Since the discovery of penicillin by Fleming in 19291), antimicrobials have been widely applied for clinical use. The number of those who die from microbial infection, which was the greatest threat to human beings, has significantly decreased and average life expectancy has been largely extended.
Antimicrobials are chemical substances inhibiting growth of microorganisms and generally classified into antibiotics, synthetic antimicrobials, antivirals and antifungals. Antibiotics are antibacterial compounds produced by microorganisms and structurally classified into the amino glycosides, the macrolides, the β-lactams, etc. Moreover, synthetic analogs of their partial chemical modifications are also broadly called antibiotics. On the other hand, synthetic antimicrobials with the same antibacterial effect, as exemplified by quinolones2) and sulfonamides, have been developed through purely organic synthetic means. Antifungals, such as butenafine hydrochloride3), are employed to inhibit the growth of fungals which are eukaryotes. Antivirals are mainly composed of modified nucleosides such as azidothymidine4) and inhibit the virus forming cycle in host-cells. Antivirals are employed to inhibit the formation of viruses, which do not have their own cells.
Antitumors act by inhibiting the growth of tumor cells. Compounds such as camptothecin5) take effect on the DNA composition of the tumor cells and their activities. It is recently reported that 5’-azacytidine6) and trichostatin A7) improved the efficiency of pluripotent stem (iPS) cell generation.8) There are some such as geldanamycin9) which have both antibacterial activity and antitumor activity.
Due to the discovery and invention of antimicrobials bacterial infections have significantly decreased. However, nosocomial infections by multiple-drug-resistant bacteria, such as methicillin resistant Staphylococcus aureus (MRSA), pose a new problem and creation of new antibacterial drugs is called for. Antimicrobials for research and development have been getting more attention, not only for comparative studies, but also as chemical synthetic starting compounds.
Antibiotics for Research & Experimental Use
Synthetic Antimicrobials for Research & Experimental Use
Antifungals for Research & Experimental Use
Antivirals for Research & Experimental Use
Antitumors for Research & Experimental Use
Antibiotics for Research & Experimental Use
β-Lactams
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Aminoglycosides
|
|
|
|
|
|
|
| F0649 | Fradiomycin Sulfate |
| G0349 | G418 Disulfate |
| K0047 | Kanamycin Monosulfate |
| S0585 | Streptomycin Sulfate |
| S0834 | Streptomycin Sulfate [for Protein Research] |
| T2503 | Tobramycin |
Macrolides
|
|
|
|
|
|
| A2076 | Azithromycin Dihydrate |
| C2220 | Clarithromycin |
| E0751 | Erythromycin |
| K0046 | Leucomycins |
| S0575 | Spiramycin |
Others
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Synthetic Antimicrobials for Research & Experimental Use
Quinolones
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Sulfonamides
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Antifungals for Research & Experimental Use
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Antivirals for Research & Experimental Use
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
|
Antitumors for Research & Experimental Use
Literature
2) Quinolone generations: P. Ball, J. Antimicrob. Chemother. 2000, 46, 17.
3) Antifungal activity in vivo: T. Arika, M. Yokoo, T. Hase, T. Maeda, K. Amemiya, H. Yamaguchi, Antimicrob. Agents Chemother. 1990, 34, 2250.
4) a) vs HIV-1 virus: H. Mitsuya, K. J. Weinhold, P. A. Furman, M. H. St. Clair, S. N. Lehrman, R. C. Gallo, D. Bolognesi, D. W. Barry, S. Broder, Proc. Natl. Acad. Sci. USA 1985, 82, 7096.
b) Sugar-modified nucleoside syntheses review: E. Ichikawa, K. Kato, Curr. Med. Chem. 2001, 8, 385.
5) Review: M. E. Wall, M. C. Wani, Cancer Res. 1995, 55, 753.
6) a) Inducing transgene silencing by DNA methylation: L. Broday, Y.-W. Lee, M. Costa, Mol. Cell. Biol. 1999, 19, 3198.
b) Chemical synthesis: M. W. Winkley, R. K. Robins, J. Org. Chem. 1970, 35, 491 [DOI].
7) a) Structure elucidation: N. Tsuji, M. Kobayashi, K. Nagashima, Y. Wakisaka, K. Koizumi, J. Antibiot. 1976, 29, 1.
b) Chemical synthesis: K. Mori, K. Koseki, Tetrahedron 1988, 44, 6013 [DOI].
8) D. Huangfu, R. Maehr, W. Guo, A. Eijkelenboom, M. Snitow, A. E. Chen, D. A. Melton, Nat. Biotechnol. 2008, 26, 795 [DOI].
9) Evaluation as an antitumor agent: J. G. Supko, R. L. Hickman, M. R. Grever, L. Malspeis, Cancer Chemother. Pharmacol. 1995, 36, 305 [DOI].
90ac4m0000003a5o





