Results 221 to 230 of about 37,689 (286)

Lowering Lipophilicity by Adding Carbon: One-Carbon Bridges of Morpholines and Piperazines.

Journal of Medicinal Chemistry, 2018
In this article, we report our investigation of a phenomenon by which bridging morpholines across the ring with one-carbon tethers leads to a counterintuitive reduction in lipophilicity.
S. Degorce, M. Bodnarchuk, I. Cumming, James S. Scott   +3 more
semanticscholar   +1 more source

Fused and Substituted Piperazines as Anticancer Agents: A Review

Chemical Biology and Drug Design
Cancer is an abnormal and uncontrolled proliferation of normal cells. The availability of safer anticancer drugs with exceptional selectivity for healthy cells and great efficacy against various cancer forms continues to be a significant obstacle.
Saumya Singh, Rajnish Kumar, Shrishti Tripathi, Salahuddin, Avijit Mazumder, Nardev Singh   +5 more
semanticscholar   +1 more source

Chrysosporazines A-E: P-Glycoprotein Inhibitory Piperazines from an Australian Marine Fish Gastrointestinal Tract-Derived Fungus, Chrysosporium sp. CMB-F214.

Organic Letters, 2019
Chemical analysis of Chrysosporium sp. CMB-F214, yielded five new piperazines, chrysosporazines A-E (1-5), with structures assigned by spectroscopic and X-ray analyses and biosynthetic considerations.
Ahmed H. Elbanna, Zeinab G. Khalil, P. Bernhardt, R. Capon   +3 more
semanticscholar   +1 more source

New phenolic Mannich bases with piperazines and their bioactivities.

Bioorganic chemistry (Print), 2019
In this study, new Mannich bases, 2-(4-hydroxy-3-methoxy-5-((substitutedpiperazin-1-yl)methyl)benzylidene)-2,3-dihydro-1H-inden-1-one (1, 2, 4, 5, 8), 2-(3-((substituted)piperazin-1-yl)methyl)-4-hydroxy-5-methoxybenzylidene)-2,3-dihydro-1H-inden-1-one (3,
H. Gul, M. Tuğrak, M. Gul, Sertac Mazlumoglu, H. Sakagami, I. Gulcin, C. Supuran   +6 more
semanticscholar   +1 more source

Synthesis and discovery of triazolo-pyridazine-6-yl-substituted piperazines as effective anti-diabetic drugs; evaluated over dipeptidyl peptidase-4 inhibition mechanism and insulinotropic activities.

European journal of medicinal chemistry, 2019
A family of 12 triazolo-pyridazine-6-yl-substituted piperazines (5a-l) was synthesized and evaluated for their Dipeptidyl peptidase-4 (DPP-4) inhibition potentials in order to develop them as anti-diabetic medications.
B. Bindu, S. Vijayalakshmi, A. Manikandan   +2 more
semanticscholar   +1 more source

High Catalytic Activity of Pd Nanoparticles Synthesized from Green Alga Chlorella vulgaris in Buchwald-hartwig Synthesis of N-Aryl Piperazines

, 2019
The N-aryl piperazines are an important component of many drug products used for the treatment of malaria, depression, anxiety and Parkinson diseases. Buchwald-Hartwig amination is the latest and well-known reaction for Pd catalyzed direct synthesis of
V. Mishra, Anju Arya, T. Chundawat
semanticscholar   +1 more source

Synthesis of N-Pyrrolyl(furanyl)-Substituted Piperazines, 1,4-Dizepanes, and 1,4-Diazocanes.

Journal of Organic Chemistry, 2019
The synthetic potential of 5-bromo-1,1,1-trifluoro-4-methoxypent-3-en-2-one toward the catalyst-free synthesis of N-pyrrolyl(furanyl)-piperazines, 1,4-diazepanes, and 1,4-diazocanes through a telescoped protocol is reported.
Mateus Mittersteiner, Valquiria P. Andrade, Lucimara L. Zachow, C. Frizzo, H. Bonacorso, M. Martins, N. Zanatta   +6 more
semanticscholar   +1 more source

Discovery and optimization of novel piperazines as potent inhibitors of fatty acid synthase (FASN).

Bioorganic & Medicinal Chemistry Letters, 2019
The discovery, structure-activity relationships, and optimization of a novel class of fatty acid synthase (FASN) inhibitors is reported. High throughput screening identified a series of substituted piperazines with structural features that enable ...
Matthew W. Martin, D. Lancia, Hongbin Li, Shawn E R Schiller, A. Toms, Zhongguo Wang, K. Bair, Jennifer Castro, S. Fessler, D. Gotur, Stephen E. Hubbs, G. Kauffman, Mark T. Kershaw, G. P. Luke, Crystal L. McKinnon, Lili Yao, W. Lu, David S. Millan   +17 more
semanticscholar   +1 more source

Selective, Catalytic, and Dual C(sp3)-H Oxidation of Piperazines and Morpholines under Transition-Metal-Free Conditions.

Journal of Organic Chemistry, 2018
By using cheap and innocuous reagents, such as NaClO2, NaOCl, and catalytic amounts of TEMPO, a new environmentally friendly protocol for the selective and catalytic TEMPO C(sp3)-H oxidation of piperazines and morpholines to 2,3-diketopiperazines (2,3 ...
Delfino Chamorro‐Arenas, Urbano Osorio-Nieto, L. Quintero, L. Hernandez-Garcia, Fernando Sartillo‐Piscil   +4 more
semanticscholar   +1 more source

Discovery and optimization of heteroaryl piperazines as potent and selective PI3Kδ inhibitors.

Bioorganic & Medicinal Chemistry Letters, 2019
A high-throughput screening (HTS) campaign identified a class of heteroaryl piperazines with excellent baseline affinity and selectivity for phosphoinositide 3-kinase δ (PI3Kδ) over closely related isoforms. Rapid evaluation and optimization of structure-
Hua Zhou, Meredeth A. McGowan, Kate Lipford, M. Christopher, X. Fradera, D. Witter, C. Lesburg, Chaomin Li, J. Methot, J. Lampe, Abdelghani Achab, Lynsey Shaffer, P. Goldenblatt, Sanjiv J. Shah, A. Bass, Gottfried K. Schroeder, Dapeng Chen, Haoyu Zeng, M. Augustin, J. Katz   +19 more
semanticscholar   +1 more source