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OrganoCATAlytic approaches towards easily synthesized, economical, and high yielding oseltamivir derivatives

Objective

Despite widespread immunization, influenza still kills thousand of people, and costs to US, Europe and Asia enormous amount of money in term of healthcare expenses and productivity losses. While immunization remains an important approach to prevent influenza, small-molecule antiviral agents represent a novel opportunity for effective prevention and therapy of flu. Inhibitors of neuraminidase, essential enzyme for viral replication in all three classes of influenza viruses, has been recently found. Two of these inhibitors have reached the market, namely, zanamivir (GSKBs Relenza (1) in July 1999, and oseltamivir phosphate (Gilead Bs Tamiflu (2), also marketed by Roche) in October 1999. The recent healthy problem related to avian flu, has increase the public demand for stockpiles of Tamiflu, both as a reasonable frontline therapy against a possible flu pandemic and as a preventive agent. However, natural sources of drug (Shikimic acid) are scarcely, and increasing demand for oseltamivir phosphate has placed further pressure on Roche and the chemical community in general to develop new routes to the drug that do not involve complex natural products. In addition, the described synthesis are expensive and difficult. Moreover, in this synthesis use of hazardous azide-based reagents was necessary. New routes to Tamiflu have been recently described, but more than 12 steps in one case and 17 in another are needed. In order to find new drug candidates, cut the drug costs and improving availability as well as efficiency, new chemical synthesis are necessary. We propose a new domino reaction based on an organocatalytic approach to the synthesis of new Tamiflu derivatives. The chemistry involved in this project is easy to perform, and well adapt to industrial contest. Moreover, new chemical structures will be prepared and evaluated as potential drug against virulent and mutated flu viruses.

Field of science

  • /medical and health sciences/health sciences/infectious disease/RNA virus/influenza
  • /natural sciences/biological sciences/microbiology/virology
  • /social sciences/economics and business/business and management/commerce

Call for proposal

FP7-HEALTH-2007-A
See other projects for this call

Funding Scheme

CP-SICA - Collaborative project for specific cooperation actions dedicated to international cooperation partner countries (SICA)

Coordinator

ALMA MATER STUDIORUM - UNIVERSITA DI BOLOGNA
Address
Via Zamboni 33
40126 Bologna
Italy
Activity type
Higher or Secondary Education Establishments
EU contribution
€ 509 610,85
Administrative Contact
Pier Giorgio Cozzi (Prof.)

Participants (6)

UNIVERZITA KOMENSKEHO V BRATISLAVE
Slovakia
EU contribution
€ 226 332,80
Address
Safarikovo Nam 6
814 99 Bratislava
Activity type
Higher or Secondary Education Establishments
Administrative Contact
Beata Rajnakova (Ms.)
UNIVERSITAET ZU KOELN
Germany
EU contribution
€ 336 573,60
Address
Albertus Magnus Platz
50931 Koeln
Activity type
Higher or Secondary Education Establishments
Administrative Contact
Albrecht Berkessel (Prof.)
SUN YAT-SEN UNIVERSITY
China
EU contribution
€ 399 176
Address
West Xin Gang Road, 135
510275 Guangzhou
Activity type
Higher or Secondary Education Establishments
Administrative Contact
Gui Lu (Prof.)
HONG KONG POLYTECHNIC UNIVERSITY
China
EU contribution
€ 285 798,80
Address
Hunghom, Kowloon
N/A Hong Kong
Activity type
Higher or Secondary Education Establishments
Administrative Contact
Albert Sun Chi Chan (Prof.)
HELSINGIN YLIOPISTO
Finland
EU contribution
€ 326 763,20
Address
Yliopistonkatu 3
00014 Helsingin Yliopisto
Activity type
Higher or Secondary Education Establishments
Administrative Contact
Satu Väisänen (Ms.)
SYNKOLA, S.R.O.
Slovakia
EU contribution
€ 215 744,75
Address
Mlynska Dolina Ch2
84215 Bratislava
Activity type
Private for-profit entities (excluding Higher or Secondary Education Establishments)
Administrative Contact
Julius Durmis (Dr.)