Research progress on the pharmacological activity, biosynthetic pathways, and biosynthesis of crocins

• Zhongwei Hua,
• Nan Liu and
• Xiaohui Yan

Beilstein J. Org. Chem. 2024, 20, 741–752, doi:10.3762/bjoc.20.68

• Pharmacokinetic investigations have shown that crocins can be hydrolyzed to crocetin (1) in the gastrointestinal tract of mice. Crocetin derivatives can penetrate the blood–brain barrier to exert therapeutic effects on neurodegenerative diseases, such as Alzheimer's disease, Parkinson's disease, retinal diseases

• , and epileptic disorders [26][27]. Four mechanisms have been reported for the treatment of Alzheimer's disease with crocins. Crocins function as antioxidants that slow down the progression of the disease by increasing the ʟ-glutathione (GSH) level and reducing the presence of reactive oxygen species

Recent developments in the engineered biosynthesis of fungal meroterpenoids

• Zhiyang Quan and
• Takayoshi Awakawa

Beilstein J. Org. Chem. 2024, 20, 578–588, doi:10.3762/bjoc.20.50

• , including the known antitumor compound subglutinol A (16) (Figure 3A and B) [17]. Among the novel compounds isolated from the production system, some exhibited intruiging pharmacological activities, such as antitumor (16), anti-HIV activity (17), and anti-Alzheimer's disease properties (18). Furthermore

Synthesis of imidazo[1,2-a]pyridine-containing peptidomimetics by tandem of Groebke–Blackburn–Bienaymé and Ugi reactions

• Oleksandr V. Kolomiiets,
• Alexander V. Tsygankov,
• Maryna N. Kornet,
• Aleksander A. Brazhko,
• Vladimir I. Musatov and
• Valentyn A. Chebanov

Beilstein J. Org. Chem. 2023, 19, 727–735, doi:10.3762/bjoc.19.53

• be used as potential drug candidate against Alzheimer's disease [14]. Compounds containing the imidazo[1,2-a]pyridine moiety are present in many natural products and marketed drugs, e.g., alpidem (an anxiolytic) [15], necopidem (anxiolytic) [16], zolpidem (hypnotic for the treatment of insomnia) [17

Cyclometalated iridium complexes-catalyzed acceptorless dehydrogenative coupling reaction: construction of quinoline derivatives and evaluation of their antimicrobial activities

• Hongling Shui,
• Yuhong Zhong,
• Renshi Luo,
• Zhanyi Zhang,
• Jiuzhong Huang,
• Ping Yang and
• Nianhua Luo

Beilstein J. Org. Chem. 2022, 18, 1507–1517, doi:10.3762/bjoc.18.159

• , quinoline and its derivatives widely exist in natural products. They have a wide range of biological activities, such as antibacterial [1], anti-inflammatory [2], antitumor [3], antihepatitis C (HCV) [4], antituberculosis (TB) [5], antimalarial [6], and anti-Alzheimer's disease (AD) [7]. Among these

Synthesis and investigation on optical and electrochemical properties of 2,4-diaryl-9-chloro-5,6,7,8-tetrahydroacridines

• Najeh Tka,
• Mohamed Adnene Hadj Ayed,
• Mourad Ben Braiek,
• Mahjoub Jabli and
• Peter Langer

Beilstein J. Org. Chem. 2021, 17, 2450–2461, doi:10.3762/bjoc.17.162

• [44][45]. In particular, they have been widely explored for the treatment of Alzheimer's disease [46][47][48][49][50][51], human cancer [52][53], and tuberculosis [54] (Figure 1). Taking into consideration the significant medicinal potential of tetrahydroacridines and the lack of knowledge concerning

2,4-Bis(arylethynyl)-9-chloro-5,6,7,8-tetrahydroacridines: synthesis and photophysical properties

• Najeh Tka,
• Mohamed Adnene Hadj Ayed,
• Mourad Ben Braiek,
• Mahjoub Jabli,
• Noureddine Chaaben,
• Kamel Alimi,
• Stefan Jopp and
• Peter Langer

Beilstein J. Org. Chem. 2021, 17, 1629–1640, doi:10.3762/bjoc.17.115

• ring, is another privileged scaffold which showed interesting biological activities [48][49][50][51][52][53][54]. As a typical example, 9-amino-1,2,3,4-tetrahydroacridine or tacrine was the first drug approved for the treatment of Alzheimer's disease [55][56][57]. Surprisingly, photophysical properties

Application of the Meerwein reaction of 1,4-benzoquinone to a metal-free synthesis of benzofuropyridine analogues

• Rashmi Singh,
• Tomas Horsten,
• Rashmi Prakash,
• Swapan Dey and
• Wim Dehaen

Beilstein J. Org. Chem. 2021, 17, 977–982, doi:10.3762/bjoc.17.79

• ][21]. These compounds are presumably multitargeting drugs because of the diverse applications as insulin-like growth factor 1 receptor (IGF-1R) inhibitors [22], selective GSK-3β inhibitors important in Alzheimer's disease [23][24], and cyclin-dependent kinase (CDK) inhibitors [25][26][27]. Lastly, the

Vicinal difluorination as a C=C surrogate: an analog of piperine with enhanced solubility, photostability, and acetylcholinesterase inhibitory activity

• Yuvixza Lizarme-Salas,
• Alexandra Daryl Ariawan,
• Ranjala Ratnayake,
• Hendrik Luesch,
• Angela Finch and
• Luke Hunter

Beilstein J. Org. Chem. 2020, 16, 2663–2670, doi:10.3762/bjoc.16.216

• for E-alkenes in medicinal chemistry. Keywords: Alzheimer's disease; bioisostere; conformational analysis; gauche effect; stereoselective synthesis; Introduction Piperine (1, Figure 1) is a well-known natural product that is derived from peppercorns [1][2][3]. Many biological studies of 1 have been

Combining enyne metathesis with long-established organic transformations: a powerful strategy for the sustainable synthesis of bioactive molecules

• Valerian Dragutan,
• Ileana Dragutan,
• Albert Demonceau and
• Lionel Delaude

Beilstein J. Org. Chem. 2020, 16, 738–755, doi:10.3762/bjoc.16.68

• metathesis steps applying the second-generation Hoveyda–Grubbs Ru catalyst, while, unexpectedly, the second-generation Grubbs ruthenium catalyst was less active and gave rise to some side-products. (−)-Galanthamine An important alkaloid active in the treatment of mild to moderate Alzheimer's disease and

Microfluidic radiosynthesis of [¹⁸F]FEMPT, a high affinity PET radiotracer for imaging serotonin receptors

• Thomas Lee Collier,
• Steven H. Liang,
• J. John Mann,
• Neil Vasdev and
• J. S. Dileep Kumar

Beilstein J. Org. Chem. 2017, 13, 2922–2927, doi:10.3762/bjoc.13.285

• supersensitivity. Significant research has been directed at the differences between agonist and antagonist binding to 5-HT1A receptors in Alzheimer's disease [10] and this interest has led to the development of a high-resolution in vivo atlas for four of the human brain's serotonin receptors and transporters [11

Synthesis of 1-indanones with a broad range of biological activity

• Marika Turek,
• Dorota Szczęsna,
• Marek Koprowski and
• Piotr Bałczewski

Beilstein J. Org. Chem. 2017, 13, 451–494, doi:10.3762/bjoc.13.48

• -1-indanone. New 1-indanone derivatives that may be used as multi-functional drugs for the treatment of Alzheimer's disease have been synthesized by Li et al. [8]. In this synthesis, ferulic acid (23) was hydrogenated in the presence of Pd/C catalyst to give the saturated derivative 24 and then

Exploration of C–H and N–H-bond functionalization towards 1-(1,2-diarylindol-3-yl)tetrahydroisoquinolines

• Michael Ghobrial,
• Marko D. Mihovilovic and
• Michael Schnürch

Beilstein J. Org. Chem. 2014, 10, 2186–2199, doi:10.3762/bjoc.10.226

• receptor ligands (Figure 1, III) [6], having potential in the treatment of Alzheimer's disease (Figure 1, IV) [7], or in treatment of diseases associated with defects in vesicular (axonal) transport (Figure 1, IV) [8]. Interestingly, 1-(indol-3-yl)-THIQs carrying additional aryl substituents on the indole

Flexible synthesis of poison- frog alkaloids of the 5,8-disubstituted indolizidine- class. II: Synthesis of (-)-209B, (-)-231C, (-)-233D, (-)-235B", (-)-221I, and an epimer of 193E and pharmacological effects at neuronal nicotinic acetylcholine receptors

• Soushi Kobayashi,
• Naoki Toyooka,
• Dejun Zhou,
• Hiroshi Tsuneki,
• Tsutomu Wada,
• Toshiyasu Sasaoka,
• Hideki Sakai,
• Hideo Nemoto,
• H. Martin Garraffo,
• Thomas F. Spande and
• John W. Daly

Beilstein J. Org. Chem. 2007, 3, No. 30, doi:10.1186/1860-5397-3-30

• . [5] Nicotinic receptors have been implicated in a wide range of neuronal dysfunctions and mental illness, such as epilepsy, Tourette's syndrome, Alzheimer's disease, Parkinson's disease, and schizophrenia. [5][6] Since different subtypes of nicotinic receptors are involved in different neurological

• , learning and memory. [5][6] Some ligand-binding and autoradiography studies with postmortem human brain suggest that loss of neuronal nicotinic receptors is related to central cholinergic disorders such as Alzheimer's disease, Parkinson's disease and schizophrenia. [4][6] For instance, in schizophrenic