Two new lanostanoid glycosides isolated from a Kenyan polypore Fomitopsis carnea

• Winnie Chemutai Sum,
• Sherif S. Ebada,
• Didsanutda Gonkhom,
• Cony Decock,
• Rémy Bertrand Teponno,
• Josphat Clement Matasyoh and
• Marc Stadler

Beilstein J. Org. Chem. 2023, 19, 1161–1169, doi:10.3762/bjoc.19.84

• well-known profuse production of bioactive molecules, Basidiomycota have already been proven to be a valuable source for new anti-infectives [4]. These include a myriad of triterpenoids which have been resourceful in the discovery of potent antimicrobials [5]. Specifically, lanostane triterpenoids are

Antibacterial scalarane from Doriprismatica stellata nudibranchs (Gastropoda, Nudibranchia), egg ribbons, and their dietary sponge Spongia cf. agaricina (Demospongiae, Dictyoceratida)

• Cora Hertzer,
• Stefan Kehraus,
• Nils Böhringer,
• Fontje Kaligis,
• Robert Bara,
• Dirk Erpenbeck,
• Gert Wörheide,
• Till F. Schäberle,
• Heike Wägele and
• Gabriele M. König

Beilstein J. Org. Chem. 2020, 16, 1596–1605, doi:10.3762/bjoc.16.132

• -diacetoxy-3,4-methylenedeoxoscalarin. Acknowledgements We thank Dr. Henrik Harms for conducting the antimicrobial assays (grant No 9.818, DZIF, Innovative microbial resources for new anti-infectives). Furthermore, we thank Adrian Galitz for support in the laboratory and Rob W. M. van Soest, Nicole J. de

Protein–protein interactions in bacteria: a promising and challenging avenue towards the discovery of new antibiotics

• Laura Carro

Beilstein J. Org. Chem. 2018, 14, 2881–2896, doi:10.3762/bjoc.14.267

• in both Gram-positive and Gram-negative microorganisms, findings that could be of value in the development of optimized antagonists for potential use as antibacterials. N-Utilization substances (Nus) B and E Another point of therapeutic intervention to develop new anti-infectives that target cell

• molecules against these PPI (or other interactions involved in bacterial transcription yet to be discovered and validated) may have something to offer in the ongoing research towards the development of new anti-infectives with novel mechanisms of action. Conclusion Pathogenic bacteria are a leading cause of

Targeting the Pseudomonas quinolone signal quorum sensing system for the discovery of novel anti-infective pathoblockers

• Christian Schütz and
• Martin Empting

Beilstein J. Org. Chem. 2018, 14, 2627–2645, doi:10.3762/bjoc.14.241

• coordinate population-wide group behaviours in the infection process like concerted secretion of virulence factors. One very important signalling network is the Pseudomonas quinolone signal (PQS) QS. With the aim to devise novel and innovative anti-infectives, inhibitors have been designed to address the

• highlights the published drug discovery efforts providing insights into the compound binding modes if available. Furthermore, suitability of the individual targets for pathoblocker design is discussed. Keywords: anti-infectives; pathoblockers; PQS; Pseudomonas aeruginosa; quorum sensing; Introduction In

Pathoblockers or antivirulence drugs as a new option for the treatment of bacterial infections

• Matthew B. Calvert,
• Varsha R. Jumde and
• Alexander Titz

Beilstein J. Org. Chem. 2018, 14, 2607–2617, doi:10.3762/bjoc.14.239

• current trends continue. To avoid this scenario, new classes of anti-infectives must urgently be developed. Antibiotics with new modes of action are needed, but other concepts are also currently being pursued. Targeting bacterial virulence as a means of blocking pathogenicity is a promising new strategy

• ]. Despite the challenges associated with the large size of the pore structures, small molecules have also been widely studied as antitoxins and there are examples at various stages of the discovery process [51]. An important example of this concept is the application of cyclodextrins as anti-infectives [57

• formation and virulence in an insect infection model or a murine model [76][77][78]. Conclusion The current antimicrobial crisis poses an enormous challenge to society, and requires a joint effort for the development of novel anti-infectives. While there is an urgent need for new antibiotics with novel

A novel and practical asymmetric synthesis of eptazocine hydrobromide

• Ruipeng Li,
• Zhenren Liu,
• Liang Chen,
• Jing Pan,
• Kuaile Lin and
• Weicheng Zhou

Beilstein J. Org. Chem. 2018, 14, 2340–2347, doi:10.3762/bjoc.14.209

• Ruipeng Li Zhenren Liu Liang Chen Jing Pan Kuaile Lin Weicheng Zhou State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, No. 285, Gebaini Rd., Shanghai 201203, P. R

Enantioselective phase-transfer catalyzed alkylation of 1-methyl-7-methoxy-2-tetralone: an effective route to dezocine

• Ruipeng Li,
• Zhenren Liu,
• Liang Chen,
• Jing Pan and
• Weicheng Zhou

Beilstein J. Org. Chem. 2018, 14, 1421–1427, doi:10.3762/bjoc.14.119

• Ruipeng Li Zhenren Liu Liang Chen Jing Pan Weicheng Zhou State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, No. 285, Gebaini Rd., Shanghai 201203, P. R. of China

A concise and practical stereoselective synthesis of ipragliflozin L-proline

• Shuai Ma,
• Zhenren Liu,
• Jing Pan,
• Shunli Zhang and
• Weicheng Zhou

Beilstein J. Org. Chem. 2017, 13, 1064–1070, doi:10.3762/bjoc.13.105

• Shuai Ma Zhenren Liu Jing Pan Shunli Zhang Weicheng Zhou State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, No. 285, Gebaini Rd., Shanghai 201203, P. R. of China

Polyketide stereocontrol: a study in chemical biology

• Kira J. Weissman

Beilstein J. Org. Chem. 2017, 13, 348–371, doi:10.3762/bjoc.13.39

• this approach to provide answers to fundamental biological questions. Keywords: chemical biology; polyketide synthases; reduced polyketides; stereocontrol; Introduction Reduced polyketides and their derivatives form the basis for a number of medicines in current clinical usage, notably anti

• -infectives [1] (e.g., erythromycin A (1) and its semi-synthetic derivatives azithromycin (2), clarithromycin (3), telithromycin (4) ([2] and others) and anticancer compounds (e.g., ixabepilone (5) [3]), a semi-synthetic derivative of the natural product epothilone B (6)) (Figure 1). Given the medical and

A novel and practical asymmetric synthesis of dapoxetine hydrochloride

• Yijun Zhu,
• Zhenren Liu,
• Hongyan Li,
• Deyong Ye and
• Weicheng Zhou

Beilstein J. Org. Chem. 2015, 11, 2641–2645, doi:10.3762/bjoc.11.283

• Yijun Zhu Zhenren Liu Hongyan Li Deyong Ye Weicheng Zhou State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, State Institute of Pharmaceutical Industry, No. 285, Gebaini Rd., Shanghai 201203, China School of Pharmacy, Fudan University, No. 826, Zhangheng Rd

Synthesis of the spiroketal core of integramycin

• Evgeny. V. Prusov

Beilstein J. Org. Chem. 2013, 9, 2446–2450, doi:10.3762/bjoc.9.282

• required ketone precursor was efficiently constructed from two simple and easily accessible subunits by means of a hydrozirconation/copper catalyzed acylation reaction. The effects of different protecting groups on the spiroketalization step were also investigated. Keywords: anti-infectives