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Chemical Optimization
Synthesis and optimization of novel X-165 inhibitor analogues with potent bioactivity to the enzyme autotaxin

Autotaxin is a specific member of the ectonucleotide pyrophosphatase/phosphodiesterase (NPP2 or ENPP2) family of enzymes that are important for generating the lipid signaling molecule lysophosphatidic acid (LPA). The activity of the secreted phosphodiesterase autotaxin produces the inflammatory signaling molecule LPA and has been associated with a number of human diseases including idiopathic pulmonary fibrosis (IPF).

Synthesis of Quinolinones as Inhibitors of mIDH1

Quinolinones - Perspective Inhibitors of mIDH1The IDH1 (isocitrate dehydrogenase (NADP+) 1, HEL-216, HEL-S-26, IDCD, IDH, IDP, IDPC, PICD) is an enzyme which catalyze the oxidative decarboxylation of isocitrate to 2-oxoglutarate. Mutations at the arginine residue (R132) in IDH1 are frequently identified in various human cancers. Inhibition of this mutated dehydrogenase (mIDH1) with small molecules has been clinically validated as a promising therapeutic treatment for multiple solid tumors and acute myeloid leukemia.

Synthesis of Arylpyridazines as Inhibitors of p38αMAPK

Arylpyridazines - Perspective Inhibitors of p38alphaMAPKThe p38αMAPK (MAPK14, mitogen-activated protein kinase 14, CSBP, CSBP1, CSBP2, CSPB1, EXIP, Mxi2, PRKM14, PRKM15, RK, SAPK2A, p38, p38ALPHA) is a serine/threonine protein kinase which plays a key role in the intracellular signaling networks that transduce and amplify stress signals into physiological changes. This kinase is a brain drug discovery target. It is involved in neuroinflammatory responses and synaptic dysfunction in multiple degenerative and neuropsychiatric brain disorders.

Synthesis of Pyrazolo[3,4-d]pyrimidines as Dual-targeted Inhibitors of HDAC1 and mTOR

Pyrazolo[3,4-d]pyrimidines - Perspective Inhibitors of HDAC1 and mTORHistone deacetylase 1 (HDAC1, GON-10, HD1, RPD3, RPD3L1, KDAC1) plays a key role in the regulation of eukaryotic gene expression. Numerous reports revealed that HDAC1 is considered one of the most promising targets for cancer therapy.

The mechanistic target of rapamycin (mTOR, mammalian target of rapamycin, FK506-binding protein 12-rapamycin-associated protein 1, FRAP, FRAP1, FRAP2, RAFT1, RAPT1, SKS) is a serine/threonine protein kinase which regulates different cellular processes - cell growth, cell proliferation, cell survival, protein synthesis, autophagy, transcription and other. mTOR is overactivated in numerous tumors.

Synthesis of 1-(Aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole Derivatives as Antiprotozoal Agents

1-(Aryl-1H-pyrrolyl)(phenyl)methyl-1H-imidazole Derivatives - Antiprotozoal AgentsTrypanosomatid and plasmodium parasites are producing a great deal of chronic diseases and affecting hundreds of millions people mainly in developing countries. However, in the last years, such diseases are dramatically disseminating worldwide, due to some factors including vector and human migrations or co-infections in immunosuppressed patients. The current antiprotozoal therapies are unsatisfactory due to their low efficacy, high toxicity and appearance of resistant parasitic strains. Therefore, there is an speedy need to develop new antiprotozoal drugs.

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.

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.

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.

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.

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.