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Journal of Natural Products Review Small-Mole Source S/NM S*S*/NM 10 1987 1987 N 33 19 304 55 32 HN- 192 326 2000 1986 112543 in T le 7.small molecules a lafungin (ND;11),a structure.As is the case with a significant number of compounds Table 6.All Anti-infective (Bacterial,Fungal,Parasitic,and Viral)Drugs (n=270) S/NM S*/NM 9490 293 dag/n0,1021/ 11ed2012.75.311-35sitafloxacin from Daiichi (9) in 2008, and besifloxacin (10) from Bausch and Lomb in 2009. Overall, in the antibacterial area, as shown in Table 7, small molecules account for 104 agents, with “N” and “ND” compounds accounting for just under 75% of the approved agents. In the antifungal area, only one drug was approved in the 2006 to 2010 time frame. This was the echinocandin derivative anidulafungin (ND; 11), approved for use in the U.S. in early 2006, and was covered in the 2007 review but without a structure. As is the case with a significant number of compounds, the final company was not the originator. This molecule was first synthesized by Lilly under the code number LY-303366, then Table 5. Antiparasitic Drugs from 01/01/1981 to 12/01/ 2010 Organized Alphabetically by Generic Name within Source generic name trade name year introduced volume page source artemisinin Artemisin 1987 ARMC 23 327 N ivermectin Mectizan 1987 ARMC 23 336 N arteether Artemotil 2000 DNP 14 22 ND artemether Artemetheri 1987 I 90712 ND artesunate Arinate 1987 I 91299 ND eflornithine HCl Ornidyl 1990 DNP 04 104 ND mefloquine HCI Fansimef 1985 ARMC 21 329 ND albendazole Eskazole 1982 I 129625 S halofantrine Halfan 1988 ARMC 24 304 S lumefantrine ? 1987 I 269095 S quinfamide Amenox 1984 ARMC 20 322 S atovaquone Mepron 1992 ARMC 28 326 S* bulaquine/ chloroquine Aablaquin 2000 DNP 14 22 S* trichomonas vaccine Gynatren 1986 I 125543 V Table 6. All Anti-infective (Bacterial, Fungal, Parasitic, and Viral) Drugs (n = 270) indication total B N ND S S/NM S* S*/NM V antibacterial 118 10 67 26 1 14 antifungal 29 1 3 22 3 antiparasitic 14 2 5 4 2 1 antiviral 109 14 4 9 2 23 10 47 total 270 15 12 79 61 5 25 11 62 percentage 100 5.6 4.4 29.3 22.6 1.8 9.3 4 23 Table 7. Small-Molecule Anti-infective (Bacterial, Fungal, Parasitic, and Viral) Drugs (n = 193) indication total N ND S S/NM S* S*/NM antibacterial 104 10 67 26 1 antifungal 28 3 22 3 antiparasitic 13 2 5 4 2 antiviral 48 4 9 2 23 10 total 193 12 79 61 5 25 11 percentage 100 6.2 40.9 31.6 2.6 13 5.7 Journal of Natural Products Review 322 dx.doi.org/10.1021/np200906s | J. Nat. Prod. 2012, 75, 311−335
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