A general and efficient asymmetric synthesis of cyclic indoline aminals was developed with a high level of 1,3-stereoinduction through a dynamic crystallization-driven condensation. Dehydrogenation of the indoline aminals with potassium permanganate produced the corresponding cyclic indole aminals in high yields and excellent enantioselectivities. This general methodology was successfully applied to the synthesis of a wide variety of chiral cyclic indoline aminals and indole aminals with aromatic and aliphatic functional groups.
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Sci Rep
December 2024
Department of Clinical Laboratory, The Affiliated People's Hospital of Jiangsu University, Zhenjiang, 212002, Jiangsu, China.
Tumor heterogeneity, immune-suppressive microenvironment and the precise killing of tumor cells by drugs are important factors affecting tumor treatment. In this study, we developed environment-responsive drug delivery system (FM@IQ/PST&ZIF-8/DOX) based on ZIF-8 for tumor photothermal/immunotherapy/chemotherapy synergistic therapy. The prepared FM@IQ/PST&ZIF-8/DOX nanoplatfrom not only has highly drug loading capacity for chemotherapeutic drug-doxorubicin, but also erythrocyte membrance modified on their surface can endow their immunity-escaping property and prolong their blood circulation time.
View Article and Find Full Text PDFAdv Respir Med
December 2024
Department of Pediatrics and Adolescent Medicine, Ulm University Medical Center, Ulm University, 89075 Ulm, Germany.
Elexacaftor/Tezacaftor/Ivacaftor (ETI) is a CFTR modulator therapy approved for people with cystic fibrosis (pwCF) who have at least one phe508del mutation. However, its approval in the European Union (EU) for pwCF with non-phe508del mutations is lacking, because data on treatment response in this subgroup are scarce. This retrospective observational study evaluated six pwCF (ages 6 to 66) with responsive CFTR mutations (M1101K, R347P, 2789+5G>A, G551D) undergoing off-label ETI therapy.
View Article and Find Full Text PDFGeorgian Med News
October 2024
2Department of Cardiology, Chapidze Heart Center, Tbilisi, Georgia.
Background: The use of beta-blockers in treating resistant hypertension remains poorly understood. While PATHWAY-2 showed a systolic blood pressure benefit with bisoprolol, further research is needed to evaluate other beta-blockers in terms of the effect of systolic blood pressure, assess diastolic blood pressure effects, and guide management in patients intolerant to CCBs as well.
Objectives: Our study aimed to evaluate the efficacy of Carvedilol (non-selective beta-blocker with alpha-1 blocking function) in the management of resistant hypertension, including in patients intolerant to calcium channel blockers.
Arch Pharm (Weinheim)
January 2025
Endocrinology and Metabolism Research Center, Endocrinology and Metabolism Clinical Sciences Institute, Tehran University of Medical Sciences, Tehran, Iran.
New derivatives 6a-m with benzimidazole-indole-amide scaffold were developed, synthesized, and assessed for potential inhibitory effects on α-glucosidase and acetylcholinesterase (AChE). These compounds were synthesized by various amine derivatives. With the exception of two compounds, the α-glucosidase inhibitory activities of the title derivatives were more than that of the positive control acarbose.
View Article and Find Full Text PDFActa Crystallogr E Crystallogr Commun
October 2024
Department of Organic Chemistry University of Madras, Guindy Campus Chennai-600 025 Tamilnadu India.
Two new phenyl-sulfonyl-indole derivatives, namely, -{[3-bromo-1-(phenyl-sulfon-yl)-1-indol-2-yl]meth-yl}--(4-bromo-3-meth-oxy-phen-yl)benzene-sulfonamide, CHBrNOS, (), and ,-bis-{[3-bromo-1-(phenyl-sulfon-yl)-1-indol-2-yl]meth-yl}benzene-sulfonamide, CHBrNOS, (), reveal the impact of intra-molecular π-π inter-actions of the indole moieties as a factor not only governing the conformation of ,-bis-(1-indol-2-yl)meth-yl)amines, but also significantly influencing the crystal patterns. For , the crystal packing is dominated by C-H⋯π and π-π bonding, with a particular significance of mutual indole-indole inter-actions. In the case of , the mol-ecules adopt short intra-molecular π-π inter-actions between two nearly parallel indole ring systems [with the centroids of their pyrrole rings separated by 3.
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