959237-16-2

Usage

Uses

Used in Pharmaceutical Industry:
Tert-butyl 4-(4-aminopiperidin-1-yl) is used as a building block for the synthesis of potential drug candidates. The presence of the piperidine ring and the amino group at the 4-position allows for various therapeutic applications, including antipsychotic, antidepressant, and analgesic effects. The tert-butyl group contributes to the stability and lipophilicity of the molecule, which can influence its pharmacokinetic properties, making it a valuable component in the development of new medications.

Upstream product

• 1185732-60-8 tert-butyl 4-(4-oxo-1-piperidyl)piperidine-1-carboxylate 
• 182223-54-7 piperidin-4-ylcarbamic acid benzyl ester 
• 87120-72-7 1-(tert-butoxycarbonyl)-4-aminopiperidine 
• 220394-97-8 4-(benzyloxycarbonylamino)-1-(tert-butoxycarbonyl)piperidine 

Relevant academic research and scientific papers

TRIAZOLE DERIVATIVES WITH ANTIFUNGAL ACTIVITY

Disclosed are compounds of the formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, Q2, L1 and n are as defined herein. The compounds have antifungal properties and are useful in the treatment of fungal infections, including infections that are resistant to conventions anti-fungal agents. Q1 is selected from: (Formulae Ia, Ib, Ic, Id, Ie, If, Ig, Ih, Ii, Ij and Ik) wherein * indicates the point of attachment to L1.

Discovery of 2-substituted 1H-benzo[d]immidazole-4-carboxamide derivatives as novel poly(ADP-ribose)polymerase-1 inhibitors with in?vivo anti-tumor activity

Novel 1H-benzo[d]immidazole-4-carboxamide derivatives bearing five-membered or six-membered N-heterocyclic moieties at the 2-position were designed and synthesized as PARP-1 inhibitors. Structure-activity relationships were conducted and led to a number of potent PARP-1 inhibitors having IC50 values in the single or double digit nanomolar level. Some potent PARP-1 inhibitors also had similar inhibitory activities against PARP-2. Among all the synthesized compounds, compound 10a and 11e displayed strong potentiation effects on temozolomide (TMZ) in MX-1?cells (PF50?=?7.10, PF50?=?4.17). In?vivo tumor growth inhibition was investigated using compound 10a in combination with TMZ, and it was demonstrated that compound 10a could strongly potentiate the cytotoxicity of TMZ in MX-1 xenograft tumor model. Two co-crystal structures of compounds 11b and 15e complexed with PARP-1 were achieved and demonstrated a unique binding mode of these benzo-imidazole derivatives.