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A NOVEL CLASS of ANTIVIRAL COMPOUNDS with POTENT ACTIVITY AGAINST SARS-CoV-2

Gordon, D. E.; Stavtsev, E.; Demchenko, A..

Topics in Antiviral Medicine ; 30(1 SUPPL):182, 2022.

Article in English | EMBASE | ID: covidwho-1880287

ABSTRACT

Background: The SARS-CoV-2 pandemic has sickened over 245 million people, and has killed more than 5 million worldwide. Recent data proves that vaccinations are highly effective in preventing Covid-19 disease, however antigenic drift and other functional mutations in the virus genome reduce the efficacy of vaccines, indicating that the development of antiviral treatments remain a crucial priority. We report potent antiviral activity against SARS-CoV-2 for a promising, novel class of nitrogen-based heterocyclic compounds. Methods: 232 compounds based on the same class of nitrogen-based hetereocyclic molecules were synthesized to final purity of greater than 99%. This library was screened for antiviral phenotypes in a cytopathic effect (CPE) assay using VeroE6 cells and the SARS-CoV-2 WA1 isolate. Based on the results of the WA1 CPE screen, 47 lead candidates were structurally analyzed, and this information was utilized to design 56 additional compounds. A second antiviral CPE-based screen was performed using these 103 candidates in VeroE6 cells with the SARS-CoV-2 delta variant. Antiviral assays studying SARS-CoV-1 (Urbani) and MERS-CoV were performed in Vero 76 cells utilizing a Neutral Red cytopathic effect assay. Results: Within the same class of structurally related small molecules, we tested an initial set of 232 compounds using a CPE-based assay with VeroE6 cells and the USA/WA1 SARS-CoV-2 isolate. Of the compounds tested, 124 demonstrated potency 10 to 540-times higher than a Remdesivir control tested in parallel. Importantly, we observed no detectable toxicity for the vast majority of these compounds when tested up to a concentration of 30 μ M. The lead candidate in this screen displayed an IC50 of 0.02 μ M and a selectivity index of >1,500. Based on structural analysis of an initial 47 lead candidates, we synthesized 56 new molecules, and tested all 103 in a CPE-based assay using the delta variant, also observing efficacy against this variant of concern. Examples of this same class of compounds also display antiviral activity against SARS-CoV-1 (Urbani) and MERS-CoV in cell-based assays. Conclusion: We have identified a novel class of antiviral compounds with potent activity against SARS-CoV-2. High potency against both the early WA1 isolate and the more recent delta variant, as well as efficacy against SARS-CoV-1 and MERS-CoV, suggest that this class of antiviral compounds has pan-Coronavirus antiviral activity.

International register “dynamics analysis of comorbidities in sars-cov-2 survivors” (Aktiv sars-cov-2): Analysis of predictors of short-term adverse outcomes in covid-19

Arutyunov, G. P.; Tarlovskaya, E. I.; Arutyunov, A. G.; Belenkov, Y. N.; Konradi, A. O.; Lopatin, Y. M.; Rebrov, A. P.; Tereshchenko, S. N.; Chesnikova, A. I.; Hayrapetyan, H. G.; Babin, A. P.; Bakulin, I. G.; Bakulina, N. V.; Balykova, L. A.; Blagonravova, A. S.; Boldina, M. V.; Vaisberg, A. R.; Galyavich, A. S.; Gomonova, V. V.; Grigorieva, N. U.; Gubareva, I. V.; Demko, I. V.; Evzerikhina, A. V.; Zharkov, A. V.; Kamilova, U. K.; Kim, Z. F.; Kuznetsova, T. Yu, Lareva, N. V.; Makarova, E. V.; Malchikova, S. V.; Nedogoda, S. V.; Petrova, M. M.; Pochinka, I. G.; Protasov, K. V.; Protsenko, D. N.; Ruzanov, D. Yu, Sayganov, S. A.; Sarybaev, A. Sh, Selezneva, N. M.; Sugraliev, A. B.; Fomin, I. V.; Khlynova, O. V.; Chizhova, O. Yu, Shaposhnik, I. I.; Sсhukarev, D. A.; Abdrahmanova, A. K.; Avetisian, S. A.; Avoyan, H. G.; Azarian, K. K.; Aimakhanova, G. T.; Ayipova, D. A.; Akunov, A. Ch, Alieva, M. K.; Aparkina, A. V.; Aruslanova, O. R.; Ashina, E. Yu, Badina, O. Y.; Barisheva, O. Yu, Batchayeva, A. S.; Bitieva, A. M.; Bikhteyev, I. U.; Borodulina, N. A.; Bragin, M. V.; Budu, A. M.; Burygina, L. A.; Bykova, G. A.; Varlamova, D. D.; Vezikova, N. N.; Verbitskaya, E. A.; Vilkova, O. E.; Vinnikova, E. A.; Vustina, V. V.; Gаlova, E. A.; Genkel, V. V.; Gorshenina, E. I.; Gostishev, R. V.; Grigorieva, E. V.; Gubareva, E. Yu, Dabylova, G. M.; Demchenko, A. I.; Dolgikh, O. Yu, Duvanov, I. A.; Duyshobayev, M. Y.; Evdokimov, D. S.; Egorova, K. E.; Ermilova, A. N.; Zheldybayeva, A. E.; Zarechnova, N. V.; Ivanova, S. Yu, Ivanchenko, E. Yu, Ilina, M. V.; Kazakovtseva, M. V.; Kazymova, E. V.; Kalinina, Y. S.; Kamardina, N. A.; Karachenova, A. M.; Karetnikov, I. A.; Karoli, N. A.; Karpov, O. V.; Karsiev, M. Kh, Кaskaeva, D. S.; Kasymova, K. F.; Kerimbekova, Z. B.; Kerimova, A. Sh, Kim, E. S.; Kiseleva, N. V.; Klimenko, D. A.; Klimova, A. V.; Kovalishena, O. V.; Kolmakova, E. V.; Kolchinskaya, T. P.; Kolyadich, M. I.; Kondriakova, O. V.; Konoval, M. P.; Konstantinov, D. Yu, Konstantinova, E. A.; Kordukova, V. A.; Koroleva, E. V.; Kraposhina, A. Yu, Kriukova, T. V.; Kuznetsova, A. S.; Kuzmina, T. Y.; Kuzmichev, K. V.; Kulchoroeva, C. K.; Kuprina, T. V.; Kouranova, I. M.; Kurenkova, L. V.; Kurchugina, N. Yu, Kushubakova, N. A.; Levankova, V. I.; Levin, M. E.; Lyubavina, N. A.; Magdeyeva, N. A.; Mazalov, K. V.; Majseenko, V. I.; Makarova, A. S.; Maripov, A. M.; Marusina, A. A.; Melnikov, E. S.; Moiseenko, N. B.; Muradova, F. N.; Muradyan, R. G.; Musaelian, S. N.; Nikitina, N. M.; Ogurlieva, B. B.; Odegova, A. A.; Omarova, Y. M.; Omurzakova, N. A.; Ospanova, S. O.; Pahomova, E. V.; Petrov, L. D.; Plastinina, S. S.; Pogrebetskaya, V. A.; Polyakov, D. S.; Ponomarenko, E. V.; Popova, L. L.; Prokofeva, N. A.; Pudova, I. A.; Rakov, N. A.; Rakhimov, A. N.; Rozanova, N. A.; Serikbolkyzy, S.; Simonov, A. A.; Skachkova, V. V.; Smirnova, L. A.; Soloveva, D. V.; Soloveva, I. A.; Sokhova, F. M.; Subbotin, A. K.; Sukhomlinova, I. M.; Sushilova, A. G.; Tagayeva, D. R.; Titojkina, Y. V.; Tikhonova, E. P.; Tokmin, D. S.; Torgunakova, M. S.; Trenogina, K. V.; Trostianetckaia, N. A.; Trofimov, D. A.; Tulichev, A. A.; Tupitsin, D. I.; Tursunova, A. T.; Ulanova, N. D.; Fatenkov, O. V.; Fedorishina, O. V.; Fil, T. S.; Fomina, I. Yu, Fominova, I. S.; Frolova, I. A.; Tsvinger, S. M.; Tsoma, V. V.; Cholponbaeva, M. B.; Chudinovskikh, T. I.; Shakhgildyan, L. D.; Shevchenko, O. A.; Sheshina, T. V.; Shishkina, E. A.; Shishkov, K. Yu, Sherbakov, S. Y.; Yausheva, E. A..

Russian Journal of Cardiology ; 26(4):116-131, 2021.

Article in Russian | EMBASE | ID: covidwho-1488885

ABSTRACT

The international AKTIV register presents a detailed description of out-and inpatients with COVID-19 in the Eurasian region. It was found that hospitalized patients had more comorbidities. In addition, these patients were older and there were more men than among outpatients. Among the traditional risk factors, obesity and hypertension had a significant negative effect on prognosis, which was more significant for patients 60 years of age and older. Among comorbidities, CVDs had the maximum negative effect on prognosis, and this effect was more significant for patients 60 years of age and older. Among other comorbidities, type 2 and 1 diabetes, chronic kidney disease, chronic obstructive pulmonary disease, cancer and anemia had a negative impact on the prognosis. This effect was also more significant (with the exception of type 1 diabetes) for patients 60 years and older. The death risk in patients with COVID-19 depended on the severity and type of multimorbidity. Clusters of diseases typical for deceased patients were identified and their impact on prognosis was determined. The most unfavorable was a cluster of 4 diseases, including hypertension, coronary artery disease, heart failure, and diabetes mellitus. The data obtained should be taken into account when planning measures for prevention (vaccination priority groups), treatment and rehabilitation of COVID-19 survivors.

International register “dynamics analysis of comorbidities in sars-cov-2 survivors” (Aktiv) and the register “analysis of hospitalizations of comorbid patients infected during the second wave of sars-cov-2 outbreak” (aktiv 2)

Arutyunov, G. P.; Tarlovskaya, E. I.; Arutyunov, A. G.; Belenkov, Y. N.; Konradi, A. O.; Lopatin, Y. M.; Rebrov, A. P.; Tereshchenko, S. N.; Che Snikova, A. I.; Hayrapetyan, H. G.; Babin, A. P.; Bakulin, I. G.; Bakulina, N. V.; Balykova, L. A.; Blagonravova, A. S.; Boldina, M. V.; Vaisberg, A. R.; Galyavich, A. S.; Gomonova, V. V.; Grigorieva, N. U.; Gubareva, I. V.; Demko, I. V.; Evzerikhina, A. V.; Zharkov, A. V.; Kamilova, U. K.; Kim, Z. F.; Kuznetsova, T. Yu, Lareva, N. V.; Makarova, E. V.; Malchikova, S. V.; Nedogoda, S. V.; Petrova, M. M.; Pochinka, I. G.; Protasov, K. V.; Protsenko, D. N.; Ruzanov, D. Yu, Sayganov, S. A.; Sarybaev, A. Sh, Selezneva, N. M.; Sugraliev, A. B.; Fomin, I. V.; Khlynova, O. V.; Chizhova, O. Yu, Shaposhnik, I. I.; Sсhukarev, D. A.; Abdrahmanova, A. K.; Avetisian, S. A.; Avoyan, H. G.; Azarian, K. K.; Aimakhanova, G. T.; Ayipova, D. A.; Akunov, A. Ch, Alieva, M. K.; Aparkina, A. V.; Aruslanova, O. R.; Ashina, E. Yu, Badina, O. Y.; Barisheva, O. Yu, Batchayeva, A. S.; Bitieva, A. M.; Bikhteyev, I. U.; Borodulina, N. A.; Bragin, M. V.; Budu, A. M.; Burygina, L. A.; Bykova, G. A.; Varlamova, D. D.; Vezikova, N. N.; Ver Bitskaya, E. A.; Vilkova, O. E.; Vinnikova, E. A.; Vustina, V. V.; Gаlova, E. A.; Genkel, V. V.; Gorshenina, E. I.; Gostishev, R. V.; Grigorieva, E. V.; Gubareva, E. Yu, Dabylova, G. M.; Demchenko, A. I.; Dolgikh, O. Yu, Duvanov, I. A.; Duyshobayev, M. Y.; Evdokimov, D. S.; Egorova, K. E.; Ermilova, A. N.; Zheldybayeva, A. E.; Zarechnova, N. V.; Ivanova, S. Yu, Ivanchenko, E. Yu, Ilina, M. V.; Kazakovtseva, M. V.; Kazymova, E. V.; Kalinina, Yu S.; Kamardina, N. A.; Karachenova, A. M.; Karetnikov, I. A.; Karoli, N. A.; Karpov, O. V.; Karsiev, M. Kh, Кaskaeva, D. S.; Kasymova, K. F.; Kerimbekova, Zh B.; Kerimova, A. Sh, Kim, E. S.; Kiseleva, N. V.; Klimenko, D. A.; Klimova, A. V.; Kovalishena, O. V.; Kolmakova, E. V.; Kolchinskaya, T. P.; Kolyadich, M. I.; Kondriakova, O. V.; Konoval, M. P.; Konstantinov, D. Yu, Konstantinova, E. A.; Kordukova, V. A.; Koroleva, E. V.; Kraposhina, A. Yu, Kriukova, T. V.; Kuznetsova, A. S.; Kuzmina, T. Y.; Kuzmichev, K. V.; Kulchoroeva, Ch K.; Kuprina, T. V.; Kouranova, I. M.; Kurenkova, L. V.; Kurchugina, N. Yu, Kushubakova, N. A.; Levankova, V. I.; Levin, M. E.; Lyubavina, N. A.; Magdeyeva, N. A.; Mazalov, K. V.; Majseenko, V. I.; Makarova, A. S.; Maripov, A. M.; Marusina, A. A.; Melnikov, E. S.; Moiseenko, N. B.; Muradova, F. N.; Muradyan, R. G.; Musaelian, Sh N.; Nikitina, N. M.; Ogurlieva, B. B.; Odegova, A. A.; Omarova, Yu M.; Omurzakova, N. A.; Ospanova, Sh O.; Pahomova, E. V.; Petrov, L. D.; Plastinina, S. S.; Pogrebetskaya, V. A.; Polyakov, D. S.; Ponomarenko, E. V.; Popova, L. L.; Prokofeva, N. A.; Pudova, I. A.; Rakov, N. A.; Rakhimov, A. N.; Rozanova, N. A.; Serikbolkyzy, S.; Simonov, A. A.; Skachkova, V. V.; Smirnova, L. A.; Soloveva, D. V.; Soloveva, I. A.; Sokhova, F. M.; Subbotin, A. K.; Sukhomlinova, I. M.; Sushilova, A. G.; Tagayeva, D. R.; Titojkina, Y. V.; Tikhonova, E. P.; Tokmin, D. S.; Torgunakova, M. S.; Trenogina, K. V.; Trostianetckaia, N. A.; Trofimov, D. A.; Tulichev, A. A.; Tupitsin, D. I.; Tursunova, A. T.; Tiurin, A. A.; Ulanova, N. D.; Fatenkov, O. V.; Fedorishina, O. V.; Fil, T. S.; Fomina, I. Yu, Fominova, I. S.; Frolova, I. A.; Tsvinger, S. M.; Tsoma, V. V.; Cholponbaeva, M. B.; Chudinovskikh, T. I.; Shakhgildyan, L. D.; Shevchenko, O. A.; Sheshina, T. V.; Shishkina, E. A.; Shishkov, K. Yu, Sherbakov, S. Y.; Yausheva, E. A..

Russian Journal of Cardiology ; 26(3):102-113, 2021.

Article in Russian | EMBASE | ID: covidwho-1488882

ABSTRACT

The organizer of the registers “Dynamics analysis of comorbidities in SARS-CoV-2 survivors” (AKTIV) and “Analysis of hospitalizations of comorbid patients infected during the second wave of SARS-CoV-2 outbreak” (AKTIV 2) is the Eurasian Association of Therapists (EAT). Currently, there are no clinical registries in the Eurasian region designed to collect and analyze information on long-term outcomes of COVID-19 survivors with comorbid conditions. The aim of the register is to assess the impact of a novel coronavirus infection on long-term course of chronic non-communicable diseases 3, 6, 12 months after recovery, as well as to obtain information on the effect of comorbidity on the severity of COVID-19. Analysis of hospitalized patients of a possible second wave is planned for register “AKTIV 2”. To achieve this goal, the register will include men and women over 18 years of age diagnosed with COVID-19 who are treated in a hospital or in outpatient basis. The register includes 25 centers in 5 federal districts of the Russian Federation, centers in the Republic of Armenia, the Republic of Kazakhstan, the Republic of Kyrgyzstan, the Republic of Belarus, the Republic of Moldova, and the Republic of Uzbekistan. The estimated capacity of the register is 5400 patients.

[International register "Analysis of Chronic Non-infectious Diseases Dynamics After COVID-19 Infection in Adult Patients (ACTIV SARS-CoV-2)"]

Arutyunov, G. P.; Tarlovskaya, E. I.; Arutyunov, A. G.; Belenkov, Y. N.; Konradi, A. O.; Lopatin, Y. M.; Tereshchenko, S. N.; Rebrov, A. P.; Chesnikova, A. I.; Fomin, I. V.; Grigorieva, N. U.; Boldina, V. M.; Vaisberg, A. R.; Blagonravova, A. S.; Makarova, E. V.; Shaposhnik, II, Kuznetsova, T. Y.; Malchikova, S. V.; Protsenko, D. N.; Evzerikhina, A. V.; Petrova, M. M.; Demko, I. V.; Saphonov, D. V.; Hayrapetyan, H. G.; Galyavich, A. S.; Kim, Z. F.; Sugraliev, A. B.; Nedogoda, S. V.; Tsoma, V. V.; Sayganov, S. A.; Gomonova, V. V.; Gubareva, I. V.; Sarybaev, A. S.; Ruzanau, D. Y.; Majseenko, V. I.; Babin, A. P.; Kamilova, U. K.; Koroleva, E. V.; Vilkova, O. E.; Fomina, I. Y.; Pudova, I. A.; Soloveva, D. V.; Doshchannikov, D. A.; Kiseleva, N. V.; Zelyaeva, N. V.; Kouranova, I. M.; Pogrebetskaya, V. A.; Muradova, F. N.; Badina, O. Y.; Kovalishena, O. V.; Gsmall a, Cyrilliclova A. E.; Plastinina, S. S.; Grigorovich, M. S.; Lyubavina, N. A.; Vezikova, N. N.; Levankova, V. I.; Ivanova, S. Y.; Ermilova, A. N.; Muradyan, R. G.; Gostishev, R. V.; Tikhonova, E. P.; Kuzmina, T. Y.; Soloveva, I. A.; Kraposhina, A. Y.; Kolyadich, M. I.; Kolchinskaya, T. P.; Genkel, V. V.; Kuznetsova, A. S.; Kazakovtseva, M. V.; Odegova, A. A.; Chudinovskikh, T. I.; Baramzina, S. V.; Rozanova, N. A.; Kerimova, A. S.; Krivosheina, N. A.; Chukhlova, S. Y.; Levchenko, A. A.; Avoyan, H. G.; Azarian, K. K.; Musaelian, S. N.; Avetisian, S. A.; Levin, M. E.; Karpov, O. V.; Sokhova, F. M.; Burygina, L. A.; Sheshina, T. V.; Tiurin, A. A.; Dolgikh, O. Y.; Kazymova, E. V.; Konstantinov, D. Y.; Chumakova, O. A.; Kondriakova, O. V.; Shishkov, K. Y.; Fil, S. T.; Prokofeva, N. A.; Konoval, M. P.; Simonov, A. A.; Bitieva, A. M.; Trostianetckaia, N. A.; Cholponbaeva, M. B.; Kerimbekova, Z. B.; Duyshobayev, M. Y.; Akunov, A. C.; Kushubakova, N. A.; Melnikov, E. S.; Kim, E. S.; Sherbakov, S. Y.; Trofimov, D. A.; Evdokimov, D. S.; Ayipova, D. A.; Duvanov, I. A.; Abdrahmanova, A. K.; Aimakhanova, G. T.; Ospanova, S. O.; Gaukhar, M. D.; Tursunova, A. T.; Kaskaeva, D. S.; Tulichev, A. A.; Ashina, E. Y.; Kordukova, V. A.; Barisheva, O. Y.; Egorova, K. E.; Varlamova, D. D.; Kuprina, T. V.; Pahomova, E. V.; Kurchugina, N. Y.; Frolova, I. A.; Mazalov, K. V.; Subbotin, A. K.; Kamardina, N. A.; Zarechnova, N. V.; Mamutova, E. M.; Smirnova, L. A.; Klimova, A. V.; Shakhgildyan, L. D.; Tokmin, D. S.; Tupitsin, D. I.; Kriukova, T. V.; Polyakov, D. S.; Karoli, N. A.; Grigorieva, E. V.; Magdeyeva, N. A.; Aparkina, A. V.; Nikitina, N. M.; Petrov, L. D.; Budu, A. M.; Rasulova, Z. D.; Tagayeva, D. R.; Fatenkov, O. V.; Gubareva, E. Y.; Demchenko, A. I.; Klimenko, D. A.; Omarova, Y. V.; Serikbolkyzy, S.; Zheldybayeva, A. E..

Kardiologiia ; 60(11):30-34, 2021.

Article in Russian | Scopus | ID: covidwho-1070011

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