Bioorganic and Medicinal Chemistry Letters This is an RSS file. You can use it to subscribe to this data in your favourite RSS reader or to display this data on your own website or blog.

Design of MERS-CoV entry inhibitory short peptides based on helix-stabilizing strategies
Bioorg Med Chem Lett. 2023 Nov 24;97:129569. doi: 10.1016/j.bmcl.2023.129569. Online ahead of print.ABSTRACTInteraction between Middle East respiratory syndrome coronavirus (MERS-CoV) spike (S) protein heptad repeat-1 domain (HR1) and heptad repeat-2 domain (HR2) is critical for the MERS-CoV fusion process. This interaction is mediated by the α-helical region from HR2 and the hydrophobic groove in a central HR1 trimeric coiled coil. We sought to develop a short peptidomimetic to act as a MERS-CoV fusion inhibitor by reproducing the key recognition features of HR2 helix. This was achieved by the use of helix-stabilizing st...
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Jichun Li Qing Li Shuai Xia Jiahuang Tu Longbo Zheng Qian Wang Shibo Jiang Chao Wang Source Type: research

Azetidine ring, salicylic acid, and salicylic acid bioisosteres as determinants of the binding characteristics of novel potent compounds to Stat3
Bioorg Med Chem Lett. 2023 Nov 24:129565. doi: 10.1016/j.bmcl.2023.129565. Online ahead of print.NO ABSTRACTPMID:38008341 | DOI:10.1016/j.bmcl.2023.129565 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Yue Chen Ning Zhai Yinsong Zhu Peibin Yue Nagendra Verma Christine Brotherton-Pleiss Wenzhen Fu Kayo Nakamura Weiliang Chen Joel Kawakami Ramachandran Murali Marcus A Tius Francisco Lopez-Tapia James Turkson Source Type: research

A novel sensitive fluorescent probe with double channels for highly effective recognition of biothiols
Bioorg Med Chem Lett. 2023 Nov 24;97:129563. doi: 10.1016/j.bmcl.2023.129563. Online ahead of print.ABSTRACTBiothiols play a crucial role in maintaining redox balance in organisms, and anomalous levels of biothiols in human organs can lead to various sicknesses and biological disorders. This work developed a novel sensitive fluorescent probe TZ-NBD with double channels for highly efficient recognition of biothiols. TZ-NBD adopts 4-Chloro-7-nitrobenzofurazan (NBD-Cl) as the recognition moiety with simultaneous fluorescence output. By incorporating NBD-Cl with the other fluorophore, benzothiazole dihydrocyclopentachromene de...
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Qiang Fei Keyi Shen Hongxiu Ke Erfei Wang Guorun Fan Feiyi Wang Jun Ren Source Type: research

Characterization of the G-quadruplexes in the Transthyretin Gene and its Role in Silencing Transthyretin mRNA Transcription
This study might shed valuable lights for the development of innovative therapeutic approach against Transthyretin Amyloidosis.PMID:38008337 | DOI:10.1016/j.bmcl.2023.129568 (Source: Bioorganic and Medicinal Chemistry Letters)
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Peimin Huang Xu Li Zhonghan Tan Yuqing Wang Jinwu Yan Source Type: research

Synthesis, in Vitro Α-Glucosidase, and Acetylcholinesterase Inhibitory Activities of Novel Indol-Fused Pyrano[2,3-D]Pyrimidine Compounds
In this study, new indol-fused pyrano[2,3-d]pyrimidines were designed and synthesized. These products were obtained in moderate to good yields and their structures were assigned by NMR, MS, and IR analysis. Afterwards, the biological important of the products was highlighted by evaluating in vitro for α-glucosidase inhibitory activity as well as acetylcholinesterase (AChE) inhibitory activity. Eleven products revealed substantial inhibitory activity against α-glucosidase enzyme, among which, two most potent products 11d,e were approximately 93-fold more potent than acarbose as a standard antidiabetic drug. Besides that, ...
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Ha Thanh Nguyen Anh Nguyen Tuan Tuyet Anh Dang Thi Ket Tran Van Giang Le-Nhat-Thuy Phuong Hoang Thi Quynh Giang Nguyen Thi Cham Ba Thi Hung Tran Quang Tuyen Van Nguyen Source Type: research

Design, synthesis and evaluation of novel thieno[2,3d]pyrimidine derivatives as potent and specific RIPK2 inhibitors
Bioorg Med Chem Lett. 2023 Nov 24:129567. doi: 10.1016/j.bmcl.2023.129567. Online ahead of print.ABSTRACTIn human cells, receptor-interacting protein kinase 2 (RIPK2) is mainly known to mediate downstream enzymatic cascades from the nucleotide-binding oligomerization domain-containing receptors 1 and 2 (NOD1/2), which are regulators of pro-inflammatory signaling. Thus, the targeted inhibition of RIPK2 has been proposed as a pharmacological strategy for the treatment of a variety of pathologies, in particular inflammatory and autoimmune diseases. In this work, we designed and developed novel thieno[2,3d]pyrimidine derivativ...
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Mbilo Misehe Michal Šála Marika Matou šová Kamil Herc ík Hugo Kocek Dominika Chalupsk á Ema Chaloupeck á Miroslav H ájek Evzen Boura Helena Mertl íková-Kaiserová Radim Nencka Source Type: research

A novel sensitive fluorescent probe with double channels for highly effective recognition of biothiols
Bioorg Med Chem Lett. 2023 Nov 24:129563. doi: 10.1016/j.bmcl.2023.129563. Online ahead of print.ABSTRACTBiothiols play a crucial role in maintaining redox balance in organisms, and anomalous levels of biothiols in human organs can lead to various sicknesses and biological disorders. This work developed a novel sensitive fluorescent probe TZ-NBD with double channels for highly efficient recognition of biothiols. TZ-NBD adopts 4-Chloro-7-nitrobenzofurazan (NBD-Cl) as the recognition moiety with simultaneous fluorescence output. By incorporating NBD-Cl with the other fluorophore, benzothiazole dihydrocyclopentachromene deriv...
Source: Bioorganic and Medicinal Chemistry Letters - November 26, 2023 Category: Chemistry Authors: Qiang Fei Keyi Shen Hongxiu Ke Erfei Wang Guorun Fan Feiyi Wang Jun Ren Source Type: research

The potential of Rhein's aromatic amines for Parkinson's disease prevention and treatment: α-Synuclein aggregation inhibition and disaggregation of preformed fibers
In this study, we developed a series of aromatic amide derivatives based on Rhein. Two of these compounds, 4,5-dihydroxy-N-(3-hydroxyphenyl)-9,10-dioxo-9,10-dihydroanthracene-2-carboxamide (a5) and 4,5-dihydroxy-N-(2-hydroxy-4-chlorophenyl)-9,10-dioxo-9,10-dihydroanthracene-2-carboxamide (a8), exhibited good binding affinities to α-Syn residues, demonstrating promising inhibitory activity against α-Syn aggregation in vitro, with low IC50 values (1.35 and 1.08 μM, respectivly). These inhibitors acted throughout the entire aggregation process by stabilizing α-Syn's conformation and preventing the formation of β-sheet ag...
Source: Bioorganic and Medicinal Chemistry Letters - November 24, 2023 Category: Chemistry Authors: Wei Zhang Wei Liu Ya-Dong Zhao Li-Zi Xing Ji Xu Rui-Jun Li Yun-Xiao Zhang Source Type: research