Results 31 to 40 of about 1,055 (154)

Synthesis and Structural Activity Relationship Study of Antitubercular Carboxamides

International Journal of Medicinal Chemistry, Volume 2014, Issue 1, 2014., 2014
The unusual structure and chemical composition of the mycobacterial cell wall, the tedious duration of therapy, and resistance developed by the microorganism have made the recurrence of the disease multidrug resistance and extensive or extreme drug resistance.
D. I. Ugwu, B. E. Ezema, F. U. Eze, D. I. Ugwuja, Arie Zask   +4 more
wiley   +1 more source

Synthesis, Computational Studies and Preliminary Pharmacological Evaluation of New Arylpiperazines

Journal of Chemistry, Volume 8, Issue 3, Page 1044-1051, 2011., 2011
A series of novel arylpiperazines were synthesized and the target compounds evaluated for atypical antipsychotic activity in apomorphine induced climbing behavior (D2 antagonism), 5‐HTP induced head twitches (5‐HT2A antagonism) and catalepsy studies in albino mice.
Sushil Kumar, A. K. Wahi, Ranjit Singh
wiley   +1 more source

Arylpiperazine Dopamineric Ligands Protect Neuroblastoma Cells from Nitric Oxide (NO)-Induced Mitochondrial Damage and Apoptosis

, 2012
The protective ability of novel arylpiperazine-based dopaminergic ligands against nitric oxide (NO)-mediated neurotoxicity is investigated. The most potent neuroprotective arylpiperazine identified during the study was N-{4-[2-(4-phenyl-piperazin-1-yl ...
Trajković, Vladimir, Vucicevic, Ljubica, Janjetovic, Kristina, Zogovic, Nevena, Vukic Soskic, Vladimir Trajkovic, Kostić Rajačić, Slađana, Gordana Tovilovic, Andre Schrattenholz, Isaković, Aleksandra, Šoškić, Vukić, Maja Misirkic‐Marjanovic, Kostić-Rajačić, Slađana, Tovilović-Kovačević, Gordana, Tovilović, Gordana, Misirkić-Marjanović, Maja, Ljubica Vucicevic, Schrattenholz, Andre, Nevena Zogovic, Kristina Janjetovic, Sladjana Kostic‐Rajacic, Misirkić Marjanović, Maja, Aleksandra Isakovic, Harhaji-Trajković, Ljubica, Ljubica Harhaji‐Trajkovic   +24 more
core   +1 more source

Recent Advances in Isatin–Thiazole Hybrids: Synthesis, Structural Design, and Biological Application

Chemistry &Biodiversity, Volume 22, Issue 12, December 2025.
ABSTRACT Isatin–thiazole hybrids are considered privileged chemical scaffolds due to their broad spectrum of pharmacological properties, making them attractive candidates for drug development. As a result, isatin–thiazole derivatives have emerged as a prominent class of hybrid heterocycles and have been the focus of extensive research in recent years ...
Isadora M. G. Andrade, Edson de O. Lima Filho, Caio F. Valadão, Luana da S. M. Forezi, Fernando de C. da Silva   +4 more
wiley   +1 more source

Towards the convergent therapeutic potential of G protein‐coupled receptors in autism spectrum disorders

British Journal of Pharmacology, Volume 182, Issue 14, Page 3044-3067, July 2025.
Abstract Autism spectrum disorders (ASDs) are diagnosed in 1/100 children worldwide, based on two core symptoms: deficits in social interaction and communication, and stereotyped behaviours. G protein‐coupled receptors (GPCRs) are the largest family of cell‐surface receptors that transduce extracellular signals to convergent intracellular signalling ...
Anil Annamneedi, Caroline Gora, Ana Dudas, Xavier Leray, Véronique Bozon, Pascale Crépieux, Lucie P. Pellissier   +6 more
wiley   +1 more source

Short Synthesis of Enantiopure trans-3-Arylpiperazine-2-carboxylic Acid Derivatives via Diaza-Cope Rearrangement

, 2016
An efficient synthetic method was developed for the construction of enantiomerically pure trans-3-arylpiperazine-2-carboxylic acid derivatives using diaza-Cope rearrangement (DCR) as a key step starting from (R,R)/(S,S)-1,2-bis(2-hydroxyphenyl)-1,2 ...
Soon Ho Kwon (2062855), Jik Chin (2062858), Sang Min Lee (507437), B. Moon Kim (1608127), Sang Moon Byun (2062852)   +4 more
core   +1 more source

In Vitro approach for identification of a leading cytochrome P450 isoenzyme responsible for biotransformation of novel arylpiperazine drug candidates and their inhibition potency towards CYP3A4. [PDF]

, 2020
Presented article is a follow-up study of previous work, published in PLoS ONE in 2015 regarding metabolic stability of arylpiperazine derivatives, a very promising group of novel antidepressants.
Król, Marek, Bączek, Tomasz, Ulenberg, Szymon, Belka, Mariusz, Georgiev, Paweł, Herold, Franciszek   +5 more
core   +1 more source

The translational value of ligand‐receptor binding kinetics in drug discovery

British Journal of Pharmacology, Volume 181, Issue 21, Page 4117-4129, November 2024.
Abstract The translation of in vitro potency of a candidate drug, as determined by traditional pharmacology metrics (such as EC50/IC50 and KD/Ki values), to in vivo efficacy and safety is challenging. Residence time, which represents the duration of drug‐target interaction, can be part of a more comprehensive understanding of the dynamic nature of drug‐
Hongli Liu, Haoran Zhang, Adriaan P. IJzerman, Dong Guo   +3 more
wiley   +1 more source

Design and synthesis of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazole derivatives as colchicine binding site inhibitors

, 2017
A series of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazol derivatives were designed as potential microtubule targeting agents. The regioselective alkylation of 5-aryl-4-(4-arylpiperazine-1-carbonyl)-2H-1,2,3-triazole was predicted by ...
Kai Bao, Peng Yan, Weige Zhang, Daiying Zuo, Qi Guan, Yue Wu, Meiqi Gao, Zhiwei Wang, Jun Sun, Yingliang Wu, Dongjie Feng, Zhenzhen Gu   +11 more
core   +1 more source

Modeling key interactions between dopamine D2 receptor second extracellular loop and arylpiperazine ligands [PDF]

, 2012
Second extracellular loop (ecl2) of dopamine (DA) D2 receptor is an essential part of dopaminergic ligands binding pocket. To form a part of the ligand binding surface it has to fold down into the transmembrane domain of the DA receptor.
Kostić-Rajačić, Slađana, Roglić Goran, Andrić, Deana, Šukalović Vladimir, Deana Andric, Kostić-Rajačić Slađana, Roglić, Goran, Vukic Soskic, Vladimir Sukalovic, Kostić Rajačić, Slađana, Šukalović, Vladimir, Goran Roglic, Andrić Deana, Sladjana Kostic-Rajacic, Šoškić, Vukić, Šoškić Vukić   +15 more
core   +2 more sources