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5-(Sulfamoyl)thien-2-yl 1,3-oxazole inhibitors of carbonic anhydrase II with hydrophilic periphery
Journal of Enzyme Inhibition and Medicinal Chemistry. 2022. Vol. 37. No. 1. P. 1005–1011.
Kalinin S., Kovalenko A., Valtari A., Nocentini A., Maxim Gureev, Urtti A., Korsakov M., Supuran C., Krasavin M.
Hydrophilic derivatives of an earlier described series of carbonic anhydrase inhibitors have been designed, prepared and profiled against a panel of carbonic anhydrase isoforms, including the glaucoma-related hCA II. For all hydrophilic derivatives, computational prediction of intraocular permeability routes showed the predominance of conjunctival rather than corneal absorption. The potentially reactive primary or secondary amine periphery of these compounds makes them suitable candidates for bioconjugation to polymeric drug carriers. As was shown previously, the most active hCA II inhibitor is efficacious in alleviating intraocular pressure in normotensive rabbits with efficacy matching that of dorzolamide.
Language:
English
Springer, 2026.
Two volumes of the SPECOM 2026 proceedings contain a collection of submitted papers presented at SPECOM 2026, which were thoroughly reviewed by members of the Program Committee and additional reviewers consisting of almost 80 experts in the conference topic areas. In total, 65 regular full papers out of 99 submissions made via the EasyChair electronic ...
Added: September 20, 2026
sobov P., Yakushev I., Shestakov A. et al., Organometallics 2025 Vol. 44 No. 24 P. 2873–2881
Interaction of {Cryptand(K+)}(C60•–) with CpCo(CO)2 yields the air-sensitive crystalline salt {Cryptand(K+)}{CpCo(CO)-η2-C60•–} (1), in which C60•– replaces carbonyl group in CpCo(CO)2. Two Co–C bonds of 2.028(9) and 2.057(8)Å are formed. The magnetic moment of 1 is 1.72 μB, indicating a doublet S = 1/2 spin state of {CpCo(CO)-η2-C60•–} at 300 K. The compound shows a broad ...
Added: September 20, 2026
Aleksei Samarin, Alexander Savelev, Aleksei Toropov et al., Pattern Recognition and Image Analysis 2026 Vol. 36 No. 2 P. 323–334
In this paper, an improved approach for automatic wildlife detection in natural environments based on the integration of a neural network architecture with a two-stream attention mechanism and a novel preclassification step based on infrared data has been presented. The proposed method addresses one of the key challenges in environmental monitoring: the need for scalable ...
Added: September 19, 2026
Aleksei Samarin, Nazarenko A., Kotenko E. et al., Proceedings of the ACM on Management of Data, USA 2026 Vol. 4 No. 1 P. 1–28
Modern knowledge and large volumes of data are increasingly encoded within neural networks, making the task of simplifying their structures and reducing the number of parameters especially relevant, both to improve efficiency and to facilitate deployment in resource-constrained environments. This paper presents a novel approach to neural network compression that addresses redundancy at both the ...
Added: September 19, 2026
Aleksei Samarin, Alexander Savelev, Aleksei Toropov et al., Pattern Recognition and Image Analysis 2025 Vol. 35 No. 2 P. 148–158
This paper describes our research on creating classifiers for microbial images (micrococci microscopy images) obtained from pictures of unfixed microscopic scenes. In our work, we propose an AutoML approach based on the automatic generation and analysis of the feature space for constructing the most optimal descriptors of microorganism images for subsequent classification. This makes it ...
Added: September 19, 2026
Aleksei Samarin, Alexander Savelev, Aleksei Toropov et al., Pattern Recognition and Image Analysis 2026 Vol. 36 No. 2 P. 302–312
The lack of annotated microscopic datasets remains a major obstacle to training robust deep learning models for microbial classification. In this paper, a novel data augmentation pipeline that uses visual–linguistic large-scale models to generate synthetic microscopic images of six different bacterial and nonbacterial classes has been proposed. Synthetic samples have gradually been added to the ...
Added: September 19, 2026
Springer, Cham, 2026.
computer vision ...
Added: September 19, 2026
Springer, Cham, 2026.
Added: September 19, 2026
FRUCT Oy, 2024.
Added: September 19, 2026
FRUCT Oy, 2024.
Added: September 19, 2026
FRUCT Oy, 2025.
Added: September 19, 2026
FRUCT Oy, 2026.
Added: September 19, 2026
Aleksei Samarin, Nazarenko A., Kotenko E. et al., Machine Learning and Knowledge Extraction 2026 Vol. 8 No. 8 P. 1–26
This paper presents a novel method for pruning deep neural networks based on the concept of flow, derived from the continuous modeling of signal propagation across layers. We derive flow functions for fully connected, convolutional, and self-attention architectures, and we propose a new iterative pruning algorithm, Iterative Flow-Aware Pruning (IFAP), that leverages these measures to ...
Added: September 19, 2026
Myachin A. L., Procedia Computer Science 2026 Vol. 287 P. 193–200
We extend the static pattern analysis method to the temporal dimension by introducing a six-type trajectory taxonomy that classifies objects according to the frequency and structure of pattern switches over an observation window of T > 8 periods. For each object, a reference pattern is designated as the most frequently occupied group over the observation ...
Added: September 18, 2026
Громов Р. С., Нестеров Р.А., Proceedings of the Institute for System Programming of the RAS 2026 Vol. 38 No. 4 P. 23–44
This paper explores the performance criteria of the newest algorithm for solving the problem of finding shortest paths on a graph from a given vertex – Bounded Multi-Source Shortest Path Algorithm
(BM-SSP). The algorithm was published in 2025 and, as its creators claim, it is asymptotically superior to Dijkstra’s deterministic algorithm. However, in the publication devoted ...
Added: September 18, 2026
Shaitan A., Ke Y., Shutao C. et al., BMC Biology 2026 No. 24 Article 181
Background Therapeutic peptides exert pivotal effects in diverse biological processes, and have attracted significant interest in the field of biomedicine in recent years. However, most existing methods often fail to adequately capture the intricate interactions among amino acid residues and the contextual dependencies within peptide sequences, which hampers the extraction of deep semantic representations and ...
Added: September 18, 2026
Ramos-Soto O., Perez-Zarate E., Ramos-Frutos J. et al., Machine Learning and Knowledge Extraction 2026 Vol. 8 No. 7 Article 173
Added: September 18, 2026
Anton Rogachev, Sysoeva O., Frontiers in Systems Neuroscience 2025 Vol. 19 Article 1658243
Added: September 17, 2026
Rogachev A.O., Sysoeva O. V., Cognitive Systems Research 2024 Vol. 86 Article 101236
Receptive speech is the ability to understand speech addressed to a person. It is a crucial process for a child’s cognitive development. We examine the relationship between receptive speech and neural tracking of natural speech in 52 children aged 3–8 years to infer the neurophysiological mechanisms underlying speech development. We registered a 32-channel electroencephalogram (EEG) ...
Added: September 17, 2026
Кузнецов М. Е., Полякова М., Лукьянович В. et al., ФАНУ "Востокгосплан", 2026.
Обзор международных практик развития робототехники и искусственного интеллекта и оценка возможностей их применения в условиях России, в первую очередь для Дальнего Востока и Арктической зоны РФ ...
Added: September 16, 2026
Sibinčić N., Kalinin S., Sharoyko V. et al., Medicinal Chemistry 2023 Vol. 19 No. 2 P. 193–210
Aims To synthesize novel sulfonamide inhibitors of carbonic anhydrase and develop in vitro prioritization workflow to select compounds for in vivo evaluation. Background Carbonic anhydrase (CA) inhibitors gain significant attention in the context of drug discovery research for glaucoma, hypoxic malignancies and bacterial infections. In previous works, we have successfully used direct sulfochlorination approach to ...
Added: February 1, 2024
Krivovicheva V., Bubyrev A., Kalinin S. et al., ChemMedChem 2023 Vol. 18 No. 10 Article e202200607
A newly introduced diazo reagent, 1-diazo-N,N-bis(4-methoxybenzyl)methanesulfonamide, enables access to a range of azole-based primary sulfonamides via [3+2] cycloaddition followed by protecting group removal. Such compounds are representative of the sulfonamide chemical space highly relevant but hitherto not investigated in the context of inhibition of therapeutically relevant isoforms of carbonic anhydrase enzyme. Using this reagent, three ...
Added: January 26, 2024
Kliuchnikova A., Samokhina N., Ilina I. et al., Proteomics 2016 Vol. 16 No. 13 P. 1938–1946
Twenty-nine human aqueous humor samples from patients with eye diseases such as cataract and glaucoma with and without pseudoexfoliation syndrome were characterized by LC-high resolution MS analysis. In total, 269 protein groups were identified with 1% false discovery rate including 32 groups that were not reported previously for this biological fluid. Since the samples were analyzed individually, but not pooled, 36 proteins were identified ...
Added: March 14, 2018