Article
Chemistry, Medicinal
Grigory Mokrov, Andry Pantileev, Milada Yarkova, Tatiana Gudasheva, Sergei Seredenin
Summary: New TSPO ligands with high anxiolytic activity in the series of N,1-diphenylpyrrolo[1,2-a]pyrazine-3-carboxamides were successfully designed using calculated pharmacophore model and molecular docking analysis.
MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
G. V. Mokrov, A. S. Pantileev, M. A. Yarkova, I. V. Rybina, T. A. Gudasheva, Yu. V. Vakhitova, S. B. Seredenin
Summary: A new group of 1-phenylpyrrolo[1,2-a]pyrazine-3-carboxamides was synthesized with various substituents at the amide nitrogen, such as alkyl, benzyl or alkoxyphenylalkyl groups, amino acid residues or their derivatives. These compounds exhibited high theoretical affinity values to the 18-kDa translocator protein (TSPO) and showed favorable pharmacokinetic properties, indicating their potential as drugs. Several compounds demonstrated anxiolytic activity in mice under emotional stress conditions, and a lead compound N-benzhydryl-1-phenylpyrrolo[1,2-a]pyrazine-3-carboxyamide was selected for further development as a potential anxiolytic agent.
RUSSIAN JOURNAL OF BIOORGANIC CHEMISTRY
(2023)
Article
Plant Sciences
Yu-Shih Lin, Wen-Huang Peng, Mei-Fen Shih, Jong-Yuh Cherng
Summary: Danshen (Salvia miltiorrhiza Bunge), a traditional Chinese medicine, has demonstrated pharmacological activities in treating CNS disorders. The study investigated the anxiolytic effect of the ethanol extract of Danshen and found that it exerts its mechanism through an activation of the BZD and 5HT(1A) receptors.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Chemistry, Organic
Chang He, Zijuan Wang, Yitong Chen, Guolin Zhang, Yongping Yu
Summary: This study presents a direct synthesis of multi-substituted pyrrolo[1,2-a]pyrazines via palladium(II)-catalyzed C(sp)-C(sp(2)) cascade coupling and intramolecular cyclization. The reaction originates from phenylboronic acids and readily synthesized 2-carbonyl- or 2-formylpyrroloacetonitriles, providing products in good to excellent yields for a diversity of substrates. Furthermore, a possible mechanism for the transformation is proposed.
SYNTHESIS-STUTTGART
(2021)
Article
Biochemistry & Molecular Biology
Diter Miranda-Sanchez, Carlos H. Escalante, Dulce Andrade-Pavon, Omar Gomez-Garcia, Edson Barrera, Lourdes Villa-Tanaca, Francisco Delgado, Joaquin Tamariz
Summary: In this study, pyrrolo[1,2-a]pyrazines were synthesized by cyclization of 2-formylpyrrole-based enaminones. The synthesized compounds showed a strong antifungal effect on Candida species, including multidrug-resistant strains.
Article
Chemistry, Organic
Devaiah Vytla, Parinita Shaw, Rajeswari Velayuthaperumal, Jithendra Emmadi, Arvind Mathur, Amrita Roy
Summary: The Castagnoli-Cushman reaction of various azaindole dicarboxylic acids with imines using acetic anhydride as a dehydrating agent was significantly accelerated by microwave irradiation, leading to the convenient preparation of novel compounds with good yields and stereoselectivity.
TETRAHEDRON LETTERS
(2021)
Article
Plant Sciences
Armando Escobar-Ramos, Abraham Gomez-Rivera, Carlos Ernesto Lobato-Garcia, Alejandro Zamilpa, Ever A. Ble-Gonzalez, Manases Gonzalez-Cortazar, Ammy Joana Gallegos-Garcia, Maribel Herrera-Ruiz
Summary: The study evaluated the anxiolytic effect of the extracts from Haematoxylum campechianum L. and Sapp, showing that they possess anxiolytic and sedative effects. The new compound 4-hydroxyhematoxylol isolated from the extracts was found to be partially responsible for these activities.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Plant Sciences
Taiwo G. Olubodun-Obadun, Ismail O. Ishola, Timisola P. Adesokan, Blessing O. Anih, Olufunmilayo O. Adeyemi
Summary: This study investigates the antidepressant and anxiolytic effects of ethanol seed extract of Cajanus cajan in mice. The extract shows potential in treating anxiety and other neurological disorders, possibly through the involvement of monoaminergic systems and GABA receptors.
JOURNAL OF ETHNOPHARMACOLOGY
(2023)
Article
Plant Sciences
Imane Es-safi, Hamza Mechchate, Amal Amaghnouje, Amine Elbouzidi, Mohamed Bouhrim, Noureddine Bencheikh, Christophe Hano, Dalila Bousta
Summary: The study aimed to investigate the effects of different doses of Pimpinella anisum total extract on anxiety, depression, and memory in mice. The results showed that PATE has anxiolytic and antidepressant effects, but no impact on memory.
Review
Chemistry, Medicinal
Constanza Meneses, Marisela Valdes-Gonzalez, Barbara B. Garrido-Suarez, Gabino Garrido
Summary: Anxiety disorders are prevalent and require effective treatment approaches. Current standard approaches include pharmacotherapy and psychotherapy, but these interventions may have adverse effects and treatment resistance. This review examines the potential therapeutic effects of flower extracts in treating anxiety disorders, and suggests the need for more reliable and predictive behavioral tests to obtain conclusive evidence with clinical significance.
PHYTOTHERAPY RESEARCH
(2023)
Article
Biochemistry & Molecular Biology
Yulia A. Antonova, Yulia V. Nelyubina, Sema L. Ioffe, Andrey A. Tabolin
Summary: A Rh(II)-catalyzed reaction of cyclic nitronates with vinyl diazoacetates proceeds as an annulation reaction, producing bicyclic unsaturated nitroso acetals. Optimization of reaction conditions revealed the use of Rh(II) octanoate as the preferred catalyst in THF at room temperature, allowing the preparation of target products in good yields and excellent diastereoselectivity. Under basic conditions, these nitroso acetals undergo ring contraction into the corresponding pyrroles, and both transformations can be performed in a one-pot fashion.
Article
Pharmacology & Pharmacy
Gabriela Belen Martinez-Hernandez, Enrique Jimenez-Ferrer, Manases Gonzalez-Cortazar, Ruben Roman-Ramos, Jaime Tortoriello, Gabriela Vargas-Villa, Maribel Herrera-Ruiz
Summary: Salvia elegans, a plant with biological activities in central nervous system, was studied for its anxiolytic and antidepressant effects. Fractions and compounds isolated from the plant were evaluated in mice, showing that TM and OA have antidepressant and anxiolytic properties and can interact with serotoninergic drugs.
NAUNYN-SCHMIEDEBERGS ARCHIVES OF PHARMACOLOGY
(2021)
Article
Endocrinology & Metabolism
Yane Costa Chaves, Karina Genaro, Jose Alexandre Crippa, Joice Maria da Cunha, Janaina Menezes Zanoveli
Summary: The study demonstrates that CBD has antidepressant and anxiolytic effects on type-1 diabetes animals, with involvement of 5-HT1A, CB1, and CB2 receptors in mediating these effects. Furthermore, CB2 receptor plays a role in the glycemic control effect of CBD in diabetic animals.
METABOLIC BRAIN DISEASE
(2021)
Article
Multidisciplinary Sciences
Harini Sri Rethinavel, Divya Bharathi Selvaraj, Sathya Jeevitha Balakrishnan, Jemi Feiona Vergil Andrews, Jerly Helan Mary Joseph, Mahesh Kandasamy
Summary: Omeprazole treatment alleviates anxiety-like behaviors in a cysteamine HCl induced mouse model of gastrointestinal disorder, supporting its anxiolytic properties. However, adverse effects associated with inappropriate intake of omeprazole may exist, necessitating further research on its long-term effects on brain function.
Article
Integrative & Complementary Medicine
Vasudevan Mani, Sultan Sajid, Syed Imam Rabbani, Abdulrahman Saud Alqasir, Hani Abdullah Alharbi, Abdullah Alshumaym
Summary: The ethanol extract of Terminalia chebula fruit exhibited antidepressant-like and anxiolytic-like effects in mice, reducing immobility time, increasing swimming time, and improving behaviors in various behavioral tests, as well as decreasing MAO-A activity in the brain as shown by the study.
JOURNAL OF TRADITIONAL AND COMPLEMENTARY MEDICINE
(2021)
Article
Chemistry, Medicinal
Grigory Mokrov, Andry Pantileev, Milada Yarkova, Tatiana Gudasheva, Sergei Seredenin
Summary: New TSPO ligands with high anxiolytic activity in the series of N,1-diphenylpyrrolo[1,2-a]pyrazine-3-carboxamides were successfully designed using calculated pharmacophore model and molecular docking analysis.
MEDICINAL CHEMISTRY
(2022)
Review
Chemistry, Medicinal
Grigory V. Mokrov
Summary: Cardiovascular diseases are widespread and continue to grow in modern society, requiring the development of new safe drugs for treatment. Many cardioprotective agents adhere to a common pharmacophore model, suggesting the potential for designing new generation agents with multitarget mechanisms.
ARCHIV DER PHARMAZIE
(2022)
Article
Clinical Neurology
Aliya A. Abdullina, Ekaterina V. Vasileva, Elizabeth A. Kulikova, Vladimir S. Naumenko, Alexandra Plyusnina, Tatyana A. Gudasheva, Georgy Kovalev, Sergei B. Seredenin
Summary: This study found that chronic CPG treatment is effective in reducing depressive-like behaviors, and the antidepressant-like effect is mediated, at least in part, by a BDNF-dependent mechanism. However, CPG does not negatively affect locomotor activity, cognition, or anxiety.
JOURNAL OF PSYCHOPHARMACOLOGY
(2022)
Article
Chemistry, Medicinal
K. N. Kolyasnikova, P. Yu Povarnina, E. A. Kuznetsova, A. G. Alyaeva, T. A. Gudasheva, S. B. Seredenin
Summary: The substituted dipeptide GZK-111 retains its pharmacological effects, including antihypoxic and anxiolytic activities, after oral administration, which is important for its development as a potential drug for treating chronic diseases.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2022)
Article
Chemistry, Medicinal
Armen G. Mezhlumyan, Anna Tallerova, Polina Y. Povarnina, Aleksey Tarasiuk, Nellya M. Sazonova, Tatiana A. Gudasheva, Sergey B. Seredenin
Summary: This study compares the antidepressant effects of different neurotrophin mimetics and identifies GSB-106 as the most promising candidate for developing antidepressant drugs.
Article
Pharmacology & Pharmacy
Sergei Ivanov, Rita U. Ostrovskaya, Ksenia N. Koliasnikova, Irina B. Alchinova, Marina S. Demorzhi, Tatiana A. Gudasheva, Sergei B. Seredenin
Summary: This study models the signs of metabolic syndrome and prediabetes preceding type 2 diabetes using a high-fat diet (HFD). It investigates the effects of a low molecular weight nerve growth factor mimetic, GK-2, on indicators of abdominal obesity, blood glucose level, glucose tolerance, cholesterol and triglyceride levels, as well as the liver structure. The results show that GK-2 can reduce blood glucose, improve glucose tolerance, and lower cholesterol and triglyceride levels. It also mitigates abdominal obesity and eliminates liver abnormalities caused by the high-fat diet.
CLINICAL AND EXPERIMENTAL PHARMACOLOGY AND PHYSIOLOGY
(2022)
Article
Pharmacology & Pharmacy
Polina Y. Y. Povarnina, Tatyana A. A. Antipova, Ilya O. O. Logvinov, Tatiana A. A. Gudasheva, Sergey B. B. Seredenin
Summary: The aim of this study was to investigate the effects of BDNF dipeptide mimetic GSB-106 on depressive-like behavior, cognitive impairments, and hippocampal neuroplasticity in an experimental model of ischemic stroke. The results showed that GSB-106 completely prevented behavior impairments and counteracted the reduction of immunoreactivity to CREB in the hippocampus. Therefore, the BDNF dipeptide mimetic GSB-106 holds promise for the treatment of poststroke neuropsychiatric disorders.
CURRENT PHARMACEUTICAL DESIGN
(2023)
Review
Biochemistry & Molecular Biology
Mikhail V. Voronin, Elena V. Abramova, Ekaterina R. Verbovaya, Yulia V. Vakhitova, Sergei B. Seredenin
Summary: Modern pharmacotherapy of neurodegenerative diseases is primarily symptomatic and ineffective in halting disease progression. Protein misfolding is regarded as a crucial pathogenic factor in these diseases. Chaperones and endoplasmic reticulum stress mechanisms show promise in regulating these processes. This review provides an analysis of the role of BiP and Sigma1R chaperones in Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, and Huntington's disease, and highlights the neuroprotective effect of Sigma1R ligand activation. The interaction between Sigma1R and BiP-associated signaling is also discussed, emphasizing the need for further study in this area.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Medicinal
Grigory V. Mokrov
Summary: A multitarget drug design approach is being developed in medicinal chemistry and pharmacology to target multifactorial diseases. This study focuses on the identification of basic pharmacophore models and the analysis of biological targets for cardioprotective drugs using the biaromatic pharmacophore as an example. It provides insights into the mechanisms of action of these drugs and their potential for treating cardiovascular diseases.
ARCHIV DER PHARMAZIE
(2023)
Article
Biochemistry & Molecular Biology
Mikhail V. Voronin, Stanislav V. Shangin, Svetlana A. Litvinova, Elena V. Abramova, Rustam D. Kurbanov, Inna V. Rybina, Yulia V. Vakhitova, Sergei B. Seredenin
Summary: Previous drug development studies have established two groups of facts about the non-benzodiazepine anxiolytic fabomotizole. Firstly, it prevents the decrease in binding ability of the GABA(A) receptor's benzodiazepine site induced by stress. Secondly, it functions as a Sigma1R chaperone agonist, and its anxiolytic effect is blocked by Sigma1R antagonists. To investigate the involvement of Sigma1R in GABA(A) receptor-dependent pharmacological effects, various experiments were conducted on mice using Sigma1R ligands. The results show that Sigma1R antagonists attenuate while Sigma1R agonists enhance GABA(A) receptor-dependent pharmacological effects.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
