📜3-羟基吡啶置于一水合肼体系中,化学反应 10.0H,反应生成 3-肼基吡啶 参考文献:A Novel Potent Metal-Binding Ndm-1 Inhibitor Was Identified By Fragment Virtual,Spr And NMR Screening 标题:A Novel Potent Metal-Binding Ndm-1 Inhibitor Was Identified By Fragment Virtual,Spr And NMR Screening 摘要:Ndm-1 Can Hydrolyze Nearly All Available β-Lactam Antibiotics,Including Carbapenems. Ndm-1 Producing Bacterial Strains Are Worldwide Threats. It Is Still Very Challenging To Find A Potent Ndm-1 Inhibitor For Clinical Use. In Our Study,We Used A Metal-Binding Pharmacophore (Mbp) Enriched Virtual Fragment Library To Screen Ndm-1 Hits. Spr Screening Helped To Verify The Mbp Virtual Hits And Identified A New Ndm-1 Binder And Weak Inhibitor A1. A Solution NMR Study Of 15N-Labeled Ndm-1 Showed That A1 Disturbed All Three Residues Coordinating The Second Zinc Ion (Zn2) In The Active Pocket Of Ndm-1. The Perturbation Only Happened In The Presence Of Zinc Ion,Indicating That A1 Bound To Zn2. Based On The Scaffold Of A1,We Designed And Synthesized A Series Of Ndm-1 Inhibitors. Several Compounds Showed Synergistic Antibacterial Activity With Meropenem Against Ndm-1 Producing K. Pneumoniae. DOI:10.1016/j.Bmc.2020.115437
专利号:US-4093812-A 优先权日:1975-03-25 标 题:(Nitrofuryl)pyrazoles, their synthesis and use, and compositions containing them 发明人:RAINER GEORG 权利人:BYK GULDEN LOMBERG CHEM FAB 摘要:3-(5-Nitro-2-furyl)pyrazoles unsubstituted in the 5-position and 5-(5-nitro-2-furyl)pyrazoles unsubstituted in the 3-position are antimicrobials and disinfectants. The compounds are structurally represented by one of the formulae: ##STR1## wherein A is --CHO, --CN, --COOH, a protected or derived aldehyde group or a protected or derived carboxylic acid group; n B is 5-nitro-2-furyl; n R 1 is --H, substituted or unsubstituted hydrocarbyl (saturated or unsaturated; acyclic, alicyclic or aromatic; or araliphatic); substituted or unsubstituted (cycloaliphatic or aromatic) heterocyclic or acyl (carboxylic or carbonic acid); n R 2 is --H; and n n is a positive whole number of at most 2.
专利号:US-9714226-B2 优先权日:2011-07-29 标题:Hydrazide containing nuclear transport modulators and uses thereof 发明人:SANDANAYAKA VINCENT P; SHACHAM SHARON; MCCAULEY DILARA; SHECHTER SHARON 权利人:KARYOPHARM THERAPEUTICS INC 摘要:The invention generally relates to nuclear transport modulators, e.g., CRM1 inhibitors, and more particularly to a compound represented by structural formula I: n nor a pharmaceutically acceptable salt thereof, wherein the values and alternative values for the variables are as defined and described herein. The invention also includes the synthesis and use of a compound of structural formula I, or a pharmaceutically acceptable salt or composition thereof, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with CRM1 activity.