5-Bromoimidazo[1,2-a]pyridine (cas: 69214-09-1) belongs to imidazole derivatives. 1H-imidazole is an imidazole tautomer which has the migrating hydrogen at position 1. It is a conjugate base of an imidazolium cation. It is a conjugate acid of an imidazolide. It is a tautomer of a 4H-imidazole. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Category: imidazoles-derivatives
Discovery of Novel PI3-Kinase δ Specific Inhibitors for the Treatment of Rheumatoid Arthritis: Taming CYP3A4 Time-Dependent Inhibition was written by Safina, Brian S.;Baker, Stewart;Baumgardner, Matt;Blaney, Paul M.;Chan, Bryan K.;Chen, Yung-Hsiang;Cartwright, Matthew W.;Castanedo, Georgette;Chabot, Christine;Cheguillaume, Arnaud J.;Goldsmith, Paul;Goldstein, David M.;Goyal, Bindu;Hancox, Timothy;Handa, Raj K.;Iyer, Pravin S.;Kaur, Jasmit;Kondru, Rama;Kenny, Jane R.;Krintel, Sussie L.;Li, Jun;Lesnick, John;Lucas, Matthew C.;Lewis, Cristina;Mukadam, Sophie;Murray, Jeremy;Nadin, Alan J.;Nonomiya, Jim;Padilla, Fernando;Palmer, Wylie S.;Pang, Jodie;Pegg, Neil;Price, Steve;Reif, Karin;Salphati, Laurent;Savy, Pascal A.;Seward, Eileen M.;Shuttleworth, Stephen;Sohal, Sukhjit;Sweeney, Zachary K.;Tay, Suzanne;Tivitmahaisoon, Parcharee;Waszkowycz, Bohdan;Wei, Binqing;Yue, Qin;Zhang, Chenghong;Sutherlin, Daniel P.. And the article was included in Journal of Medicinal Chemistry in 2012.Category: imidazoles-derivatives This article mentions the following:
PI3Kδ is a lipid kinase and a member of a larger family of enzymes, PI3K class IA(α, β, δ) and IB (γ), which catalyze the phosphorylation of PIP2 to PIP3. PI3Kδ is mainly expressed in leukocytes, where it plays a critical, nonredundant role in B cell receptor mediated signaling and provides an attractive opportunity to treat diseases where B cell activity is essential, e.g., rheumatoid arthritis. We report the discovery of novel, potent, and selective PI3Kδ inhibitors and describe a structural hypothesis for isoform (α, β, γ) selectivity gained from interactions in the affinity pocket. The critical component of our initial pharmacophore for isoform selectivity was strongly associated with CYP3A4 time-dependent inhibition (TDI). We describe a variety of strategies and methods for monitoring and attenuating TDI. Ultimately, a structure-based design approach was employed to identify a suitable structural replacement for further optimization. In the experiment, the researchers used many compounds, for example, 5-Bromoimidazo[1,2-a]pyridine (cas: 69214-09-1Category: imidazoles-derivatives).
5-Bromoimidazo[1,2-a]pyridine (cas: 69214-09-1) belongs to imidazole derivatives. 1H-imidazole is an imidazole tautomer which has the migrating hydrogen at position 1. It is a conjugate base of an imidazolium cation. It is a conjugate acid of an imidazolide. It is a tautomer of a 4H-imidazole. Imidazole based anticancer drug find applications in cancer chemotherapy. It is used as buffer component for purification of the histidine tagged recombinant proteins in immobilized metal-affinity chromatography (IMAC).Category: imidazoles-derivatives
Referemce:
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem