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Projects / Programmes source: ARRS

Medicinal chemistry - drug design, synthesis and evaluation

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Periods
January 1, 2022 - December 31, 2027
Research activity

Code Science Field Subfield
1.09.00  Natural sciences and mathematics  Pharmacy   
1.04.00  Natural sciences and mathematics  Chemistry   

Code Science Field
3.01  Medical and Health Sciences  Basic medicine 
1.04  Natural Sciences  Chemical sciences 
Keywords
Medicinal chemistry, drug discovery, drug development, drug design, organic synthesis, biological evaluation, anti-neurodegeneration drugs, antimicrobial drugs, immunomodulatory drugs, anticancer drugs, toxicology.
Evaluation (rules)
source: COBISS
Points
22,346.43
A''
4,504.81
A'
11,712.22
A1/2
15,971.1
CI10
17,003
CImax
344
h10
56
A1
79.83
A3
36.42
Data for the last 5 years (citations for the last 10 years) on June 9, 2023; A3 for period 2017-2021
Data for ARRS tenders ( 04.04.2019 – Programme tender , archive )
Citations Citations for bibliographic records in COBIB.SI that are linked to records in citation databases
source: WoS source: Scopus source: COBISS
Database Linked records Citations Pure citations Average pure citations
WoS  1,051  21,546  18,334  17.44 
Scopus  1,100  23,460  20,046  18.22 
Researchers (57)
no. Code Name and surname Research area Role Period No. of publications
1.  21456  PhD Marko Anderluh  Natural sciences and mathematics  Researcher  2022 - 2023  359 
2.  52092  Damjan Avsec  Natural sciences and mathematics  Junior researcher  2022 - 2023  43 
3.  36454  PhD Maruša Bizjak  Natural sciences and mathematics  Researcher  2022  28 
4.  34350  PhD Aljoša Bolje  Natural sciences and mathematics  Researcher  2022  45 
5.  37459  PhD Andrej Emanuel Cotman  Natural sciences and mathematics  Researcher  2022 - 2023  43 
6.  19281  PhD Zdenko Časar  Natural sciences and mathematics  Researcher  2022 - 2023  153 
7.  54784  Jaka Dernovšek  Natural sciences and mathematics  Junior researcher  2022 - 2023  23 
8.  50400  PhD Ana Dolšak  Natural sciences and mathematics  Researcher  2022 - 2023  22 
9.  50490  Martina Durcik  Natural sciences and mathematics  Junior researcher  2022 - 2023  54 
10.  55890  Svit Ferjančič Benetik  Natural sciences and mathematics  Junior researcher  2022 - 2023  1 
11.  31879  Petra Ferkov    Technician  2022 - 2023  0 
12.  34841  Maja Frelih  Biotechnical sciences  Technician  2022 - 2023  16 
13.  26512  PhD Rok Frlan  Natural sciences and mathematics  Researcher  2022 - 2023  107 
14.  15706  PhD Tanja Gmeiner  Natural sciences and mathematics  Researcher  2022  146 
15.  15284  PhD Stanislav Gobec  Natural sciences and mathematics  Principal Researcher  2022 - 2023  801 
16.  50814  Katarina Grabrijan  Natural sciences and mathematics  Researcher  2022 - 2023  9 
17.  32036  PhD Martina Hrast Rambaher  Natural sciences and mathematics  Researcher  2022 - 2023  110 
18.  24400  PhD Janez Ilaš  Natural sciences and mathematics  Researcher  2022 - 2023  227 
19.  18619  PhD Maša Kandušer  Natural sciences and mathematics  Researcher  2022 - 2023  159 
20.  21459  PhD Nataša Karas Kuželički  Natural sciences and mathematics  Researcher  2022 - 2023  163 
21.  01463  PhD Danijel Kikelj  Natural sciences and mathematics  Researcher  2022 - 2023  561 
22.  21692  Irena Klančnik Mavec    Technician  2022 - 2023  0 
23.  36438  PhD Damijan Knez  Natural sciences and mathematics  Researcher  2022 - 2023  176 
24.  26495  PhD Nina Kočevar Glavač  Natural sciences and mathematics  Researcher  2022 - 2023  217 
25.  55892  Anja Kodila  Natural sciences and mathematics  Junior researcher  2022 - 2023  1 
26.  30815  PhD Meta Kokalj Ladan  Natural sciences and mathematics  Researcher  2022 - 2023  31 
27.  55572  PhD Alen Krajnc  Natural sciences and mathematics  Researcher  2022 - 2023  28 
28.  36423  PhD Eva Kranjc  Natural sciences and mathematics  Researcher  2022  30 
29.  34223  PhD Tijana Markovič  Natural sciences and mathematics  Researcher  2022 - 2023  52 
30.  53584  Anže Meden  Natural sciences and mathematics  Junior researcher  2022 - 2023  32 
31.  12443  PhD Irena Mlinarič Raščan  Natural sciences and mathematics  Researcher  2022 - 2023  509 
32.  23419  PhD Janez Mravljak  Natural sciences and mathematics  Researcher  2022 - 2023  194 
33.  50623  PhD Doroteja Novak  Natural sciences and mathematics  Researcher  2022 - 2023  18 
34.  19061  PhD Aleš Obreza  Natural sciences and mathematics  Researcher  2022 - 2023  319 
35.  28861  PhD Stane Pajk  Natural sciences and mathematics  Researcher  2022 - 2023  171 
36.  37648  Katja Perc    Technician  2022 - 2023  11 
37.  19317  PhD Lucija Peterlin Mašič  Natural sciences and mathematics  Researcher  2022 - 2023  385 
38.  55894  Martina Piga  Natural sciences and mathematics  Junior researcher  2022 - 2023  5 
39.  52376  Matic Proj  Natural sciences and mathematics  Junior researcher  2022 - 2023  54 
40.  55895  Edvin Purić  Natural sciences and mathematics  Junior researcher  2022 - 2023  2 
41.  29603  PhD Matjaž Ravnikar  Natural sciences and mathematics  Researcher  2022 - 2023  69 
42.  08519  PhD Marija Sollner Dolenc  Natural sciences and mathematics  Researcher  2022 - 2023  625 
43.  30816  PhD Izidor Sosič  Natural sciences and mathematics  Researcher  2022 - 2023  227 
44.  25490  PhD Matej Sova  Natural sciences and mathematics  Researcher  2022 - 2023  153 
45.  53583  Maša Sterle  Natural sciences and mathematics  Junior researcher  2022 - 2023  10 
46.  52378  Nika Strašek Benedik  Natural sciences and mathematics  Junior researcher  2022 - 2023  0 
47.  29982  PhD Alenka Šmid  Natural sciences and mathematics  Researcher  2022 - 2023  113 
48.  52094  Andrej Šterman  Natural sciences and mathematics  Junior researcher  2022  14 
49.  33335  PhD Eva Tavčar  Natural sciences and mathematics  Researcher  2022 - 2023  66 
50.  35325  Martina Tekavec    Technician  2022 - 2023  0 
51.  28334  PhD Tihomir Tomašić  Natural sciences and mathematics  Researcher  2022 - 2023  337 
52.  52375  PhD Žan Toplak  Natural sciences and mathematics  Researcher  2022 - 2023  24 
53.  34512  PhD Dunja Urbančič  Natural sciences and mathematics  Researcher  2022 - 2023  46 
54.  50503  PhD Matjaž Weiss  Natural sciences and mathematics  Junior researcher  2022  33 
55.  17438  Damijana Zalar    Technician  2022 - 2023  0 
56.  18633  PhD Anamarija Zega  Natural sciences and mathematics  Researcher  2022 - 2023  180 
57.  28905  PhD Nace Zidar  Natural sciences and mathematics  Researcher  2022 - 2023  204 
Organisations (1)
no. Code Research organisation City Registration number No. of publications
1.  0787  University of Ljubljana, Faculty of Pharmacy  Ljubljana  1626973  16,562 
Abstract
The long-term goal of the research programme is the discovery of new bioactive small molecules with a potential for development into drugs for use in important therapeutic areas through combined medicinal chemistry approaches. In the next period, the research programme will focus on the discovery and rational design, synthesis and biological evaluation of molecules with the ability of modulating validated drug targets. This process will produce new anti-neurodegenerative, antimicrobial, immunomodulatory and anticancer agents of high importance for public health. The research programme will address a variety of drug targets involved in transmembrane and intracellular signalling, i.e. bacterial and human enzymes, membrane, intracellular and nuclear receptors and ion channels. Contemporary medicinal chemistry strategies, including biomimetic and natural products-inspired design, fragment-based drug design (FBDD), approaches for achieving selectivity and drug-like properties will be applied. Ligands capable of modulating two or more drug targets of interest at the same time (MTDLs) will also be designed. The major proposed research topics for the next research programme period include development of new drugs targeting (i) neurodegeneration through inhibition of cholinesterases, monoamine oxidases and kinases, and modulation of monoaminergic receptors and oxidative targets, (ii) multidrug resistant bacteria and coronaviruses through inhibition of DNA gyrase, topoisomerase IV, MurA, D-Ala-D-Ala ligase B, penicillin biding proteins, proteasome, enoyl acyl carrier protein reductase (InhA) and cysteine proteases, (iii) the immune system through modulation of Toll-like receptors and galectins, inhibition of immunoproteasome and O-linked ß-N-acetylglucosamine transferase (OGT), (iv) cancer through inhibition of the human ether-a-go-go channels (hERG), potassium voltage-gated channels (Kv1.3), heat shock protein 90 (Hsp90), DNA topoisomerase II?, proteasome and modulation of the prostaglandin E2 receptor 4 (EP4). Toxicological aspects of the drug discovery process including the determination of (i) PADMET properties of new compounds, (ii) the mechanism of toxicity of endocrine disrupting chemicals, (iii) the influence of metabolism on biological activity and toxicity, and (iv) the effects of antioxidants on oxidative stability of compounds will also be a major research topic in this research programme.
Significance for science
The importance of the proposed research programme for the development of science lies in (i) the discovery of novel bioactive compounds that have the potential to be developed into drugs for important therapeutic areas and (ii) the development of methods for their design, synthesis and insight into their mechanism of action at the molecular level. The outcome of the research programme will be innovative new molecules that act as modulators of important validated drug targets in antineurodegenerative, antimicrobial, immunomodulatory and anticancer therapeutic areas. The PADMET properties of these new compounds and the impact of their metabolism on biological activity and toxicity will also be determined. The knowledge gained from this proposed research programme will be of high scientific value and will be directly applicable in the preclinical drug discovery process. The treatment strategies presented in this research programme for neurodegenerative diseases such as Alzheimer's and Parkinson's disease, infectious diseases caused by resistant bacteria and coronaviruses, immunodeficiency diseases, and cancer have been neglected, but may lead to promising new lead compounds and potential drugs. The information obtained in this proposed research programme on the occurrence and adverse effects of some chemicals on human health will also be a very important contribution to the development of guidelines, policies and regulations for harmonized assessment and risk management at national and European level. This will make an important contribution to the science platform for the protection of public health.
Significance for the country
The Slovenian pharmaceutical industry is currently one of the most important industries in the Slovenian economy. Despite its current generic character, the Slovenian pharmaceutical industry is research-oriented and needs creative and competent scientists. Young scientists trained in the proposed research programme will gain competences for autonomous creative work in the pharmaceutical industry, where they will set novel research priorities. They will be perfectly trained for research work in pharmaceutical industry, universities, other research institutes and government agencies. During the last funding period, members of the programme group supervised twenty-two completed scientific PhDs, all of whom successfully found employment: 12 of them in the pharmaceutical industry, eight in universities and public research institutions, and two abroad. This is an important socio-economic achievement of the research program to date and is a guarantee of prosperity for future PhD students. The proposed research programme will generate novel bioactive compounds with high potential for development into lead compounds and drugs. They can be an excellent starting point for the development of innovative drugs in collaboration with the Slovenian and international pharmaceutical industry. The results related to the development of alternative synthetic routes for drug synthesis, protected by several patent applications, find their direct application in the Slovenian generic pharmaceutical industry. Some of the results of the research programme have reached a high level of technological maturity, which will enable creation of spin-off companies. The promotion of scientific excellence, which is one of the main objectives of the proposed research program, will contribute to the validation of Slovenian science through publications in leading scientific journals and participation in the most important international scientific conferences worldwide. A broad network of international collaborations, which are an important attribute of the proposed research programme, is a good way to promote Slovenian science and build strategic alliances for the benefit of Slovenian and global science. All these activities will contribute to the creation and preservation of the country's national identity in Europe and in the world. The social development of Slovenia and the growth of its scientific culture is an important goal of the proposed research programme. Therefore, communication of the programme activities to various target groups is mandatory. All researchers involved in the programme will promote the programme and ensure that their research results are presented to the public in a way that can be understood by all. This will improve public understanding of drug discovery processes, cancer, multi-drug resistant bacterial infections, neurodegenerative diseases and immune system diseases. It will also raise awareness of the challenges to which the proposed programme is responding and contribute to the popularization of science among young people and in society.
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