U.S. flag

An official website of the United States government

Dot gov

Official websites use .gov
A .gov website belongs to an official government organization in the United States.

Https

Secure .gov websites use HTTPS
A lock ( ) or https:// means you’ve safely connected to the .gov website. Share sensitive information only on official, secure websites.

PubAg

Main content area

You searched for: Subject "drugs" Remove constraint Subject: "drugs"
Start Over

Search

60,087  Search Results

« Previous | 1 - 20 of 60,087 |
Number of results to display per page

Search Results

1. Oxetan-3-ols as 1,2-bis-Electrophiles in a Brønsted-Acid-Catalyzed Synthesis of 1,4-Dioxanes

Author:
Juan J. Rojas; Elena Torrisi; Maryne A. J. Dubois; Riashat Hossain; Andrew J. P. White; Giovanni Zappia; James J. Mousseau; Chulho Choi; James A. Bull
Source:
Organic letters 2022 v.24 no.12 pp. 2365-2370
ISSN:
1523-7052
Subject:
drugs,   etc   ; diastereoselectivity; glycols;     Show all 3 Subjects
Abstract:
... Annulations that combine diacceptors with bis-nucleophiles are uncommon. Here, we report the synthesis of 1,4-dioxanes from 3-aryloxetan-3-ols, as 1,2-bis-electrophiles and 1,2-diols. Brønsted acid Tf₂NH catalyzes both the selective activation of the oxetanol, to form an oxetane carbocation that reacts with the diol, and intramolecular ring opening of the oxetane. High regio- and diastereoselectiv ...
DOI:
10.1021/acs.orglett.2c00568

2. Testing drug release from medicated contact lenses: The missing link to predict in vivo performance

Author:
Ana F. Pereira-da-Mota; Chau-Minh Phan; Angel Concheiro; Lyndon Jones; Carmen Alvarez-Lorenzo
Source:
Journal of controlled release 2022 v.343 pp. 672-702
ISSN:
0168-3659
Subject:
drugs,   etc   ; eyes; therapeutics;     Show all 3 Subjects
Abstract:
... Contact lenses (CLs) offer a wide variety of advantages as ocular drug-releasing platforms, but the feasibility of medicated CL development is constrained by numerous scientific, technological, and regulatory challenges. One main difficulty is the setting of release rate specifications for each drug, since at present there are no standardized in vitro release models that can appropriately predict ...
DOI:
10.1016/j.jconrel.2022.02.014

3. Controlled directional drug release from poly(ε-caprolactone)/polyethylene oxide/metoprolol tartrate composites with multi-layered structures

Author:
Li Zhang; Qibo Xia; Cong Zhang; Hong Wu; Guiting Liu; Rong Chen; Shaoyun Guo
Source:
Composites 2022 v.157 pp. 106939
ISSN:
1359-835X
Subject:
drugs,   etc   ; epoxides; face; models;     Show all 4 Subjects
Abstract:
... Nowadays, it is a challenge to achieve the controlled directional release of multi-layered dosage forms due to the difficulty of flexible and controllable regulation of the layered structure. Herein, we utilized layer-multiplying co-extrusion (LMCE) technology to construct poly(ε-caprolactone) (PCL)/polyethylene oxide (PEO)/ metoprolol tartrate (MPT) composites with controlled multi-layered struct ...
DOI:
10.1016/j.compositesa.2022.106939

4. Difluoroalkylation of Tertiary Amides and Lactams by an Iridium-Catalyzed Reductive Reformatsky Reaction

Author:
Phillip Biallas; Ken Yamazaki; Darren J. Dixon
Source:
Organic letters 2022 v.24 no.10 pp. 2002-2007
ISSN:
1523-7052
Subject:
drugs,   etc   ; alkylation; lactams; methodology;     Show all 4 Subjects
Abstract:
... An iridium-catalyzed, reductive alkylation of abundant tertiary lactams and amides using 1–2 mol % of Vaska’s complex (IrCl(CO)(PPh₃)₂), tetramethyldisiloxane (TMDS), and difluoro-Reformatsky reagents (BrZnCF₂R) for the general synthesis of medicinally relevant α-difluoroalkylated tertiary amines is described. A broad scope (46 examples), including N-aryl- and N-heteroaryl-substituted lactams, dem ...
DOI:
10.1021/acs.orglett.2c00438

5. Nickel-Catalyzed anti-Markovnikov Hydrodifluoroalkylation of Unactivated Alkenes

Author:
Li-Ming Yin; Meng-Chan Sun; Xiao-Ju Si; Dandan Yang; Mao-Ping Song; Jun-Long Niu
Source:
Organic letters 2022 v.24 no.4 pp. 1083-1087
ISSN:
1523-7052
Subject:
drugs,   etc   ; alkenes; hydrides; regioselectivity;     Show all 4 Subjects
Abstract:
... An efficient Ni-catalyzed hydrodifluoroalkylation of unactivated alkenes with bromodifluoroacetate by using PhSiH₃ as hydride source was developed. The transformation affords aliphatic difluorides with anti-Markovnikov regioselectivity. A wide range of highly remote alkenes, simple alkenes, drug molecules, commercially available CF₂ precursors, and even nonfluorinated substrates are competent in t ...
DOI:
10.1021/acs.orglett.1c04346

6. On the Origin of Rh-Catalyzed Selective Ring-Opening Amidation of Substituted Cyclopropanols to Access β²-Amino Ketones

Author:
Minhan Lee; Joon Heo; Dongwook Kim; Sukbok Chang
Source:
Journal of the American Chemical Society 2022 v.144 no.8 pp. 3667-3675
ISSN:
1520-5126
Subject:
drugs,   etc   ; Americans; journals; ketones;     Show all 4 Subjects
Abstract:
... β²-Amino carbonyls, an α-substituted β-amino scaffold, hold a prominent place in the development of new pharmaceuticals and peptidomimetics. Herein, we report a highly efficient Rh-catalyzed ring-opening amidation of substituted cyclopropanols, which turned out to serve as a linchpin for the selective synthesis of β²-amino ketones to outcompete the formation of β³-isomers. Instead of the generally ...
DOI:
10.1021/jacs.1c12934

7. Social amoebae as a new chassis for drug production

Author:
Vincent Courdavault; Nicolas Papon
Source:
Trends in biotechnology 2022 v.40 no.5 pp. 529-531
ISSN:
0167-7799
Subject:
drugs,   etc   ; Dictyostelium discoideum; biotechnology;     Show all 3 Subjects
Abstract:
... Engineered bacteria and yeasts have progressively emerged in the past decade as convenient cell factories for supplying plant and fungal natural products (NPs). A new study by Reimer et al. provides compelling evidence that the amoeba Dictyostelium discoideum could be also engineered in favor of the production of plant drug precursors. ...
DOI:
10.1016/j.tibtech.2022.02.002

8. Study of the Pauson–Khand reaction in flow over alkynylphenyl vinyl ethers: towards the synthesis of tricyclic multisubstituted benzofurans

Author:
Jorge García-Lacuna; Maialen Alonso; Gema Domínguez; Javier Pérez Castells
Source:
RSC advances 2022 v.12 no.12 pp. 7313-7317
ISSN:
2046-2069
Subject:
drugs,   etc   ; benzofurans; ethers; temperature;     Show all 4 Subjects
Abstract:
... The use of flow methodology allows the use of alkynylphenyl vinyl ethers (benzo-fused 1,7 enynes) as substrates for the intramolecular Pauson–Khand reaction (PKr). Forced temperature and pressure conditions during a short reaction time minimize the substrate decomposition allowing the formation of the PK adduct. Substrates substituted at the internal position of the double bond and with internal t ...
DOI:
10.1039/d2ra01062c

9. Synthesis, α-glucosidase inhibition, α-amylase inhibition, and molecular docking studies of 3,3-di(indolyl)indolin-2-ones

Author:
Mardi Santoso; Li Lin Ong; Nur Pasca Aijijiyah; First Ambar Wati; Azminah Azminah; Rose Malina Annuur; Arif Fadlan; Zaher M.A. Judeh
Source:
Heliyon 2022 v.8 no.3 pp. e09045
ISSN:
2405-8440
Subject:
drugs,   etc   ; acarbose; alpha-amylase;     Show all 3 Subjects
Abstract:
... The synthesized 3,3-di(indolyl)indolin-2-ones 1a-p showed desired higher α-glucosidase inhibitory activities and lower α-amylase inhibitory activities than standard drug acarbose. Particularly, compound 1i showed favorable higher α-glucosidase % inhibition of 67 ± 13 and lower α-amylase % inhibition of 51 ± 4 in comparison to acarbose with % inhibition activities of 19 ± 5 and 90 ± 2, respectively ...
DOI:
10.1016/j.heliyon.2022.e09045

10. Tandem acid-promoted intramolecular azide-hydrazone electrocyclization/hydrolysis approach for the synthesis of N-Aminotetrazoles

Author:
Kseniia Yu Titenkova; Alexander V. Shaferov; Alexander A. Larin; Margarita A. Epishina; Alexander S. Kulikov; Ivan V. Ananyev; Leonid L. Fershtat
Source:
Tetrahedron 2022 v.103 pp. 132563
ISSN:
0040-4020
Subject:
drugs,   etc   ; heterocyclic compounds; hydrolysis;     Show all 3 Subjects
Abstract:
... A general method for the synthesis of a series of previously unknown N-(heteroaryl)- and N-(aryl)aminotetrazoles through the tandem electrocyclization/hydrolysis of azidohydrazones was accomplished. The described protocol was suitable for a wide array of the target N-substituted aminotetrazoles which were prepared in good to high yields under smooth reaction conditions. Importantly, the presented ...
DOI:
10.1016/j.tet.2021.132563

11. A network representation approach for COVID-19 drug recommendation

Author:
Haifeng Liu; Hongfei Lin; Chen Shen; Liang Yang; Yuan Lin; Bo Xu; Zhihao Yang; Jian Wang; Yuanyuan Sun
Source:
Methods 2022 v.198 pp. 3-10
ISSN:
1046-2023
Subject:
drugs,   etc   ; COVID-19 infection; medicine;     Show all 3 Subjects
Abstract:
... The coronavirus disease 2019 (COVID-19) has outbreak since early December 2019, and COVID-19 has caused over 100 million cases and 2 million deaths around the world. After one year of the COVID-19 outbreak, there is no certain and approve medicine against it. Drug repositioning has become one line of scientific research that is being pursued to develop an effective drug. However, due to the lack o ...
DOI:
10.1016/j.ymeth.2021.09.009

12. Boron-Promoted Umpolung Reaction of Sulfonyl Chlorides for the Stereospecific Synthesis of Thioglycosides via Reductive Deoxygenation Coupling Reactions

Author:
Siyu Li; Yujuan Wang; Lei Zhong; Siyu Wang; Zhengli Liu; Yuanwei Dai; Yun He; Zhang Feng
Source:
Organic letters 2022 v.24 no.13 pp. 2463-2468
ISSN:
1523-7052
Subject:
drugs,   etc   ; glycosides; stereoselectivity; stereospecificity; therapeutics;     Show all 5 Subjects
Abstract:
... S-Glycosides have broad biological activities and serve as stable mimics of natural O-glycoside counterparts and thus are of great therapeutic potential. Herein we disclose an efficient method for the stereospecific synthesis of 1-thioglycosides via a boron-promoted reductive deoxygenation coupling reaction from readily accessible sulfonyl chlorides and glycosyl bromides. Our protocol features mil ...
DOI:
10.1021/acs.orglett.2c00353

13. Chiral resolution of DL‐glutamic acid by a chiral additive

Author:
Xin‐hui Zhou; Qing Liu; Hai‐shui Wang
Source:
Journal of chemical technology and biotechnology 2022 v.97 no.5 pp. 1240-1246
ISSN:
0268-2575
Subject:
drugs,   etc   ; arginine; biotechnology; crystallization; phenylalanine;     Show all 5 Subjects
Abstract:
... BACKGROUND: Enantiomerically pure compounds occupy an important position in industrial production of pharmaceuticals, food, chemical engineering, etc. The separation of d and l molecules is an important and challenging task. The ‘tailor‐made’ additive method is a simple and efficient crystallization separation technology. However, according to reports, there is a poor crystal yield when obtaining ...
DOI:
10.1002/jctb.7018

14. Heterogeneous Rate Constant for Amorphous Silica Nanoparticle Adsorption on Phospholipid Monolayers

Author:
Alex Vakurov; Rik Drummond-Brydson; Nicola William; Didem Sanver; Neus Bastús; Oscar H. Moriones; V. Puntes; Andrew L. Nelson
Source:
Langmuir 2022 v.38 no.18 pp. 5372-5380
ISSN:
1520-5827
Subject:
drugs,   etc   ; adsorption; cytotoxicity; phosphatidylcholines; silica;     Show all 5 Subjects
Abstract:
... The interaction of amorphous silica nanoparticles with phospholipid monolayers and bilayers has received a great deal of interest in recent years and is of importance for assessing potential cellular toxicity of such species, whether natural or synthesized for the purpose of nanomedical drug delivery and other applications. This present communication studies the rate of silica nanoparticle adsorpt ...
DOI:
10.1021/acs.langmuir.1c03155

15. Steric Interaction of Polyglycerol-Functionalized Detonation Nanodiamonds

Author:
Taro Yoshikawa; Ming Liu; Shery L. Y. Chang; Inga C. Kuschnerus; Yuto Makino; Akihiko Tsurui; Tomoaki Mahiko; Masahiro Nishikawa
Source:
Langmuir 2022 v.38 no.2 pp. 661-669
ISSN:
1520-5827
Subject:
drugs,   etc   ; nanodiamonds; transmission electron microscopy;     Show all 3 Subjects
Abstract:
... Detonation nanodiamonds have found numerous potential applications in a diverse array of fields such as biomedical imaging and drug delivery. Here, we systematically characterized non-functionalized and polyglycerol-functionalized detonation nanodiamond particles (DNPs) dispersed in aqueous suspensions at different ionic strengths (∼1.0 × 10–⁷ to 1.0 × 10–² M) via dynamic light scattering and cryo ...
DOI:
10.1021/acs.langmuir.1c02283

16. SyntaLinker-Hybrid: A deep learning approach for target specific drug design

Author:
Yu Feng; Yuyao Yang; Wenbin Deng; Hongming Chen; Ting Ran
Source:
Artificial intelligence in the life sciences 2022 v.2 pp. 100035
ISSN:
2667-3185
Subject:
drugs,   etc   ; artificial intelligence; drug design;     Show all 3 Subjects
Abstract:
... Target specific drug design has attracted much attention in drug discovery. But, it is a great challenge to efficiently explore the target-focused chemical space. Fragment-based drug design (FBDD) has shown its potential to do this thing. In this study, we introduced a deep learning-based fragment linking method, namely SyntaLinker-Hybrid, for target specific molecular generation. By carrying out ...
DOI:
10.1016/j.ailsci.2022.100035

17. Tannic acid: a crosslinker leading to versatile functional polymeric networks: a review

Author:
Chen Chen; Hao Yang; Xiao Yang; Qinghai Ma
Source:
RSC advances 2022 v.12 no.13 pp. 7689-7711
ISSN:
2046-2069
Subject:
drugs,   etc   ; crosslinking; polymers; polyphenols; tannins;     Show all 5 Subjects
Abstract:
... With the thriving of mussel-inspired polyphenol chemistry as well as the demand for low-cost analogues to polydopamine in adhesive design, tannic acid has gradually become a research focus because of its wide availability, health benefits and special chemical properties. As a natural building block, tannic acid could be used as a crosslinker either supramolecularly or chemically, ensuring versatil ...
DOI:
10.1039/d1ra07657d

18. Cp*Rh(III)-Catalyzed Regioselective C(sp²)–H Mono- and Dialkynylation of Thioamides by Sulfur Coordination

Author:
Lin Ma; Xiaohui Zhang; Yanyan Tuo; Qing-Zhong Zheng
Source:
Journal of organic chemistry 2022 v.87 no.5 pp. 3691-3700
ISSN:
1520-6904
Subject:
drugs,   etc   ; organic chemistry; regioselectivity; sulfur; thioamides;     Show all 5 Subjects
Abstract:
... An efficient Cp*Rh(III)-catalyzed regioselective C(sp²)–H mono- and dialkynylation of thioamides was described. This reaction was performed under mild conditions in high yields (up to 98%) with a broad substrate scope. Significantly, the versatility of this method was further demonstrated by controlled mono- and dialkynylation. Application of this protocol in the late stage functionalization of tw ...
DOI:
10.1021/acs.joc.1c02622

19. Engaging scientists in a sustainability culture

Author:
Louis J. Diorazio; Alex Mullen
Source:
Current research in green and sustainable chemistry 2022 v.5 pp. 100247
ISSN:
2666-0865
Subject:
drugs,   etc   ; green chemistry; objectives; research; scientists;     Show all 5 Subjects
Abstract:
... Any improvement activity requires the means to assess progress towards the intended goal. Herein, we report how the use of simple metrics has supported the adoption of a more sustainable approach to drug substance processing across AstraZeneca. We describe our journey to this point and highlight some of the key factors behind this culture shift. ...
DOI:
10.1016/j.crgsc.2021.100247

20. Ethyl cellulose-chitosan complex particles stabilized W/O Pickering emulsion as a recyclable bio-catalytic microreactor

Author:
Xin-Hao Yu; Fu-Zhen Zhou; Yong-Kang Xi; Xiao-Nan Huang; Shou-Wei Yin; Xiao-Quan Yang
Source:
Colloids and surfaces 2022 v.639 pp. 128375
ISSN:
0927-7757
Subject:
drugs,   etc   ; carboxylic ester hydrolases; emulsions; encapsulation;     Show all 4 Subjects
Abstract:
... Water-in-oil (W/O) emulsions have numerous applications in many industries like foods, pharmaceuticals, in particular biphasic bio-catalysis. However, most of them are stabilized by surfactants or synthetic particles, which lead to limited uses in foods. Here, a W/O type Pickering emulsion was successfully prepared firstly by ordered ethyl cellulose-chitosan complex particles (ECCPs) and used for ...
DOI:
10.1016/j.colsurfa.2022.128375