T 86 Triazaverin prophylactic efficacy against influenza virus A (H5N1) [Электронный ресурс] / S. Ya. Loginova, S. V. Borisevich, B. A. Maksimov, V. P. Bondarev, S. K. Kotovskaya, V. L. Rusinov, V. N. Charushin, O. N. Chupakhin // Antibiotiki i Khimioterapiya . - 2010. - Vol.55, №9-10. - P25-28 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANTIVIRAL EFFICACY -- INFLUENZA VIRUS A -- PROPHYLAXIS Аннотация: The experimental study of the prophylactic efficacy of Triazaverin against the experimental form of the influenza virus A (H5N1) on albino mice intranasally infected with the influenza virus A/Chicken/Kurgan/Russia/02/05 vs. the reference drugs Tamiflu ®, Remantadin and Arbidol ® showed that in doses of 1 to 100 mg/kg it was efficient in the animal protection from death. The drug was also efficient in the urgent prophylaxis. Triazaverin effectively inhibited the influenza A virus multiplication in the lungs of the albino mice |
A 62 Antiviral properties, metabolism, and pharmacokinetics of a novel azolo-1,2,4-triazine-derived inhibitor of influenza A and B virus replication [Электронный ресурс] / I. L. Karpenko, S. L. Deev, O. I. Kiselev, V. N. Charushin, V. L. Rusinov, E. N. Ulomskii, E. G. Deeva, M. K. Kukhanova // Antimicrobial Agents and Chemotherapy . - 2010. - Vol.54, №5. - P2017-2022 Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANIMAL CELL -- ANIMAL EXPERIMENT -- ANTIVIRAL ACTIVITY Аннотация: Influenza viruses of types A and B cause periodic pandemics in the human population. The antiviral drugs approved to combat influenza virus infections are currently limited. We have investigated an effective novel inhibitor of human influenza A and B viruses, triazavirine {2-methylthio-6-nitro-1,2,4- triazolo[5,1-c]-1,2,4-triazine-7(4Í)-one} (TZV). TZV suppressed the replication of influenza virus in cell culture and in chicken chorioallantoic membranes, and it protected mice from death caused by type A and B influenza viruses. TZV was also effective against a rimantadine-resistant influenza virus strain and against avian influenza A virus H5N1 strains. The pharmacokinetic parameters and bioavailability of TZV were calculated after the administration of TZV to rabbits. The TZV metabolite AMTZV {2-methylthio-6-amino-1,2,4- triazolo[5,1-s]-1,2,4-triazin(e)-7(4Í)-one} was discovered inÍÅK 293T and Huh7 cell cultures, a liver homogenate, and rabbit blood after intragastric administration of TZV. AMTZV was nontoxic and inactive as an inhibitor of influenza virus in cell culture. Most likely, this metabolite is a product of TZV elimination |
T 44 The antiaggregant action of 2-morpholino-5-(thienyl-2)-6-H-1,3,4-thiadiazine in in vitro and ex vivo experiments [Electronic resource] / I. S. Loginova, V. A. Makarov, O. N. Chupakhin, L. P. Sidorova, N. M. Perova, V. L. Rusinov // Eksperimental'naia i klinicheskaia farmakologiia . - 2013. - Vol.76, №2. - С. 13-16. - Библиогр.: с. Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): ANIMAL -- BLOOD CLOTTING -- CYTOLOGY Аннотация: The influence of 2-morpholino-5-(thienyl-2)-6-H-1,3,4-thiadiazine (H-29) on the platelet aggregation has been studied in experiments on donor plasma in vitro. It is established that H-29 causes a decrease in the platelet interaction induced by ADP and arachidonic acid. The influence of H-29 on platelet aggregation was also studied in ex vivo experiments with intravenous and oral administration, and some parameters of plasmatic hemostasis were evaluated |
T 44 The correctional modification of inflammatory response at the experimental acute pancreatitis / A. Sarapultsev, O. N. Chupakhin, M. Rantsev, P. Sarapultsev, I. Danilova, S. Medvedeva, L. P. Sidorova // Advances in Bioscience and Biotechnology. - 2012. - Vol.3, №4A. - С. 442-448. - Bibliogr.: p. 447-448 (26 ref.) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): L-17 COMPOUND -- EXPERIMENTAL mODEL -- INFLAMMATION Аннотация: This study investigated the effects of the L-17 compound of the group of substituted 5R1, 6H2-1,3,4- thiadiazine-2-amines on the possibility of inflammatory reaction evolvement correction in experimental acute pancreatitis. The study was based upon recent clinical and experimental work which demonstrated the role of local and systemic inflammatory reactions in pancreatonecrosis. Pancreatonecrosis modeling in rats was performed in accordance with the author’s modification of ligation model of acute pancreatitis. The biochemical and hematological analysis were performed in all groups at day 1. For microscopic analysis, five histological slices of each animal were analyzed. The main group, consisting of 15 animals with the average body weight 223 g each, got intraperitoneal injection of L-17 compound, dozed 40 mg/kg in an hour after surgery of pancreatitis formation. Later on, a 40 mg/kg doze of L-17 compound was repeatedly injected as often as once every 24 hours. Already during the 1st day of the experiment, no leucopenia was observed and the signs of proliferative inflammation were detected. Later, at the background of L-17 compound introduction (5th day of the experiment) the necrosis area got surrounded by demarcation bank, and further on (by the 7th day) had been entirely replaced by granulation tissue. Thus, the application of L-17 compound in experimental acute pan-creatitis results in replacement of destructive purulent inflammation by exudative-proliferative one, prevents lympho- and monocytopenia development, minimizes amylase and pancreatic ferments level during the first day of development of the disease and cuts down the lethality rate as result of pancreatonecrosis complications tw |
T 44 The impact of immunomodulator compound from the group of substituted thiadiazines on the course of stress reaction [Electronic resource] / P. Sarapultsev, O. N. Chupakhin, S. Medvedeva, E. A. Mukhlynina, S. A. Brilliant, L. P. Sidorova, I. Danilova, A. Sarapultsev // International Immunopharmacology. - 2015. - Vol. 25, № 2. - С. 440-449. - Bibliogr. : p. 447-449 (101 ref) Рубрики: ХИМИЧЕСКИЕ НАУКИ Кл.слова (ненормированные): STRESS -- THIADIAZINES -- L-17 COMPOUND Аннотация: A significant role of the stress response to many different diseases prompted a search for new specialized and non-specialized anti-stress agents. This study examines the effect of the compound L17 from the group of 5-phenyl substituted-6H-1,3,4-thiadiazine-2-amines, on the manifestations of the stress response. The authors used a standard model of immobilization stress, in which an animal was immobilized on its back for 6 ha day. Parameters of the morphological and functional states of the organs studied were measured and biochemical and enzyme-immunoassays were carried out on the first and second days. This study reveals that the main mechanism by which the L17 compound mediates of its anti-stress was by activation of macrophages on the second day of the experiments and the inhibition of apoptosis in the thymus. The results enable us to suggest that the compound L17 does not improve resistance to stress; however, it does lower the reaction to stress. \\\\expert2\\nbo\\International Immunopharmacology\\2015. V. 25, N 2. P. 440-449.pdf |
Pyrrolylquinoxaline-2-one derivative as a potent therapeutic factor for brain trauma rehabilitation / E. A. Dutysheva, M. A. Mikeladze, N. D. Aksenov [и др.] // Pharmaceutics. - 2020. - Vol. 12, № 5. - С. 414 Кл.слова (ненормированные): APOPTOSIS -- CEREBROSPINAL FLUID -- HSP70 -- SMALL MOLECULE -- TRAUMATIC BRAIN INJURY Аннотация: Traumatic brain injury (TBI) often causes massive brain cell death accompanied by the accumulation of toxic factors in interstitial and cerebrospinal fluids. The persistence of the damaged brain area is not transient and may occur within days and weeks. Chaperone Hsp70 is known for its cytoprotective and antiapoptotic activity, and thus, a therapeutic approach based on chemically induced Hsp70 expression may become a promising approach to lower post-traumatic complications. To simulate the processes of secondary damage, we used an animal model of TBI and a cell model based on the cultivation of target cells in the presence of cerebrospinal fluid (CSF) from injured rats. Here we present a novel low molecular weight substance, PQ-29, which induces the synthesis of Hsp70 and empowers the resistance of rat C6 glioma cells to the cytotoxic effect of rat cerebrospinal fluid taken from rats subjected to TBI. In an animal model of TBI, PQ-29 elevated the Hsp70 level in brain cells and significantly slowed the process of the apoptosis in acceptor cells in response to cerebrospinal fluid action. The compound was also shown to rescue the motor function of traumatized rats, thus proving its potential application in rehabilitation therapy after TBI. |
Pharmacological characterization of a novel putative nootropic beta-alanine derivative, MB-005, in adult zebrafish / T. O. Kolesnikova, K. A. Demin, A. V. Kalueff [et al.] // Journal of Psychopharmacology. - 2022. - Vol. 36, № 7. - P779-902 Рубрики: ХИМИЧЕСКИЕ НАУКИ Аннотация: Cognitive deficits represent an urgent biomedical problem, and are commonly reduced by nootropic drugs. Animal models, including both rodents and zebrafish, offer a valuable tool for studying cognitive phenotypes and screening novel nootropics. Beta-alanine and its derivatives have recently been proposed to exert nootropic activity. |
Antiviral properties of verdazyls and leucoverdazyls and their activity against group b enteroviruses / A. S. Volobueva, V. V. Zarubaev, T. G. Fedorchenko [et al.] // Russian journal of infection and immunity. - 2023. - Vol. 13, № 1. - P107-118 Рубрики: ХИМИЧЕСКИЕ НАУКИ ЗДРАВООХРАНЕНИЕ. МЕДИЦИНСКИЕ НАУКИ Кл.слова (ненормированные): ENTEROVIRUSES -- ENTEROVIRAL INFECTION -- COXSACKIEVIRUS Аннотация: Enteroviruses are non-enveloped viruses of Enterovirus genus, Picornaviridae family, causing a variety of human diseases: from acute respiratory and intestinal infections to more severe pathologies including poliomyelitis, encephalitis, myocarditis, pancreatitis. Currently, no approved direct-acting antiviral drugs for treatment of enterovirus infections exists, whereas vaccination is available only for prevention of poliomyelitis and enterovirus 71 infection. Therefore, it is promising to conduct a search for inhibitors of enteroviruses life cycle in drug development to treat enterovirus infections. Here, antiviral properties of stable free radicals, verdazyls, and their precursors, leucoverdazyls, were investigated. It has been shown that leucoverdazyls vs verdazyls increased the survival of permissive cell culture infected with coxsackievirus. The activity range of the lead leucoverdazyl against RNA-containing and DNA-containing human viruses (in the viral yield reduction assay) and its proposed mechanism of action (time of addition assay) was studied. The lead compound suppressed reproduction of group B enteroviruses in vitro, with modest activity against influenza A virus and no activity against herpes virus type 1 and adenovirus type 5. The maximum decrease in viral titers was observed upon its addition to infected cells during early and middle stages of the virus life cycle. Thus, we concluded that the studied compound has a pronounced inhibitory activity against group B enteroviruses not belonging to the class of capsid binder inhibitors, without virucidal properties. Previously, we described antioxidant properties of leucoverdazyls. It is known that many viral infections are accompanied by production of reactive oxygen species and oxidative stress, and some compounds with antioxidant properties exhibit antiviral potential. Targeted chemical modifications of leucoverdazyls and further studies of leucoverdazyl mechanism of action as well as in vivo animal studies are needed. However, the results obtained may be useful for future development of new antiviral drugs to treat enteroviral infections. |