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A Friedel-Crafts alkylation of pyrrole was developed to afford the β,γ-unsaturated α-hydroxy esters bearing a quaternary stereogenic center with good enantioselectivities and yields. This protocol represents the first report of 1,2-addition of Friedel-Crafts alkylation of pyrrole to β,γ-unsaturated α-ketoesters.
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http://dx.doi.org/10.1021/acs.joc.7b00159 | DOI Listing |
Arch Pharm (Weinheim)
September 2025
Pharmaceutical Organic Chemistry Department, Faculty of Pharmacy, Assiut University, Assiut, Egypt.
Nitazoxanide (NTZ), an FDA-approved drug, served as the framework for synthesizing 22 new broad-spectrum antimicrobial agents from 4-aminosalicylic acid via protection-deprotection, Staudinger reduction, Clauson-Kaas pyrrole synthesis, and nucleophilic substitution. These compounds were evaluated for antibacterial, antimycobacterial, and antitrypanosomal activities. Several compounds, particularly 10, 11, 13, and 22, surpassed the antibacterial activity of NTZ and its active metabolite tizoxanide (TIZ) against all tested pathogens, with MICs ranging from 1.
View Article and Find Full Text PDFMedicine (Baltimore)
September 2025
Department of Internal Medicine, The First Affiliated Hospital of Guangxi University of Science and Technology, Liuzhou, Guangxi, China.
Coronary artery atherosclerosis (CAA) stands as a prominent etiological contributor to global cardiovascular morbidity and mortality. Its pathogenesis entails intricate interplays among genetic predisposition, environmental factors, and lifestyle determinants. Trace elements, though necessitated in minuscule quantities, have emerged as potential modulators of CAA progression, yet their exact impact remains unclear.
View Article and Find Full Text PDFACS Infect Dis
September 2025
Department of Biochemistry, University of Texas Southwestern Medical Center, Dallas, Texas 75390, United States.
Malaria treatments are compromised by drug resistance, creating an urgent need to discover new drugs. We used a phenotypic high-throughput screening (HTS) platform to identify new antimalarials, uncovering three related pyrrole-, indole-, and indoline-based series with a shared α-azacyclic acetamide core. These compounds showed fast-killing activity on asexual blood-stage parasites, were not cytotoxic, and disrupted parasite intracellular pH and Na regulation similarly to cipargamin (KAE609), a clinically advanced inhibitor of the Na pump (ATP4).
View Article and Find Full Text PDFOrg Lett
September 2025
Graduate School of Science and Engineering, Ehime University, Matsuyama 790-8577, Japan.
A fused octapyrrolylanthracene, representing a nonplanar pyrrole-fused aza-nanographene with two deep gulf-edge regions, was readily synthesized and found to exhibit a ladder-shaped bent structure. Electrochemical studies revealed reversible multielectron oxidation up to four electrons. Stepwise oxidation with AgPF or I afforded a singlet diradical dication and a closed-shell aromatic tetracation.
View Article and Find Full Text PDFMar Biotechnol (NY)
September 2025
Department of Marine Life Science, Jeju National University, Jeju, 63243, South Korea.
This study assessed the optimum dietary vitamin B requirement of Pacific white shrimp, Penaeus vannamei, for growth, feed efficiency, hemocyte counts, innate immunity, and ammonia stress resistance. Semi-purified experimental diets were prepared by adding vitamin B at 0.0, 0.
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