Monitoring carbohydrate 3D structure quality with the Privateer database

• Jordan S. Dialpuri,
• Haroldas Bagdonas,
• Lucy C. Schofield,
• Phuong Thao Pham,
• Lou Holland and
• Jon Agirre

Beilstein J. Org. Chem. 2024, 20, 931–939, doi:10.3762/bjoc.20.83

• further inspection [16]. In addition to the SNFG, also displayed for each table entry is a copyable WURCS link, which encodes the complete glycan format in a linear code. The decision to present this information as a copyable link, as opposed to as plaintext is due to the inherent difficulty and

Direct synthesis of acyl fluorides from carboxylic acids using benzothiazolium reagents

• Lilian M. Maas,
• Alex Haswell,
• Rory Hughes and
• Matthew N. Hopkinson

Beilstein J. Org. Chem. 2024, 20, 921–930, doi:10.3762/bjoc.20.82

• . Keywords: acyl fluorides; amides; benzothiazolium salts; carboxylic acids; deoxygenative reactions; Introduction Acyl fluorides are attracting much attention as versatile reagents for different applications in organic synthesis. In addition to their use as sources of fluoride ions, they are most commonly

• -handle solids that can be readily produced on a multigram scale from relatively inexpensive starting materials. During the optimisation studies for the latter process with carboxylic acid substrates, in addition to the desired (trifluoromethyl)thioester products, small amounts of the corresponding acyl

• from a self-propagating process initiated by addition of an adventitious nucleophile to the electrophilic thioester. This results in elimination of a (trifluoromethyl)thiolate (−SCF3) anion (C, Scheme 4), which can subsequently undergo β-fluoride elimination, releasing a fluoride anion. Addition of F

One-pot Ugi-azide and Heck reactions for the synthesis of heterocyclic systems containing tetrazole and 1,2,3,4-tetrahydroisoquinoline

• Jiawei Niu,
• Yuhui Wang,
• Shenghu Yan,
• Yue Zhang,
• Xiaoming Ma,
• Qiang Zhang and
• Wei Zhang

Beilstein J. Org. Chem. 2024, 20, 912–920, doi:10.3762/bjoc.20.81

• oxidative cycloisomerization reactions for the synthesis of 2-tetrazolyl-substituted 3-acylpyrroles (Scheme 2C) [42]. The Ding group also reported sequential Ugi-azide/Staudinger/aza-Wittig/addition/Ag-catalyzed cyclization reactions for obtaining 12-tetrazolyl-substituted (E)-5H-quinazolino[3,2-a

•  5). A mixture of 2-bromobenzaldehyde (1a, 1 mmol), allylamine hydrochloride (2, 1 mmol), trimethylsilyl azide (3, 1 mmol) and benzyl isocyanide (1 mmol) in MeOH was reacted at 40 °C for 24 h. After evaporating the solvent, 3 mL CH3CN were added to the crude 1,5-DS-1H-T 5a followed by the addition of

• and 13C NMR, and HRMS analysis. In addition, single crystals of compound 6d and 8c were obtained for X-ray analysis to confirm the structures (Figure 2). Conclusion In conclusion, we have developed a one-pot synthesis with two or three steps for making tetrazolo-pyrazino[2,1-a]isoquinolin-6(5H)-ones

Synthesis and properties of 6-alkynyl-5-aryluracils

• Ruben Manuel Figueira de Abreu,
• Till Brockmann,
• Alexander Villinger,
• Peter Ehlers and
• Peter Langer

Beilstein J. Org. Chem. 2024, 20, 898–911, doi:10.3762/bjoc.20.80

• be activated, and the 5-position deactivated for the nucleophilic attack that occurs during the oxidative addition of the metal catalyst. This may explain the formation of only the 6-substituted product during the Sonogashira reaction. As mentioned above, new reaction conditions had to be chosen to

• that the distance between the molecules within the unit cell is higher than the distance between the unit cells. In addition, the molecules are arranged parallel-displaced to each other, which is considered to be more stable than the sandwich arrangement [64][65][66][67][68]. Consequently, the distance

• , this negligible influence could also be explained by the distance between the functional group and the core system. Compound 5f is extended by a double bond between the uracil entity and the phenyl group. In addition, it is not influenced by groups other than methyl. Interestingly, it has the second

Three-component N-alkenylation of azoles with alkynes and iodine(III) electrophile: synthesis of multisubstituted N-vinylazoles

• Jun Kikuchi,
• Roi Nakajima and
• Naohiko Yoshikai

Beilstein J. Org. Chem. 2024, 20, 891–897, doi:10.3762/bjoc.20.79

• agents, preferably with well-defined stereochemistry, is a nontrivial task. The addition of azoles to alkynes represents an alternative approach to N-vinylazoles. For example, Nolan and co-workers recently reported a gold-catalyzed addition of azoles to alkynes (hydroazolation; Scheme 1b) [10]. The gold

• catalysis encompassed various azoles such as pyrazole, indazole, and (benzo)triazole, exhibiting high Z-selectivity. In addition, Cao et al. reported a gold-catalyzed addition of 5-substituted tetrazoles to terminal alkynes [11]. Analogous hydroazolation reactions of alkynes have also been achieved under

• to 66% and 55%, respectively (Table 1, entries 6 and 7). The addition of a base such as K2CO3 completely shut down the desired reaction (Table 1, entry 8). It is worth noting that the replacement of 1 with N-iodosuccinimide, a common iodine(I) electrophile, failed to promote an analogous

(Bio)isosteres of ortho- and meta-substituted benzenes

• H. Erik Diepers and
• Johannes C. L. Walker

Beilstein J. Org. Chem. 2024, 20, 859–890, doi:10.3762/bjoc.20.78

• addition to the above physicochemical data, Mykhailiuk and co-workers assessed the antifungal activity of the suggested fluxapyroxad and boscalid bioisosteres (±)-75 and (±)-76 (Figure 12) [45]. The collected data shows that the isosteres, while still biologically active, are overall less active than the

• addition and cyclisation. Styrenyl (to 79a,c–e), acrylonitrile (to 79b) as well as acrylate-based alkenes could be inserted under the reaction conditions. The authors were then able to apply their method to the synthesis of isosteres of both boscalid (isostere = 80) and norharmane (isostere = 81) (Scheme

• 1,4-BCHs (Scheme 11B) [55]. From carboxylic acid 100e, Curtius rearrangement led to amine 101 and a photoredox decarboxylative conjugate addition to diester 102. From boronate ester 100f, oxidative deborylation led to alcohol 103, arylation led to furan 104 and Matteson homologation to boronate ester

Confirmation of the stereochemistry of spiroviolene

• Yao Kong,
• Yuanning Liu,
• Kaibiao Wang,
• Tao Wang,
• Chen Wang,
• Ben Ai,
• Hongli Jia,
• Guohui Pan,
• Min Yin and
• Zhengren Xu

Beilstein J. Org. Chem. 2024, 20, 852–858, doi:10.3762/bjoc.20.77

• organoborane intermediate, which was formed by elimination of BH3 from IM-16 followed by re-addition of BH3 from the opposite β-face to the proposed C8–C9 double bond intermediate, would also be possible. To further advance the intermediate to crystalline hydrazone product (Scheme 2B), we have found that both

Activity assays of NnlA homologs suggest the natural product N-nitroglycine is degraded by diverse bacteria

• Kara A. Strickland,
• Brenda Martinez Rodriguez,
• Ashley A. Holland,
• Shelby Wagner,
• Michelle Luna-Alva,
• David E. Graham and
• Jonathan D. Caranto

Beilstein J. Org. Chem. 2024, 20, 830–840, doi:10.3762/bjoc.20.75

• reduction of which is required for NNG degradation activity. In addition, we show that NnlA cannot degrade 2-NAE. Combined with previous substrate scope studies, this result strongly suggests that NnlA is specific for NNG. The implications of our results in understanding the environmental abundance and

• these homologs exist mostly as dimers in solution. Next, the heme incorporation of the isolated homologs was measured. UV–vis absorption spectra showed that each NnlA homolog exhibited characteristic Soret absorption features consistent with heme binding to the protein (Figure 3). In addition, the A412

• metabolic enzymes. In addition, it has been shown to irreversibly inhibit isocitrate lyase 1 (ICL1) from Mycobacterium tuberculosis [40], and key metabolic protein for these pathogens [41]. Isocitrate lyases convert isocitrate to glyoxylate and succinate. Deprotonation of 3NP (pKa = 9.0) results in the

Skeletal rearrangement of 6,8-dioxabicyclo[3.2.1]octan-4-ols promoted by thionyl chloride or Appel conditions

• Martyn Jevric,
• Julian Klepp,
• Johannes Puschnig,
• Oscar Lamb,
• Christopher J. Sumby and
• Ben W. Greatrex

Beilstein J. Org. Chem. 2024, 20, 823–829, doi:10.3762/bjoc.20.74

• ]octane, while O6 migrated when the C4–OH was axial leading to 2,4-dioxabicyclo[2.2.2]octanes. The formation of both anomers from the non-selective addition of fluoride suggested intermediates with oxocarbenium character. This work has recently been extended by Banwell and co-workers to include a set of

• groups were small, and attempts to prevent the formation of 13d by slow addition of alcohol 10d to a solution of SOCl2/pyridine in DCE reduced the yield of 11d to 14%. Heating sulfite 13d with tetrabutylammonium chloride led only to hydrolysis back to 10d without rearrangement, indicating that these

• vicinal proton. These results suggested that the formation of the allylic cation occurred readily from alcohols 15 and 18; however, the transition states leading to the rearrangement products were inaccessible and so only chloride addition occurred. The generation of the rearrangement products from the

Advancements in hydrochlorination of alkenes

• Daniel S. Müller

Beilstein J. Org. Chem. 2024, 20, 787–814, doi:10.3762/bjoc.20.72

• hydrochlorinations, followed by metal-promoted radical hydrochlorinations, and concludes with a brief overview of recent anti-Markovnikov hydrochlorinations. Keywords: addition reactions; alkenes; alkyl chlorides; hydrochlorination; Markovnikov; Introduction The hydrochlorination of alkenes dates back to its

• on metal-catalyzed radical hydrochlorinations [11] and anti-Markovnikov hydrochlorination reactions, highlighting the ongoing challenges in achieving a simple addition of HCl across a simple double bond. During our literature review for this article, we identified two other significant reviews

• focusing on hydrochlorination reactions. Firstly, an outstanding overview, including extensive research from the former Soviet Union, was reported in 1982 by Sergeev and co-workers [12]. Secondly, the chapter on “Addition of H-X Reagents to Alkenes and Alkynes” in comprehensive organic synthesis gives a

Synthesis and characterization of water-soluble C₆₀–peptide conjugates

• Yue Ma,
• Lorenzo Persi and
• Yoko Yamakoshi

Beilstein J. Org. Chem. 2024, 20, 777–786, doi:10.3762/bjoc.20.71

• derivatives by covalently attaching water-soluble moieties to the fullerene core. Subsequently, Nakamura and co-workers further developed reactions between C60 and organocopper reagents, enabling the sequential addition of functional groups to obtain penta- and decaadducts, which largely enhanced the water

• C60–peptide conjugates in this study. In addition to the water solubility introduced by the peptides, these conjugates have a superior biocompatibility compared to those with synthetic polymers, such as PEG and PVP. We utilized the previously reported biscarboxylic acid derivative 3, which was

• purified. Solubility in water The water solubility of C60–peptide conjugates 5a–c was tested after the removal of any remaining solvent traces by lyophilization. Upon addition of Milli-Q® water (pH 7.0), C60–oligo-Lys (5a) was immediately and thoroughly solubilized. In contrast, the other conjugates, C60

Synthesis of new representatives of A₃B-type carboranylporphyrins based on meso-tetra(pentafluorophenyl)porphyrin transformations

• Victoria M. Alpatova,
• Evgeny G. Rys,
• Elena G. Kononova and
• Valentina A. Ol'shevskaya

Beilstein J. Org. Chem. 2024, 20, 767–776, doi:10.3762/bjoc.20.70

• compounds allowing for the preparation of porphyrins with different reactive groups such as hydroxy and amino derivatives capable for further functionalization and conjugation of these porphyrins to other substrates. In addition, conjugates containing maleimide or biotin entities in the structure of

• has become one of the most popular route for the site-selective modification of cysteine residues in bioconjugation technology. We suppose that the maleimide group in porphyrin 11 is a useful target for thiol conjugation via Michael addition reactions [44]. This also concerns biotin-conjugated organic

Methodology for awakening the potential secondary metabolic capacity in actinomycetes

• Shun Saito and
• Midori A. Arai

Beilstein J. Org. Chem. 2024, 20, 753–766, doi:10.3762/bjoc.20.69

• Zeeck and co-workers in the early 2000s, is a method in which the target bacteria are cultured under various conditions (medium composition, temperature, pH, oxygen supply, light quality and quantity, addition of precursors and enzyme inhibitors, etc.) and all metabolites obtained from them are analyzed

• pH of the culture medium from becoming too acidic [17]. In addition, Mehmood et al. reported that the oxygen supply controls the production of pristinamycins 27 in Streptomyces pristinaespiralis (Figure 3e) [68]. Takano et al. discovered the light-induced production of carotenoid pigments, including

• generates ROS) to the culture medium [96]. In addition, there are also reports of cases in which denatured proteins are folded by molecular chaperones in high-temperature environments, and such activity may affect the production of secondary metabolites [97]. Saito et al. are currently attempting to

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

• family are the monoglycosyl, diglycosyl, or triglycosyl products of 8,8′-diapocarotene-8,8′-dioic acid (crocetin, 1) or derivatives thereof. In addition to C. sativus and G. jasminoides, Buddleja officinalis and Buddleja davidii from the Loganiaceae family [1][2], Nyctanthes arbor-tristis from the

• diseases, epilepsy, convulsion, and insomnia) and cardiovascular diseases (hypertension, hyperlipidemia, and atherosclerosis). In addition, they also have anticancer, anti-inflammatory, antioxidative, liver- and kidney-protective, antidepressant, and antidiabetic properties (Figure 2). Neuroprotection

• crocins in gastric adenocarcinoma cells [48]. In addition to the cervical cancer cell lines and gastric cancer cell lines, crocins also exhibit anticancer effects on breast, prostate, liver, colon, and leukemia cancer cell lines [49][50][51][52][53]. Besides regulating the Bax/Bcl-2 ratio, crocins were

Substrate specificity of a ketosynthase domain involved in bacillaene biosynthesis

• Zhiyong Yin and
• Jeroen S. Dickschat

Beilstein J. Org. Chem. 2024, 20, 734–740, doi:10.3762/bjoc.20.67

• of the reaction mixture potentially containing the free substrate surrogates was exchanged through repeated centrifugation using an ultrafiltration centrifugal tube (3 kDa cut-off), followed by the addition of incubation buffer. In total, through this method five successive ≈10:1 dilutions were

Chemoenzymatic synthesis of macrocyclic peptides and polyketides via thioesterase-catalyzed macrocyclization

• Senze Qiao,
• Zhongyu Cheng and
• Fuzhuo Li

Beilstein J. Org. Chem. 2024, 20, 721–733, doi:10.3762/bjoc.20.66

• cyclization and hydrolytic activities that are not easily predictable, related mechanism studies indicated that the pre-reaction states of the enzyme and substrate are critical for selectivity [15][16]. Thus, both the mutation of key residues in the active pocket and the addition of a nonionic detergent can

• TycC TE, the precursor was effectively converted into the macrocyclic tyrocidine A (1), exhibiting a low rate of substrate hydrolysis (Scheme 2a). In addition, TycC TE demonstrated a broad range of substrate tolerance, as it can cyclize a series of decapeptide-NACs that contain non-native residues in

• the resin before the SPPS, as well as a leaving group in further enzymatic cyclization (17c). Utilizing this approach, the overall yield of surugamide B (82.8%) was greater than the SNAC-based peptides with the same sequence used in the previous study (30%, Scheme 5a). In addition to investigating the

Genome mining of labdane-related diterpenoids: Discovery of the two-enzyme pathway leading to (−)-sandaracopimaradiene in the fungus Arthrinium sacchari

• Fumito Sato,
• Terutaka Sonohara,
• Shunta Fujiki,
• Akihiro Sugawara,
• Yohei Morishita,
• Taro Ozaki and
• Teigo Asai

Beilstein J. Org. Chem. 2024, 20, 714–720, doi:10.3762/bjoc.20.65

• extract of E. coli expressing ObCPS_11g, which synthesizes normal-CPP [32]. As expected, the formation of 1 was observed (Figure 4A and Figure S2 in Supporting Information File 1), indicating that the product of AsCPS was the same as that of ObCPS_11g. In addition,we incubated AsCPS in the presence of

SOMOphilic alkyne vs radical-polar crossover approaches: The full story of the azido-alkynylation of alkenes

• Julien Borrel and
• Jerome Waser

Beilstein J. Org. Chem. 2024, 20, 701–713, doi:10.3762/bjoc.20.64

• building blocks bearing two of the most versatile functional groups, allowing a rich panel of functionalization. They have been used as intermediates in numerous syntheses to access bioactive compounds [1][2][3][4] or materials [5][6][7]. In addition, azide reduction affords homopropargylic amines, which

• presence of transition metal catalysts [11][12][13][14]. Currently, this motif is synthesized by sequential introduction of the two functional groups [11][12][13]. Addition of a lithium acetylide to an epoxide affords the corresponding homopropargylic alcohol which can then undergo a sequence of mesylation

• , greatly increasing the molecular complexity of the starting substrate. Using radical chemistry would lead to a regioselective addition of azide radicals to the alkene, forming selectively the most stabilized C-centered radical. A prominent method for the generation of azide radicals relies on hypervalent

New variochelins from soil-isolated Variovorax sp. H002

• Jabal Rahmat Haedar,
• Aya Yoshimura and
• Toshiyuki Wakimoto

Beilstein J. Org. Chem. 2024, 20, 692–700, doi:10.3762/bjoc.20.63

• accessible for the cell [2][3]. In addition to the siderophores forming the stable Fe(III) complexes described above, certain siderophores create Fe(III) complexes with the ability to release Fe(II) ions in a light-responsive manner within the extracellular environment. The released Fe(II) ions in the ocean

• C45H79O17N11, as suggested by the HRESIMS data (m/z 1044.5603 for the [M − H]− ion), indicating the loss of two methylene groups (C2H4) from 1. In addition, the MS/MS fragmentation profile of 3 was consistent with those of 1 and 2, except for the loss of 28 mass units in the N-terminal Nγ-acyl-γ-amino acid

• )-ʟ-alaninamide) derivatives [5]. In addition, a combination of NOESY and bioinformatics analyses proposed all three stereocenters of 4-amino-7-guanidino-3-hydroxy-2-methylheptanoic acid as S configured [5]. The stereochemistry of these moieties in 3–5 are discussed in the next section, regarding the

Evaluation of the enantioselectivity of new chiral ligands based on imidazolidin-4-one derivatives

• Jan Bartáček,
• Karel Chlumský,
• Jan Mrkvička,
• Lucie Paloušová,
• Miloš Sedlák and
• Pavel Drabina

Beilstein J. Org. Chem. 2024, 20, 684–691, doi:10.3762/bjoc.20.62

• the C=O bond. In this manner, the asymmetric induction results in the restricted addition of nitromethane influenced by imidazolidin-4-one moieties. The higher enantioselectivity of complexes of the ligands with cis-cis configuration could be explained by the fact that the larger (RL) alkyl group is

Regioselective quinazoline C2 modifications through the azide–tetrazole tautomeric equilibrium

• Dāgs Dāvis Līpiņš,
• Andris Jeminejs,
• Una Ušacka,
• Anatoly Mishnev,
• Māris Turks and
• Irina Novosjolova

Beilstein J. Org. Chem. 2024, 20, 675–683, doi:10.3762/bjoc.20.61

• terazosin and prazosin [20]. Herein, we report the use of the sulfonyl group dance to synthesize novel 4-azido-2-sulfonylquinazolines and their C2-selective modification in SNAr reactions. In addition, we offer an approach for the synthesis of terazosin and prazosin, known medications against hypertension

• hydrolysis product 5a. In MeCN the conversion to derivative 2a was stopped at 50% and was not facilitated by an extra addition of sulfinate. To our delight, in MeOH we observed the formation of intermediate 2a over 5 hours, and after the subsequent addition of sodium azide product 4a was isolated in 31

• % yield over 2 steps. The full conversion was achieved by keeping the reaction mixture at a temperature of 0 °C and by the stepwise additions of the sulfinate and NaN3. Any deviation from these conditions facilitated the formation of byproducts. In addition, the sulfonyl group dance reactions were carried

Organic electron transport materials

• Joseph Cameron and
• Peter J. Skabara

Beilstein J. Org. Chem. 2024, 20, 672–674, doi:10.3762/bjoc.20.60

• soluble in ethyl acetate, a green solvent, and solution-processed for PM6:Y6 bulk-heterojunction solar cells with power conversion efficiency > 13% [6]. In addition to orthogonal processing, it has been shown that treatment with base [7] or photo-crosslinking [8] can insolubilise solution-processed layers

Palladium-catalyzed three-component radical-polar crossover carboamination of 1,3-dienes or allenes with diazo esters and amines

• Geng-Xin Liu,
• Xiao-Ting Jie,
• Ge-Jun Niu,
• Li-Sheng Yang,
• Xing-Lin Li,
• Jian Luo and
• Wen-Hao Hu

Beilstein J. Org. Chem. 2024, 20, 661–671, doi:10.3762/bjoc.20.59

• a challenge. In addition, many studies show that unsaturated AAs exhibit a variety of unique biological activities [21][22][23][24]. Accordingly, the development of efficient methods to synthesize unsaturated γ- and ε-AA derivatives is a highly sought-after target to enrich non-natural AA chemistry

• diverse alkenes followed by a diradical coupling or radical addition process to achieve the difunctionalization (Scheme 1b, middle) [32][33][34][35][36][37]. However, to the best of our knowledge, the methodology involving the addition of a carbon radical from a diazo compound onto the double bond of an

• alkene followed by a nucleophilic addition, is unknown (Scheme 1b, bottom). The radical-polar crossover strategy has been steadily emerging in synthetic organic chemistry during the last few years [43][44][45][46]. This strategy allows complex chemicals to be assembled with high step economy that would

Enhanced reactivity of Li⁺@C₆₀ toward thermal [2 + 2] cycloaddition by encapsulated Li⁺ Lewis acid

• Hiroshi Ueno,
• Yu Yamazaki,
• Hiroshi Okada,
• Fuminori Misaizu,
• Ken Kokubo and
• Hidehiro Sakurai

Beilstein J. Org. Chem. 2024, 20, 653–660, doi:10.3762/bjoc.20.58

• member of the emerging ion-endohedral fullerene family, have attracted significant attention owing to the distinctive ionic properties originating from the ion pair structure consisting of a cationic endohedral fullerene core and an external counter anion. Despite being a relatively recent addition, Li

• , resulting in much better yields of the target monoadducts. Electrochemical measurements revealed that the functionalization raised the LUMO level of Li+@C60, leading to lower reactivity for the second addition. With this facile, selective, and high-yield approach for the derivatization of ion-endohedral

Isolation and structure determination of a new analog of polycavernosides from marine Okeania sp. cyanobacterium

• Kairi Umeda,
• Naoaki Kurisawa,
• Ghulam Jeelani,
• Tomoyoshi Nozaki,
• Kiyotake Suenaga and
• Arihiro Iwasaki

Beilstein J. Org. Chem. 2024, 20, 645–652, doi:10.3762/bjoc.20.57

• geometry of the remaining double bond at C-18 was established to be trans by comparing the 13C NMR chemical shifts at C-16 and C-21 between 1 and polycavernoside D (5) (Table S1 in Supporting Information File 1) [5]. In addition, a 4J long-range coupling between δH 1.95 (H-26) and δH 2.18 (H-24) and three

• chain structure from C-2 to C-8. In addition, eight HMBC, δH 5.17 (H-15)/δC 171.9 (C-1), δH 2.29 (H-2)/δC 171.9 (C-1), δH 0.85 (H-28)/δC 83.5 (C-13), δH 0.85 (H-28)/δC 39.8 (C-14), δH 0.85 (H-28)/δC 78.4 (C-15), δH 0.86 (H-29)/δC 83.5 (C-13), δH 0.86 (H-29)/δC 39.8 (C-14), and δH 0.86 (H-29)/δC 78.4 (C

• trypanosomiasis) (Table 3). As a result, 1 showed moderate growth-inhibitory activities against Trypanosoma brucei rhodesiense (IC50: 9.9 μM). In addition, we examined the growth-inhibitory activity of 1 on normal human fibroblasts WI-38 (Table 3). In summary, 1 showed a moderate activity against Trypanosoma