi-synthetic analog of kanamycin, has also been used clinically. ...

antibiotic, but because it can cause fatal blood dyscrasias(i.e., bone marrow suppression and failure) its use is largely restri ...

isolated from Streptomyces lincolnensis. Lincomycin (9.87) is the prototype compound in this class. It consists of a pyrrolidine ...

deep cleft across the enzyme, and about a dozen amino acids are involved in binding substrate or inhibitor. The biochemical role ...

enzymes releases the active free sulfanilamide. Succinyl-sulfathiazole was therefore widely used for intestinal infections. The ...

Correlations between physicochemical parameters and the antibacterial activity of sulfa drugs have been explored for a long time ...

The fluoroquinolones represent an important therapeutic advance and are extremely useful agents. They are important for the trea ...

[tinea capitis], nails [tinea unguium; Microsporum canis, Trichophyton mentagrophytes]), subcutaneous (abscess in muscle or even ...

agents that interact with sterols in the microbial plasma membrane. From five to ten molecules of these antifungals form a condu ...

Morpholines such as tridemorph (9.112) attack sterol biosynthesis via ∆^14 -reductase enzyme inhibition and are valuable agricul ...

EXOGENOUS PATHOGENS AND TOXINS 585 c. Sporozoa Plasmodium(causing malaria—high fever, sweating, headache, nausea) d. Ciliophora ...