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Chemical Optimization
Synthesis of Arylpiperazines as Perspective Toxoplasma gondii Dihydrofolate Reductase Inhibitors

Arylpiperazines as Perspective T. gondii DHFR InhibitorsToxoplasmosis is a parasitic disease caused by Toxoplasma gondii. Approximately one-third of the population worldwide is chronically infected with T. gondii. First-line treatment of toxoplasmosis is a therapy based on dihydrofolate reductase (DHFR, DHFRP1, DYR) inhibitors which act on the folate metabolic pathway, thereby inhibiting T. gondii proliferation and survival.

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Synthesis of Styryl-phenyl-ureas as Dual-targeted Inhibitors of PD-L1 and VEGFR-2

Styryl-phenyl-ureas as Perspective Inhibitors of PD-L1 and VEGFR-2Programmed death-ligand 1 (PD-L1, cluster of differentiation 274, CD274, B7 homolog 1 or B7-H1) is a transmembrane protein that plays a major role in suppressing the adaptive arm of immune system during particular events such as tissue allografts, pregnancy, autoimmune disease and some other pathological disease states. Upregulation of PD-L1 may allow cancers to evade the host immune system.

Vascular endothelial growth factor receptor 2 (VEGFR-2, Kinase insert domain receptor, KDR, CD309, FLK1) is a VEGF receptor that plays an essential role in the regulation of angiogenesis, vascular development, vascular permeability, and embryonic hematopoiesis. Abnormal functioning of VEGFR-2 is associated with cancer.

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Synthesis of Novel Derivatives of NMDARs Allosteric Modulators

Syntheses of novel allosteric modulators of NMDARsN-methyl-D-aspartate receptors (NMDARs) are ligand-gated ion channels wich is activated by L-glutamate (the brain’s primary excitatory neurotransmitter). They have many critical roles in CNS function and in various neurological and psychiatric disorders.

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Synthesis of Tetrahydroisoquinoline Derivatives as Perspective Inhibitors of P-glycoprotein 1

Tetrahydroisoquinoline Derivatives as Perspective Inhibitors of P-glycoprotein 1P-glycoprotein 1 (P-gp, Pgp, multidrug resistance protein 1, MDR1, ATP-binding cassette sub-family B member 1, ABCB1, cluster of differentiation 243 or CD243) is an important protein of the cell membrane that pumps many foreign substances out of cells. It is an ATP-dependent efflux pump with broad substrate specificity wich evolved as a defense mechanism against harmful substances. But at the same time it pumps many drugs, including anticancer chemotherapeutics, from the cell thereby weakening their action. Consequently, P-gp overexpression is one of the main mechanisms behind decreased intracellular drug accumulation and development of multidrug resistance.

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Synthesis of Barbadin Analogs as Perspective Inhibitors of the ß-Arrestin/ß2-Adaptin Interaction

Analogs of Barbadin as Perspective Inhibitors of the ß-Arrestin/ß2-Adaptin InteractionOur company, OTAVA Ltd., is offering the following chemical optimization service - synthesis of target-specific sets of novel Barbadin analogs for your biological tests. These novel compounds will be selected from a set of 1,000 unique virtual Barbadin analogs using our company’s proprietary molecular modeling platform.

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