Results 41 to 50 of about 58,537 (265)

AI‐Based D‐Amino Acid Substitution for Optimizing Antimicrobial Peptides to Treat Multidrug‐Resistant Bacterial Infection

open access: yesAdvanced Science, EarlyView.
This study constructed the first D‐amino acid antimicrobial peptide dataset and developed an AI model for efficient screening of substitution sites, with 80% of candidate peptides showing enhanced activity. The lead peptide dR2‐1 demonstrated potent antimicrobial activity in vitro and in vivo, high stability, and low toxicity.
Yinuo Zhao   +14 more
wiley   +1 more source

Chemical Synthesis of Pseudomonas aeruginosa, Staphylococcus aureus, and Acinetobacter baumannii Capsular Polysaccharide Fragments as Leads for Cross‐Protection

open access: yesAngewandte Chemie, EarlyView.
A total of 16 chemically synthesized capsular polysaccharide (CPS) fragments related to Pseudomonas aeruginosa, Staphylococcus aureus, and Acinetobacter baumannii were analyzed by glycan microarray. Comparative screening revealed three conserved epitopes that act as cross‐protective vaccine lead candidates against multidrug‐resistant (MDR) bacterial ...
Amar Kumar Mishra   +9 more
wiley   +2 more sources

Stereochemical outcomes of C–F activation reactions of benzyl fluoride

open access: yesBeilstein Journal of Organic Chemistry, 2018
In recent years, the highly polar C–F bond has been utilised in activation chemistry despite its low reactivity to traditional nucleophiles, when compared to other C–X halogen bonds.
Neil S. Keddie   +4 more
doaj   +1 more source

Synthesis, Enantiomeric Resolution and Biological Evaluation of HIV Capsid Inhibition Activity for Racemic, (S)- and (R)-PF74

open access: yesMolecules, 2021
PF74 is a capsid-targeting inhibitor of HIV replication that effectively perturbs the highly sensitive viral uncoating process. A lack of information regarding the optical purity (enantiomeric excess) of the single stereogenic centre of PF74 has resulted
Stuart Ruddell   +5 more
doaj   +1 more source

Higher‐Level Structural Classification of Pseudomonas Cyclic Lipopeptides through Their Bioactive Conformation

open access: yesAdvanced Science, EarlyView.
Solution structures of a series of cyclic lipodepsipeptides from Pseudomonas reveal that these specialized metabolites adopt left‐handed alpha helical conformations of only two types, being either ‘stapled’ or ‘catch‐pole’ helix. The particular modular distribution of the biosynthetic gene clusters is found to determine the extent of their conserved ...
Benjámin Kovács   +9 more
wiley   +1 more source

Copper‐Catalyzed Three‐Component Selective 1,4‐Amino Oxygenation of 1,3‐Dienes

open access: yesAngewandte Chemie, EarlyView.
Enclosed is a copper‐catalyzed selective 1,4‐amino oxgenation of 1,3‐dienes with the presence of a strong Brønsted acid. This three‐component transformation offers a novel and powerful approach to construct (E)‐1,4‐allylic amino oxygenated motifs by the simultaneous installation of structurally diverse alkylamines and alcohols directly onto 1,3‐dienes.
Guangshou Feng   +2 more
wiley   +2 more sources

Ipertrofan Revisited—The Proposal of the Complete Stereochemistry of Mepartricin A and B

open access: yesMolecules, 2021
Being a methyl ester of partricin, the mepartricin complex is the active substance of a drug called Ipertrofan (Tricandil), which was proven to be useful in treatment of benign prostatic hyperplasia and chronic nonbacterial prostatitis/chronic pelvic ...
Paweł Szczeblewski   +5 more
doaj   +1 more source

Beyond Traditional RAFT Polymerization: Emerging Strategies and Future Perspectives; A Third Update

open access: yesAdvanced Science, EarlyView.
This review explores recent advances in the past five years for non‐traditional RAFT polymerization, focusing on new activation strategies, sustainable depolymerization, and integration with automated and AI‐driven synthesis. Together, these innovations advance polymer chemistry and reveal how the pieces of the non‐traditional RAFT puzzle are steadily ...
Vianna F. Jafari   +10 more
wiley   +1 more source

Nonheme Fe Enzyme‐Catalyzed Enantiodivergent Nitrogen Migration: Directed Evolution and Computational Study of Isopenicillin N Synthases for Biocatalytic Synthesis of Arylglycines

open access: yesAngewandte Chemie, EarlyView.
Nonheme Fe enzyme isopenicillin N synthase was reprogrammed and evolved as an efficient nitrogen migratase IPNSNim, converting diverse azanyl esters to valuable l‐arylglycines with up to 16 000 TTN and 97:3 e.r. IPNSNim and ACCONim allowed enantiodivergent preparation of both l‐ and d‐arylglycines.
Ken Lin   +7 more
wiley   +2 more sources

Five-membered ring annelation in [2.2]paracyclophanes by aldol condensation

open access: yesBeilstein Journal of Organic Chemistry, 2014
Under basic conditions 4,5,12,13-tetraacetyl[2.2]paracyclophane (9) cyclizes by a double aldol condensation to provide the two aldols 12 and 15 in a 3:7 ratio.
Henning Hopf   +2 more
doaj   +1 more source

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