Antimicrobials & Antitumors for Research and Experimental Use

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

A0800 A0800 A1266 A1266 A2075 A2075
A2099 A2099 A2092 A2092 C2242 C2242
C2224 C2224 C2225 C2225 C2226 C2226
C2248 C2248 C2244 C2244 O0353 O0353
P1772 P1772 P1770 P1770 P1774 P1774
A0800 6-Aminopenicillanic Acid
A1266 7-Aminocephalosporanic Acid
A2075 7-Aminodesacetoxycephalosporanic Acid
A2099 Amoxicillin Trihydrate
A2092 Ampicillin Trihydrate
C2242 Cefazolin Sodium Salt
C2224 Cefotaxime Sodium Salt
C2225 Ceftazidime (contains ca. 10% Na2CO3)
C2226 Ceftriaxone Disodium Salt Hemiheptahydrate
C2248 Cephalexin Monohydrate
C2244 Cloxacillin Sodium Salt Monohydrate
O0353 Oxacillin Sodium Salt Monohydrate
P1772 Penicillin G Potassium Salt
P1770 Penicillin G Sodium Salt
P1774 Piperacillin Sodium Salt

Aminoglycosides

G0349 G0349 K0047 K0047 S0585 S0585
S0834 S0834 T2503 T2503
F0649 Fradiomycin Sulfate
G0349 G418 Disulfate
K0047 Kanamycin Monosulfate
S0585 Streptomycin Sulfate
S0834 Streptomycin Sulfate [for Protein Research]
T2503 Tobramycin

Macrolides

A2076 A2076 C2220 C2220 E0751 E0751
S0575 S0575
A2076 Azithromycin Dihydrate
C2220 Clarithromycin
E0751 Erythromycin
K0046 Leucomycins
S0575 Spiramycin

Others

A2190 A2190 A2118 A2118 A2191 A2191
C2255 C2255 C2256 C2256 C2257 C2257
C2408 C2408 D3793 D3793 F0811 F0811
G0334 G0334 H1306 H1306 L0166 L0166
Q0056 Q0056 Q0028 Q0028 R0079 R0079
T2525 T2525 T2802 T2802
A2190 Artemether
A2118 Artemisinin
A2191 Artesunate
C2255 Chloramphenicol
C2256 Clindamycin Hydrochloride Monohydrate
C2257 Clindamycin Phosphate
C2408 Cyclosporin A
D3793 Dihydroartemisinin
F0811 Florfenicol
G0334 Geldanamycin
H1306 Hydroxychloroquine Sulfate
L0166 Lincomycin Hydrochloride Monohydrate
P1923 Polymyxin B Sulfate
Q0056 Quinacrine Dihydrochloride Hydrate
Q0028 Quinine
R0079 Rifampicin
T2525 Tetracycline Hydrochloride
T2802 Thiamphenicol

Synthetic Antimicrobials for Research & Experimental Use

Quinolones

C2293 C2293 C2227 C2227 E0762 E0762
E0786 E0786 F0646 F0646 L0193 L0193
L0216 L0216 M2240 M2240 N0490 N0490
N0817 N0817 P1962 P1962 P1773 P1773
T2506 T2506
C2293 7-Chloro-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic Acid
C2227 Ciprofloxacin Hydrochloride Monohydrate
E0762 Enoxacin Sesquihydrate
E0786 Enrofloxacin
F0646 Fleroxacin
L0193 Levofloxacin
L0216 Lomefloxacin Hydrochloride
M2240 Marbofloxacin
N0490 Nalidixic Acid
N0817 Norfloxacin
P1962 Pazufloxacin Mesylate
P1773 Pipemidic Acid Trihydrate
T2506 Tosufloxacin p-Toluenesulfonate Hydrate

Sulfonamides

S0595 S0595 S0581 S0581 S0582 S0582
S0577 S0577 S0578 S0578 S0579 S0579
S0359 S0359 S0589 S0589 S0464 S0464
S0586 S0586 S0583 S0583 S0360 S0360
S0361 S0361 S0591 S0591 S0592 S0592
S0119 S0119 S0381 S0381 S0833 S0833
S0071 S0071 S0580 S0580 S0272 S0272
S0362 S0362
S0595 Silver Sulfadiazine
S0581 Succinylsulfathiazole Hydrate
S0582 Sulfabenzamide
S0577 Sulfacetamide
S0578 Sulfacetamide Sodium Salt Hydrate
S0579 Sulfadiazine
S0359 Sulfadimethoxine
S0589 Sulfadimethoxine Sodium Salt
S0464 Sulfaguanidine
S0586 Sulfamethazine
S0583 Sulfamethazine Sodium Salt
S0360 Sulfamethizole
S0361 Sulfamethoxazole
S0591 Sulfamethoxypyridazine
S0592 Sulfamonomethoxine
S0119 Sulfanilamide
S0381 Sulfanilamide [for Diazotization Titration]
S0833 Sulfanilamide [for Biochemical Research]
S0071 Sulfapyridine
S0580 Sulfasalazine
S0272 Sulfathiazole
S0362 Sulfisomidine

Antifungals for Research & Experimental Use

A2161 A2161 B3293 B3293 C2025 C2025
D2049 D2049 F0677 F0677 F0321 F0321
I0666 I0666 I0732 I0732 K0045 K0045
M1769 M1769 T2722 T2722
A2161 Amorolfine Hydrochloride
B3293 Butenafine Hydrochloride
C2025 Climbazole
D2049 trans-N-(6,6-Dimethyl-2-hepten-4-ynyl)-N-methyl-1-naphthylmethylamine Hydrochloride
F0677 Fluconazole
F0321 5-Fluorocytosine
I0666 3-Iodo-2-propynyl N-Butylcarbamate
I0732 Itraconazole
K0045 Ketoconazole
M1769 Miconazole Nitrate
T2722 2-(1H-1,2,4-Triazol-1-yl)-2',4'-difluoroacetophenone

Antivirals for Research & Experimental Use

A1915 A1915 A2414 A2414 A2052 A2052
B3404 B3404 C2035 C2035 D3580 D3580
D3065 D3065 D3581 D3581 D3066 D3066
D0964 D0964 I0747 I0747 I0037 I0037
I0258 I0258 L0217 L0217 R0077 R0077
T2511 T2511 V0111 V0111 V0110 V0110
V0098 V0098
A1915 Acyclovir
A2414 Adefovir Dipivoxil
A2052 3'-Azido-3'-deoxythymidine
B3404 (E)-5-(2-Bromovinyl)-2'-deoxyuridine
C2035 Cytarabine
D3580 2',3'-Didehydro-3'-deoxythymidine
D3065 2',3'-Dideoxyadenosine
D3581 2',3'-Dideoxycytidine
D3066 2',3'-Dideoxyinosine
D0964 1-Docosanol
I0747 Imiquimod
I0037 Inosine
I0258 5-Iodo-2'-deoxyuridine
L0217 Lamivudine
R0077 Ribavirin
T2511 Trifluorothymidine
V0111 Valacyclovir Hydrochloride Hydrate
V0110 Venlafaxine Hydrochloride
V0098 Vidarabine Monohydrate

Antitumors for Research & Experimental Use

A0907 A0907 A2063 A2063 A1947 A1947
A2033 A2033 B1022 B1022 C2235 C2235
C1495 C1495 C2043 C2043 C2236 C2236
D3634 D3634 D3579 D3579 D1961 D1961
D3371 D3371 E0781 E0781 E0748 E0748
E0675 E0675 F0635 F0635 F0151 F0151
F0663 F0663 G0334 G0334 G0367 G0367
C2243 C2243 H1309 H1309 H0310 H0310
I0747 I0747 I0714 I0714 K0045 K0045
M1964 M1964 M1949 M1949 M0063 M0063
M1664 M1664 N0821 N0821 N0822 N0822
O0372 O0372 P1632 P1632 P1905 P1905
P0637 P0637 P1276 P1276 R0064 R0064
M0913 M0913 T2510 T2510 T2744 T2744
T0212 T0212 T2477 T2477 V0098 V0098
A0907 Allopurinol
A2063 9-Aminocamptothecin
A1947 DL-Aminoglutethimide
A2033 5-Azacytidine
B1022 1,4-Butanediol Dimethanesulfonate
C2235 Calcium Folinate Hydrate
C1495 (S)-(+)-Camptothecin
C2043 Carboplatin
C2236 Cyclophosphamide Monohydrate
D3634 Dacarbazine
D3579 5'-Deoxy-5-fluorouridine
D1961 Dexamethasone
D3371 cis-Diammineplatinum(II) Dichloride
E0781 7-Ethylcamptothecin
E0748 7-Ethyl-10-hydroxycamptothecin
E0675 Etoposide
F0635 5-Fluoro-1-(tetrahydro-2-furfuryl)uracil
F0151 5-Fluorouracil
F0663 Flutamide
G0334 Geldanamycin
G0367 Gemcitabine Hydrochloride
C2243 Gimeracil
H1309 Honokiol
H0310 Hydroxyurea
I0747 Imiquimod
I0714 Irinotecan Hydrochloride Trihydrate
K0045 Ketoconazole
M1964 Medroxyprogesterone Acetate
M1949 Megestrol Acetate
M0063 6-Mercaptopurine Monohydrate
M1664 Methotrexate Hydrate
N0821 Nimustine Hydrochloride
N0822 9-Nitrocamptothecin
O0372 Oxaliplatin
P1632 Paclitaxel
P1905 Piroxicam
P0637 Prednisolone
P1276 Prednisone
R0064 Retinoic Acid
M0913 Sodium 2-Mercaptoethanesulfonate
T2510 Tamoxifen Citrate
T2744 Temozolomide
T0212 6-Thioguanine
T2477 Trichostatin A
V0098 Vidarabine Monohydrate

Literature

1) A. Fleming, Br. J. Exp. Pathol. 1929, 10, 226.
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].


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