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Benzimidazole Screening Library - Structures & Pharmacology

320 compounds

The benzimidazole privileged scaffold occupies a prominent position in medical research. Benzimidazoles are widespread in many different therapeutic areas. They are useful as analgesics (opioids, cannabinoids), anti-viral (Hep C, HIV,...), anti-fungal and anti-tumor agents, they are used in cardiovascular and neuro research, in endocrinology (diabetes, renal failure, osteoporosis,...), in opthalmology (glaucoma)... just to name a few.

Many benzimidazoles are known to exhibit several different biological activities. Using our drug-like benzimidazole library, you are bound to discover novel, biologically active molecules against your target. The BioQuadrant benzimidazole screening library consists of 320 unique benzimidazole compounds that you will not easily find somewhere else. The collection has been distributed over four 96 polypropylene 1mL deep-well plates, each plate containing exactly 80 structures. Each well contains a single product in 1 micromole quantity per well. Adding 100 microliter of DMSO will yield a 10mM solution.

This diverse collection of benzimidazoles has been sub-divided into 4 different 96-well plates as follows:

Plate# BQ-B1: 80 molecules An 80-member exploratory discovery library containing unique benzimidazoles bearing substituted pyrrolidine or tetrahydro-isoquinoline moieties. Substituents are located both on the benzimidazole aromatic ring and on the pyrrolidines or tetrahydroisoquinolines. In addition, the compounds are available with and without a sulfonamide moiety. To learn more about this collection and to view all individual structures, click here.

Plate# BQ-B2: 80 molecules A set of 80 benzimidazoles carrying an acetyl group at position 5 or the benzimidazole ring. The benzimidazole scaffold is further populated with a variety of pharmacologically interesting groups, including heterocycles (pyridyl- and imidazoyl), aryl moieties (carrying halogens or alkoxy substituents), alkyl and/or hydroxyalkyl groups. To learn more about this collection and to view all individual structures, click here.

Plate# BQ-B3: 80 molecules A set of 80 unique benzimidazoles. A common characteristic within this plate is that each molecules carries a sulfonamide group. The sulfonamide is linked to the benzmidazole ring via linker. The linker is either a pyrrolidine, piperidine, phenylpropyl or tetrahydroisoquinolinyl moiety. Substituents on the sulfonyl group include alkyl and aryl groups functionalized with electron donors or electron acceptors. To learn more about this collection and to view all individual structures, click here.

Plate# BQ-B4: 80 molecules A diverse set of 80 unique benzimidazoles. The aromatic ring of the benzimidazole moiety carries substituents such as piperidine, piperidine carboxamide, hydroxymethyl pyrrolidine, sulfonyl piperazines, hydroxypiperidine, trifluoromethyl, imidazole, carboxyl,... The 2-position of the benzimidazole carries both aryl (e.g dimethoxyphenyl, pyridinyl, chlorophenyl, dichlorophenyl) and alkyl (isobutyl, isopropyl) groups. A third group of substituents placed on the benzimidazole nitrogen atom (position 1) consists i.a of imidazolyl-propyl, hydroxy ethyl, morpholinyl-ethyl, cyclohexyl, diethylamino ethyl, and a chiral phenylpropanol group. To learn more about this collection and to view all individual structures, click here.

Pharmacology of Benzimidazoles

The benzimidazole motif occurs in many approved and investigational drugs. Well-known examples of approved benzimidazole-based drugs include omeprazole (Prilosec, a proton-pump inhibitor), candesertan (anti-hypertensive, an angiotensin II receptor antagonist), mebendazole (treatment of worm infestations) and astemizole (an anti-histamine):

Reported bioactivities of benzimidazole-based inhibition of proteins include but are not limited to the following:

• inhibition of histone deacetylase (HDAC)
• inhibition of poly(ADP-ribose)polymerase (PARP)
• inhibition of transient receptor potential cation channel C4 (TRPC4)
• inhibition of serine/threonine kinase 33 activity
• inhibition of the mTORC1 signaling pathway
• inhibition of sentrin-specific protease 6 (SENP6)
• inhibition of Bloom's syndrome helicase (BLM)
• inhibition of the ras-converting enzyme
• inhibition of nuclear receptor ROR gamma transcriptional activity
• inhibition of sentrin-specific protease 8 (SENP8)
• inhibition of the Human Apurinic/apyrimidinic Endonuclease 1 (APE1)
• inhibition of A1 Apoptosis
• inhibition of HPGD (15-Hydroxyprostaglandin Dehydrogenase)
• inhibition of Respiratory syncytial virus (RSV)
• inhibition of Protein Phosphatase Methylesterase 1 (PME-1)
• inhibition Activity against HIV-1 Fusion (CCR5 Tropic HIV-1 Fusion Inhibition Assay
• inhibition of Human Pyruvate Kinase M2 isoform
• inhibition of VIM-2 metallo-beta-lactamase
• inhibition of lysophospholipase 1 (LYPLA1)
• inhibition of Protein Phosphatase Methylesterase 1 (PME-1)
• inhibition of the Plasmodium falciparum M18 Aspartyl Aminopeptidase (PFM18AAP)
• inhibition of BCL2-related protein, long isoform (BCLXL)
• inhibition of GASC-1 Activity
• inhibition of glycogen synthase kinase 3 beta activity
• inhibition of Protein Phosphatase 5 (PP5)
• inhibition of the oxidoreductase glutathione S-transferase omega 1(GSTO1)
• inhibition of Streptokinase Promotor Activity
• inhibition of Hepatitis C Virus (HCV) core protein dimerization
• inhibitors of TNF-a-specific NF-kB induction