Five new sesquiterpenoids from agarwood of Aquilaria sinensis

• Hong Zhou,
• Xu-Yang Li,
• Hong-Bin Fang,
• He-Zhong Jiang and
• Yong-Xian Cheng

Beilstein J. Org. Chem. 2023, 19, 998–1007, doi:10.3762/bjoc.19.75

• revealed the structure–activity relationships (SAR). Keywords: agarwood; Aquilaria sinensis; SAR studies; sesquiterpenoids; Introduction Agarwood is the resinous wood of the Aquilaria species of the Thymelaeaceae family [1]. It is a precious traditional Chinese medicinal material and a kind of natural

Synthesis and biological evaluation of 1,2-disubstituted 4-quinolone analogues of Pseudonocardia sp. natural products

• Stephen M. Geddis,
• Teodora Coroama,
• Suzanne Forrest,
• James T. Hodgkinson,
• Martin Welch and
• David R. Spring

Beilstein J. Org. Chem. 2018, 14, 2680–2688, doi:10.3762/bjoc.14.245

• transposition, whilst 4, 7 and 8 were derivatised from 1. In this current work, we turn to the further elucidation of the biological activity of this class of compounds. In order to gain additional insight into the associated structure–activity relationships (SAR), it was desired to generate analogues of the

Synthesis of 1,4-imino-L-lyxitols modified at C-5 and their evaluation as inhibitors of GH38 α-mannosidases

• Maroš Bella,
• Sergej Šesták,
• Ján Moncoľ,
• Miroslav Koóš and
• Monika Poláková

Beilstein J. Org. Chem. 2018, 14, 2156–2162, doi:10.3762/bjoc.14.189

• be more potent and selective inhibitors of the target enzyme. Moreover, proposed N-benzyl substituent at the pyrrolidine core was also confirmed to be essential for selectivity [30]. In this study, we explored structure–activity relationships (SAR) of pyrrolidine derivatives 1 with different

Defining the hydrophobic interactions that drive competence stimulating peptide (CSP)-ComD binding in Streptococcus pneumoniae

• Bimal Koirala,
• Robert A. Hillman,
• Erin K. Tiwold,
• Michael A. Bertucci and
• Yftah Tal-Gan

Beilstein J. Org. Chem. 2018, 14, 1769–1777, doi:10.3762/bjoc.14.151

• stimulating peptide (CSP); protein–peptide interactions; quorum sensing; Streptococcus pneumoniae; structure–activity relationships (SAR); Introduction Quorum sensing (QS), a cell-density mechanism utilized by bacteria to assess their population density through the detection of diffusible signal molecules

Beta-hydroxyphosphonate ribonucleoside analogues derived from 4-substituted-1,2,3-triazoles as IMP/GMP mimics: synthesis and biological evaluation

• Tai Nguyen Van,
• Audrey Hospital,
• Corinne Lionne,
• Lars P. Jordheim,
• Charles Dumontet,
• Christian Périgaud,
• Laurent Chaloin and
• Suzanne Peyrottes

Beilstein J. Org. Chem. 2016, 12, 1476–1486, doi:10.3762/bjoc.12.144

• effectiveness of cN-II inhibitors in the treatment of these diseases [4][5]. As a result of our interest in this area, we and others [6] have investigated a number of structure–activity relationships (SAR) [7][8] and various medicinal chemistry approaches [9][10] to identify potential cN-II inhibitors. As part

Synthesis and antibacterial activity of monocyclic 3-carboxamide tetramic acids

• Yong-Chul Jeong and
• Mark G. Moloney

Beilstein J. Org. Chem. 2013, 9, 1899–1906, doi:10.3762/bjoc.9.224

• influenzae, including an efflux-negative strain, and 2 strains of Escherichia coli, including an efflux-negative strain (Table 2). Relevant physicochemical properties of the analogues are also shown in Table 3. These were used to elaborate structure–activity relationships (SAR) [26]. In the assay against

ML212: A small-molecule probe for investigating fluconazole resistance mechanisms in Candida albicans

• Willmen Youngsaye,
• Cathy L. Hartland,
• Barbara J. Morgan,
• Amal Ting,
• Partha P. Nag,
• Benjamin Vincent,
• Carrie A. Mosher,
• Joshua A. Bittker,
• Sivaraman Dandapani,
• Michelle Palmer,
• Luke Whitesell,
• Susan Lindquist,
• Stuart L. Schreiber and
• Benito Munoz

Beilstein J. Org. Chem. 2013, 9, 1501–1507, doi:10.3762/bjoc.9.171

• closely related analogues were prepared to enable investigation of possible structure–activity relationships (SAR) [18]. In addition to indazole 1, two other structurally distinct scaffolds (2 and 3) were also selected for follow-up studies and those works are communicated elsewhere [19][20]. Chemistry

Synthesis and physicochemical characterization of novel phenotypic probes targeting the nuclear factor-kappa B signaling pathway

• Paul M. Hershberger,
• Satyamaheshwar Peddibhotla,
• E. Hampton Sessions,
• Daniela B. Divlianska,
• Ricardo G. Correa,
• Anthony B. Pinkerton,
• John C. Reed and
• Gregory P. Roth

Beilstein J. Org. Chem. 2013, 9, 900–907, doi:10.3762/bjoc.9.103

• –activity relationships (SAR) through analogue synthesis [9]. This probe was discovered after two separate screening campaigns totaling ~110,000 compounds. At concentrations up to 8 μM, 4 failed to suppress PKCβ and PKCθ (the PKC family members implicated in TCR/BCR signaling) and IKKβ, while known PKC and

• other NF-κB activation pathways such as those including the cytosolic proteins CARMA1, Bcl-10, MALT1, TRAF6 and Ubc13 [8]. The first probe identified within this series was the benzimidazole ML029 (4), which exhibited an IC50 of 0.07 μM in the HEK 293 cell assay with corresponding well-defined structure

The multicomponent approach to N-methyl peptides: total synthesis of antibacterial (–)-viridic acid and analogues

• Ricardo A. W. Neves Filho,
• Sebastian Stark,
• Bernhard Westermann and
• Ludger A. Wessjohann

Beilstein J. Org. Chem. 2012, 8, 2085–2090, doi:10.3762/bjoc.8.234

• , with competitive Passerini reaction in the latter case [28][29]. With the general process in place, the MCR approach was employed to generate a library of synthetic derivatives of 1 with the hope of gaining a first glimpse of structure–activity relationships (SAR), and to give hints for further

Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors

• Chao Che,
• Song Li,
• Bo Yang,
• Shengchang Xin,
• Zhixiong Yu,
• Taofeng Shao,
• Chuanye Tao,
• Shuo Lin and
• Zhen Yang

Beilstein J. Org. Chem. 2012, 8, 841–849, doi:10.3762/bjoc.8.94

• secondary alkylamine due to the different conformational changes induced. This promising result prompted us to further investigate the structure–activity relationships (SAR) of Sant-75. Herein we describe our efforts in the development of synthetic methods for the construction of a library of Sant-75

Synthetic glycopeptides and glycoproteins with applications in biological research

• Ulrika Westerlind

Beilstein J. Org. Chem. 2012, 8, 804–818, doi:10.3762/bjoc.8.90

• ]. Synthetic glycoproteins An important task for chemists is to make homogenous glycoproteins and complex glycopeptides available for biological research. Studies of glycosylation effects on protein conformation, stability and structure–activity relationships (SAR) are a few examples of the applications of

Synthesis of crispine A analogues via an intramolecular Schmidt reaction

• Ajoy Kapat,
• Ponminor Senthil Kumar and
• Sundarababu Baskaran

Beilstein J. Org. Chem. 2007, 3, No. 49, doi:10.1186/1860-5397-3-49

• the synthesis of a library of anti-cancer analogues. The structure activity relationships (SAR) and anti-cancer activities of our synthetic derivatives will be reported in due course of time. ORTEP diagram of the acid derivative 4. Epoxide initiated electrophilic cyclization of azide. Crispine A and