Naslov
Novel approach to drug discovery in PLIVA - establishing of HTS unit and unique Compounds Library

Autori
Jelić, Dubravko ; Mesar, Vesna ; Bašic, Ivan ; Nadramija, Damir ; Verbanac, Donatella

Izvornik
Pharmachem (1720-4003) 2 (2003), 6; 64-67

Vrsta, podvrsta i kategorija rada
Radovi u časopisima, članak, stručni

Ključne riječi
HTS; compounds library; drug discovery

Sažetak
Drug discovery process is long and expensive. Following a common objective to shorten this process through a production and/or collection of high-quality drug-like compounds that in turn, generate high volumes of quality data thanks to the High Throughput Screening technologies, a new PLIVA's Compound Library was established in the year 2000. Our HTS collection today has an impressive number of organic compounds, either in-house produced or acquired from different companies or institutions. The Compound Library contains many different structural classes. Some of them are literally handcrafted compounds, produced by original synthetic techniques, often unique to PLIVA because of its more than 60 years long experience in the medicinal chemistry. The compounds in PLIVA’ s collection are diverse ; most of them follow Lipinski’ s “ the rule of 5” describing the characteristics of chemical compounds with a stronger prospect of becoming potential drug candidates. But Lipinski’ s rules are not absolute and should not be used to automatically eliminate compounds from consideration. One of the best known exceptions is the Azithromycin, a successful “ blockbuster” antibiotic and one of PLIVA-s inventions. Our objective is to collect high quality compounds in a sufficient volume necessary to perform screening on selected targets. Our compounds undergo rigorous analysis before they can be registered as PL compounds (a unique PLIVA's code). The compounds’ structures are typically confirmed by LC-MS and H1NMR. Compounds are stored in vials and microtiter plates that are then used for producing mother-plates for targeted screening. PLIVA Compounds Library and a data produced in HTS are important part of the PLIVA R&D Database, developed and maintained by Research Information Center, where many UserClient applications are built in support of R&D.

Izvorni jezik
Engleski

Znanstvena područja
Farmacija

POVEZANOST RADA