Pyrazole-Based Acid Ceramidase Inhibitors: Design, Synthesis, and Structure–Activity Relationships
نویسندگان
چکیده
منابع مشابه
Fragment-Based Hologram QSAR Studies on a Series of 2,4-Dioxopyrimidine-1-Carboxamides As Highly Potent Inhibitors of Acid Ceramidase
A series of structurally related 2,4-dioxopyrimidine-1-carboxamide derivatives as highly potent inhibitors against acid ceramidase were subjected to hologram quantitative structure-activity relationship (HQSAR) analysis. A training set containing 24 compounds served to establish the HQSAR model. The best HQSAR model was generated using atoms, bond, connectivity, donor and acceptor as fragment d...
متن کاملFragment-Based Hologram QSAR Studies on a Series of 2,4-Dioxopyrimidine-1-Carboxamides As Highly Potent Inhibitors of Acid Ceramidase
A series of structurally related 2,4-dioxopyrimidine-1-carboxamide derivatives as highly potent inhibitors against acid ceramidase were subjected to hologram quantitative structure-activity relationship (HQSAR) analysis. A training set containing 24 compounds served to establish the HQSAR model. The best HQSAR model was generated using atoms, bond, connectivity, donor and acceptor as fragment d...
متن کاملDesign and synthesis of pyrazole/isoxazole linked arylcinnamides as tubulin polymerization inhibitors and potential antiproliferative agents.
As pyrazole and isoxazole based derivatives are well-known for displaying a considerable biological profile, an attempt has been made to unravel their cytotoxic potential. In this context, a number of pyrazole/isoxazole linked arylcinnamide conjugates (15a-o and 21a-n) have been synthesized by employing a straight forward route. The basic structure comprised three ring scaffolds (A, B and C): m...
متن کاملDesign, synthesis and evaluation of pyrazole derivatives as non-nucleoside hepatitis B virus inhibitors.
In continuation of our efforts toward the discovery of potent non-nucleoside hepatitis B virus (HBV) inhibitors with novel structures, we have employed bioisosterism and hybrid pharmacophore-based strategy to explore the chemically diverse space of bioactive compounds. In this article, the original thiazole platform was replaced with pyrazole scaffold to yield the optimal pharmacophore moieties...
متن کاملBioengineered Peptides Based on α1-PDX Structure as Inhibitors of Furin: Design, Synthesis and Comparative Efficacy
Furin is a Ca 2+ <span style="color: #231f20; font-family: Times New...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Synthesis
سال: 2016
ISSN: 0039-7881,1437-210X
DOI: 10.1055/s-0035-1561456