Microwave-Assisted synthesis and evaluation of antibacterial activity of novel 6-fluoroaryl-[1,2,4]triazolo[1,5-A]pyrimidines

A series of 6-fluoroaryl substituted [1,2,4]triazolo[1,5-A]pyrimidines have been synthesized by using the microwave-Assisted Suzuki cross-coupling reaction from readily available 6-bromo-[1,2,4]triazolo[1,5-A]pyrimidine. The antimicrobial activity of new compounds has been evaluated in vitro against Mycobacterium tuberculosis H37Rv and gram-negative (Neisseria gonorrhoeae ATCC 49226) bacteria. © ARKAT-USA, Inc

Modern methods for acne scar correction. Review

The article presents recent data on the acne scars occurrence frequency, etiopathogenesis and classification. It was conducted the effectiveness analysis of existing methods of atrophic acne scars correction, including chemical peels, dermabrasion, needling, surgical techniques, fillers augmentation, laser and light therapy, objectively were assessed side effects and complications during treatment. It were reviewed indications, advantages and disadvantages of each method. The topicality, efficacy and safety of ablative fractional thermolysis were justified.В статье представлены современные данные о частоте встречаемости, этиопатогенезе и классификации рубцов постакне. Проведен анализ эффективности существующих методик коррекции атрофических рубцов постакне, в том числе с помощью химических пилингов, дермабразии, нидлинга, хирургических техник, аугментации филлерами, лазеро- и светотерапии, дана объективная оценка побочных действий и осложнений в процессе лечения. Рассмотрены показания, преимущества и недостатки каждого метода. Обоснована актуальность, эффективность и безопасность применения аблятивного фракционного термолиза

The Atmospheric Chemistry Suite (ACS) of Three Spectrometers for the ExoMars 2016 Trace Gas Orbiter

The Atmospheric Chemistry Suite (ACS) package is an element of the Russian contribution to the ESA-Roscosmos ExoMars 2016 Trace Gas Orbiter (TGO) mission. ACS consists of three separate infrared spectrometers, sharing common mechanical, electrical, and thermal interfaces. This ensemble of spectrometers has been designed and developed in response to the Trace Gas Orbiter mission objectives that specifically address the requirement of high sensitivity instruments to enable the unambiguous detection of trace gases of potential geophysical or biological interest. For this reason, ACS embarks a set of instruments achieving simultaneously very high accuracy (ppt level), very high resolving power (>10,000) and large spectral coverage (0.7 to 17 μm—the visible to thermal infrared range). The near-infrared (NIR) channel is a versatile spectrometer covering the 0.7–1.6 μm spectral range with a resolving power of ∼20,000. NIR employs the combination of an echelle grating with an AOTF (Acousto-Optical Tunable Filter) as diffraction order selector. This channel will be mainly operated in solar occultation and nadir, and can also perform limb observations. The scientific goals of NIR are the measurements of water vapor, aerosols, and dayside or night side airglows. The mid-infrared (MIR) channel is a cross-dispersion echelle instrument dedicated to solar occultation measurements in the 2.2–4.4 μm range. MIR achieves a resolving power of >50,000. It has been designed to accomplish the most sensitive measurements ever of the trace gases present in the Martian atmosphere. The thermal-infrared channel (TIRVIM) is a 2-inch double pendulum Fourier-transform spectrometer encompassing the spectral range of 1.7–17 μm with apodized resolution varying from 0.2 to 1.3 cm−1. TIRVIM is primarily dedicated to profiling temperature from the surface up to ∼60 km and to monitor aerosol abundance in nadir. TIRVIM also has a limb and solar occultation capability. The technical concept of the instrument, its accommodation on the spacecraft, the optical designs as well as some of the calibrations, and the expected performances for its three channels are described

Synthesis of novel [1,2,4]triazolo[1,5-b][1,2,4,5]tetrazines and investigation of their fungistatic activity

A series of novel [1,2,4]triazolo[1,5-b][1,2,4,5]tetrazines has been synthesized through oxidation reaction of the corresponding 3,6-disubstituted 1,2,4,5-tetrazines bearing amidine fragments. It is shown that the heterocyclic systems obtained can be modified easily at C(3) position in the reactions with aliphatic alcohols and amines. Also, the reactivity of [1,2,4]triazolo[1,5-b][1,2,4,5]tetrazines towards CH-active compounds has been studied. The obtained triazolo[1,5-b]annulated 1,2,4,5-tetrazines proved to be active in micromolar concentrations in vitro against filamentous anthropophilic and zooanthropophilic dermatophyte fungi (Trichophyton, Microsporum and Epidermofiton), which cause skin and its appendages (hair, nails) diseases. © 2022 Korotina et al.; licensee Beilstein-Institut.Ministry of Education and Science of the Russian Federation, Minobrnauka: 075-15-2020-777; Ural Branch, Russian Academy of Sciences, UB RASThis work was supported by the Ministry of Education and Science of the Russian Federation (Agreement No. 075-15-2020-777).Analytical studies were carried out using equipment of the Center for Joint Use “Spectroscopy and Analysis of Organic Compounds”, located in Postovsky Institute of Organic Synthesis of the Ural Branch of the Russian Academy of Sciences. This work was supported by the Ministry of Education and Science of the Russian Federation (Agreement No. 075-15-2020-777)

Infliximab plus methotrexate is superior to methotrexate alone in the treatment of psoriatic arthritis in methotrexate-naive patients: the RESPOND study

Objective: To compare the efficacy and safety of treatment with infliximab plus methotrexate with methotrexate alone in methotrexate-naive patients with active psoriatic arthritis (PsA). Methods: In this open-label study, patients 18 years and older with active PsA who were naive to methotrexate and not receiving disease-modifying therapy (N=115) were randomly assigned (1:1) to receive either infliximab (5 mg/kg) at weeks 0, 2, 6 and 14 plus methotrexate (15 mg/week); or methotrexate (15 mg/week) alone. The primary assessment was American College of Rheumatology (ACR) 20 response at week 16. Secondary outcome measures included psoriasis area and severity index (PASI), disease activity score in 28 joints (DAS28) and dactylitis and enthesitis assessments. Results: At week 16, 86.3% of patients receiving infliximab plus methotrexate and 66.7% of those receiving methotrexate alone achieved an ACR20 response (p<0.02). Of patients whose baseline PASI was 2.5 or greater, 97.1% receiving infliximab plus methotrexate compared with 54.3% receiving methotrexate alone experienced a 75% or greater improvement in PASI (p<0.0001). Improvements in C-reactive protein levels, DAS28 response and remission rates, dactylitis, fatigue and morning stiffness duration were also significantly greater in the group receiving infliximab. In the infliximab plus methotrexate group, 46% (26/57) had treatment-related adverse events (AE) and two patients had serious AE, compared with 24% with AE (13/54) and no serious AE in the methotrexate-alone group. Conclusions: Treatment with infliximab plus methotrexate in methotrexate-naive patients with active PsA demonstrated significantly greater ACR20 response rates and PASI75 improvement compared with methotrexate alone and was generally well tolerated. This trial is registered in the US National Institutes of Health clinicaltrials.gov database, identifier NCT00367237

Development of zinc pyrithione cream

Investigated effect of excipients on the organoleptic properties of cream zinc pyrithione. Cream containing zinc pyrithione and urea is optima] on the skin of patients with atopic dermatitis and psoriasis without exacerbation of the disease.Целью настоящей работы является разработка состава крема, определение концентрации вспомогательных и активных веществ, обеспечивающих увлажняющее, противовоспалительное и смягчающее действие на кожу больных атопическим дерматитом и псориазом в межрецидивный период

ГЕНЕЗИС И СОДЕРЖАНИЕ КАТЕГОРИИ ПРЕДПРИНИМАТЕЛЬСКОЙ ЭКОСИСТЕМЫ

В данной статье представлен подробный анализ зарубежных научных исследований, основанных на понятии "предпринимательская экосистема", и описание ключевых компонентов структуры предпринимательской экосистемы, а также ключевых факторов и принципов эффективного функционирования предпринимательских экосистем. Основная цель данной статьи – раскрыть происхождение понятия "предпринимательская система", определение этого понятия в различных исследованиях, выделить основные особенности предпринимательских экосистем, а также расширить и систематизировать знания данной категории.This article presents a detailed analysis of foreign scientific research based on the concept of "entrepreneurial ecosystem" and description of the key components of the structure of the entrepreneurial ecosystem, as well as the key factors and principles of the effective functioning of entrepreneurial ecosystems. The main purpose of this article is to reveal the origin of the concept of "entrepreneurial system", the definition of this concept in various studies, to highlight the main features of entrepreneurial ecosystems, as well as to expand and systematize the knowledge of this category

Revisiting the emergence of pastoralism in the Altai Mountains through interactions between local hunter-gatherer and Afanasievo communities

The Altai Mountains represent a critical region for the earliest trans-Eurasian dispersals of bovid domesticates. However, settlement data from Altaic hunter-gatherer communities and incoming pastoralists remain rare, which precludes understanding the subsistence transitions and associated cultural dynamics underlying the spread of pastoralism to Inner Asia. Here, we report new radiocarbon dates and analysis of archaeological deposits, suggesting previously unrecognized inter-community interactions in the Altai Mountains. We have launched the Rise of Altai Mountain Pastoralism Project (RAMPP) to examine the emergence of livestock herding in the Russian Altai by focusing on new excavations and biomolecular methods on ancient faunal remains.1. Introduction 2. Ust’-Biyke-I: a key hunter-gatherer site 2.1. Radiocarbon dating 2.2. Mesolithic traditions 2.3. Eneolithic transitions 3. Nizhnyaya Sooru: an Afanasievo settlement revisited 4. Conclusion

Two-coordinate pointing and tracking system for an infrared Fouriertransform spectrometer

We describe a 1-inch aperture pointing system realized with a rope transmission driven by geared stepper motors for operation at the surface of Mars. The system is intended to serve in the Fourier-transform spectrometer to observe both the sun through the atmosphere and the thermal emission of the atmosphere. The scanner covers a full 2π field of view (the upper hemisphere). The accuracy of 0.1 mrad (~21 arcsec) for the sun tracking is achieved using an automatic control system with an IR array sensor (32x32) in the loop. The optics of the pointing system consists of three flat mirrors and a germanium inlet window. The mass of the subsystem does not exceed 0.8 kg. The design accounts for the necessity of dust protection in the Martian environment. The effect of a finite accuracy of the pointing and tracking on the instrument signal to noise ratio is modeled

METHOD OF DETERMINING SHEAR DEFORMATION RESISTANCE OF MATERIALS

FIELD: physics. SUBSTANCE: invention relates to determination of physical and mechanical properties of materials. Method comprises testing samples with cylindrical working part of length l of solid circular cross section with radius r for torsion in one direction. Tests are carried out at constant temperature value of working part of sample θ, and during testing method includes measuring values of swirling angle of sample ϕ, as well as torque values M, under action of which plastic deformation of working part of sample is carried out, at the beginning of test up to arbitrary moment of time t* values of twisting angle are monotonously increased, and starting from moment of time t*, providing condition, where ξu is true strain rate, εu - true degree of deformation, for which value of twisting angle is changed by exponential dependenceИзобретение относится к области определения физико-механических свойств материалов. Сущность: осуществляют испытание образцов с цилиндрической рабочей частью длиной l сплошного круглого сечения радиусом r на кручение в одном направлении. Испытания проводят при поддерживаемом на постоянном уровне значении температуры рабочей части образца θ, а в ходе испытания производят измерение значений угла закручивания образца ϕ, а также значений крутящего момента М, под действием которого осуществляется пластическая деформация рабочей части образца, при этом в начале испытания до произвольного момента времени t* значения угла закручивания монотонно увеличивают, а начиная с момента времени t*, обеспечивают выполнение условия , где ξu - истинная скорость деформации, εu - истинная степень деформации, для чего значения угла закручивания изменяют по экспоненциальной зависимости , где с и k - произвольные коэффициенты, а значения сопротивления деформации сдвига, начиная с того же момента времени t*, определяют по формуле: , где . Технический результат: возможность повысить точность определения значений сопротивления деформации сдвига материалов