Search Results - "KIKELJ, D"
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Multitarget cardiovascular drugs
Published in Current medicinal chemistry (01-06-2011)“…Cardiovascular disease is the number one cause of death globally. Design of cardiovascular drugs based on new paradigms is therefore a prominent goal of…”
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Dual inhibitors of the blood coagulation enzymes
Published in Current medicinal chemistry (01-10-2004)“…The search for an ideal anticoagulant has spanned decades and has resulted in several approaches and the identification of novel target molecules for…”
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3
Recent advances in the discovery of tissue factor/factor VIIa inhibitors and dual inhibitors of factor VIIa/factor Xa
Published in Current pharmaceutical design (01-01-2005)“…The search for an ideal anticoagulant has spanned decades and has taken several approaches to the identification of novel target molecules for preventing and…”
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4
Influence of Chirality of the Preceding Acyl Moiety on the cis/trans Ratio of the Proline Peptide Bond
Published in Journal of organic chemistry (19-10-2001)“…We report that the cis/trans ratio of the proline peptide bond can be strongly influenced by the chirality of the acyl residue preceding proline. Acyl moieties…”
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5
Design and structure–activity relationship of thrombin inhibitors with an azaphenylalanine scaffold: potency and selectivity enhancements via P2 optimization
Published in Bioorganic & medicinal chemistry (01-10-2001)“…Theoretical and structural studies followed by the directed synthesis and in vitro biological tests lead us to novel noncovalent thrombin pseudopeptide…”
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6
Discovery and Hit-to-Lead Optimization of Benzothiazole Scaffold-Based DNA Gyrase Inhibitors with Potent Activity against Acinetobacter baumannii and Pseudomonas aeruginosa
Published in Journal of medicinal chemistry (26-01-2023)“…We have developed compounds with a promising activity against Acinetobacter baumannii and Pseudomonas aeruginosa, which are both on the WHO priority list of…”
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7
Recent advances in the synthesis of 2H-1,4-benzoxazin-3-(4H)-ones and 3,4-dihydro-2H-1,4-benzoxazines
Published in Tetrahedron (01-08-2005)Get full text
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Arginine mimetics
Published in Tetrahedron (13-08-2001)“…Arginine mimetics, which were designed and synthesised to mimic the function of the arginine moiety in numerous peptidomimetics, e.g. serine protease…”
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Substituted 4-phenyl-2-aminoimidazoles and 4-phenyl-4,5-dihydro-2-aminoimidazoles as voltage-gated sodium channel modulators
Published in European journal of medicinal chemistry (03-03-2014)“…Voltage-gated sodium channels play an integral part in neurotransmission and their dysfunction is frequently a cause of various neurological disorders. On the…”
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Toward a Novel Class of Antithrombotic Compounds with Dual Function. Discovery of 1,4-Benzoxazin-3(4H)-one Derivatives Possessing Thrombin Inhibitory and Fibrinogen Receptor Antagonistic Activities
Published in Journal of medicinal chemistry (05-05-2005)“…A novel class of potential antithrombotic compounds with moderate thrombin inhibitory and fibrinogen receptor antagonistic activity is described. Combination…”
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11
Peptidomimetic thrombin inhibitors
Published in Pathophysiology of haemostasis and thrombosis (01-01-2003)“…The central position of thrombin in the coagulation cascade has made it a popular target for discovery of novel antithrombotic agents. Starting with hirudin, a…”
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12
Design and synthesis of novel platelet fibrinogen receptor antagonists with 2H-1,4-benzoxazine-3(4H)-one scaffold. A systematic study
Published in European journal of medicinal chemistry (2005)“…New platelet glycoprotein IIb/IIIa (GP IIb/IIIa, integrin alpha(IIb)beta3) antagonists were prepared on a 2H-1,4-benzoxazine-3(4H)-one scaffold. Their…”
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13
Phosphonate inhibitors of antigen 85C, a crucial enzyme involved in the biosynthesis of the Mycobacterium tuberculosis cell wall
Published in Bioorganic & medicinal chemistry letters (05-07-2004)“…Graphic The first phosphonate inhibitors of antigen 85C––a major protein component of the Mycobacterium tuberculosis cell wall possessing mycolyltransferase…”
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14
Synthesis of alkyl 4-alkyl-2-hydroxy-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-2-carboxylates as peptidomimetic building blocks
Published in Tetrahedron (01-09-2003)Get full text
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15
Novel thrombin inhibitors incorporating non-basic partially saturated heterobicyclic P 1-Arginine mimetics
Published in Bioorganic & medicinal chemistry letters (10-03-2003)“…The design, synthesis and biological activity of non-covalent thrombin inhibitors incorporating 4,5,6,7-tetrahydroindazole,…”
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Novel pyrazinone and pyridinone thrombin inhibitors incorporating weakly basic heterobicyclic P 1-arginine mimetics
Published in European journal of medicinal chemistry (01-08-2005)“…The design, synthesis and biological activity of new thrombin inhibitors with a pyridinone or pyrazinone core and different heterobicyclic P 1 arginine…”
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Novel thrombin inhibitors incorporating weakly basic heterobicyclic P 1-arginine mimetics: optimization via modification of P 1 and P 3 moieties
Published in Bioorganic & medicinal chemistry letters (21-06-2004)“…The optimization of 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic heterobicyclic P 1-arginine side-chain mimetics is described…”
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18
A general synthetic approach to novel conformationally restricted arginine side chain mimetics
Published in Tetrahedron (18-02-2002)“…A general synthesis of several novel partially saturated, conformationally restricted heterobicyclic arginine side chain mimetics is described. These compounds…”
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Selective 3-Amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P 1-Arginine mimetics
Published in Bioorganic & medicinal chemistry letters (06-10-2003)“…Novel, highly selective and potent thrombin inhibitors were identified as a result of combing the 3-benzylsulfonylamino-2-pyridinone acetamide P 2–P 3…”
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A convenient synthesis of 4-aminomethyl-4,5,6,7-tetrahydro-1,3-benzothiazole arginine side-chain mimetics
Published in Tetrahedron letters (10-12-2001)Get full text
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