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Design, Synthesis and Biological Activity of Organic Compounds

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A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Organic Chemistry".

Deadline for manuscript submissions: closed (31 July 2023) | Viewed by 18389

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Special Issue Editors

Dr. Hari Krishna Namballa

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Guest Editor

Department of Chemistry, Hunter College, City University of New York, 695 Park Avenue, New York, NY 10065, USA
Interests: medicinal chemistry; HDAC inhibitors; cancer; CNS ligands; total synthesis; method development
Special Issues, Collections and Topics in MDPI journals

Dr. Wayne W. Harding

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Guest Editor

Department of Chemistry, Hunter College, New York, NY, USA
Interests: medicinal chemistry; CNS ligands; natural products total synthesis; cancer
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Chemistry is often referred to as the central science, as it bridges the divide between the life sciences and the physical sciences. Organic chemistry is no exception, incorporating physics (and with it mathematics and computational sciences) into biology and medicine through the design, synthesis, and biological evaluation and application of organic compounds. Isolated compounds from natural sources have made (and will continue to make) major contributions to drug discovery due to their application for optimization of the treatment of essentially every known disease and illness. Yet, the synthesis of natural products and their analogues is often easier said than done, requiring truly exceptional dedication and skill. With each day, astonishing advances are made in computational sciences that assist organic/medicinal chemists in drug discovery and development.

For this Special Issue, we welcome papers that highlight organic chemistry in terms of its biological relevance (this can be addressed from the perspective of several sub-disciplines, such as medicinal chemistry, natural products chemistry, total synthesis, and computational chemistry).

Dr. Hari Krishna Namballa
Dr. Wayne W. Harding
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Molecules is an international peer-reviewed open access semimonthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2700 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Keywords

medicinal chemistry
natural products
total synthesis
bioactive ligands
computer-aided drug design (cadd)
drug discovery
pharmacology

Published Papers (11 papers)

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30 pages, 5561 KiB

Open AccessArticle

Synthesis, Computational, and Anticancer In Vitro Investigations of Aminobenzylnaphthols Derived from 2-Naphtol, Benzaldehydes, and α-Aminoacids via the Betti Reaction

by Mateusz Kciuk, Martyna Malinowska, Adrianna Gielecińska, Rajamanikandan Sundaraj, Somdutt Mujwar, Anna Zawisza and Renata Kontek

Molecules 2023, 28(20), 7230; https://doi.org/10.3390/molecules28207230 - 23 Oct 2023

Viewed by 1063

Abstract

Multicomponent reactions have emerged as an important approach for the synthesis of diverse and complicated chemical compounds. They have various advantages over two-component reactions, including the convenience of one-pot procedures and the ability to modify the structure of agents. Here, we employed in vitro and in silico studies to explore the anticancer potential of novel aminobenzylnaphthols derived from the Betti reaction (MMZ compounds). MTT assay was used to explore the cytotoxic activity of the compounds in pancreatic (BxPC-3 cells) and colorectal (HT-29) cancer cell lines or normal human lung fibroblasts (WI-38 cells). Proapoptotic properties of two derivatives MMZ-45AA and MMZ-140C were explored using AO/EB and annexin V-FITC/PI staining. In silico studies including ADMET profiling, molecular target prediction, docking, and dynamics were employed. The compounds exhibited cytotoxic properties and showed proapoptotic properties in respective IC₅₀ concentrations. As indicated by in silico investigations, anticancer activity of MMZs can be attributed to the inhibition of ADORA1, CDK2, and TRIM24. Furthermore, compounds exhibited favorable ADMET properties. MMZs constitute an interesting scaffold for the potential development of new anticancer agents. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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17 pages, 1163 KiB

Open AccessArticle

Structure–Activity Relationship Studies on 6-Chloro-1-phenylbenzazepines Leads to the Identification of a New Dopamine D1 Receptor Antagonist

by Rajan Giri, Hari K. Namballa, Vishwashiv Emogaje and Wayne W. Harding

Molecules 2023, 28(16), 6010; https://doi.org/10.3390/molecules28166010 - 11 Aug 2023

Viewed by 1008

Abstract

The 1-phenylbenzazepine template has yielded a number of D1R-like ligands, which, though useful as pharmacological tools, have significant drawbacks in terms of selectivity versus D5R as well as pharmacokinetic behavior. A number of 1-phenylbenzazepines contain a 6-chloro functional group, but extensive SAR studies around the 6-chloro-1-phenylbenzazepine framework have not been reported in the literature. To further understand the tolerance of the 6-chloro-1-phenylbenzazepine template for various substituent groups towards affinity and selectivity at D1R, we synthesized two series of analogs with structural variations at the C-7, C-8, N-3, C-3′ and C-4′ positions. The series 2 analogs differed from series 1 analogs in possessing a nitrogenated functionality at C-8 and lacked a C-4′ substituent, but were otherwise similar. Analogs were assessed for affinity at D1R, D2R and D5R. For both series, we found that the analogs lacked affinity for D2R and showed modest D1R versus D5R selectivity. For series 1 analogs, an N-3 methyl substituent group was better tolerated than N-H or an N-3 allyl substituent. The C-8 position appears to be tolerant of amino and methanesulfonamide substituents for high D1R affinity, but C-8 amides displayed low to moderate D1R affinities. A C-3′ methyl substituent appeared to be critical for the D1R affinity of some analogs, but the C-4′ substituents tried (hydroxy and methoxy; series 1) did not result in any significant boost in D1R affinity. Compound 15a was the most potent and selective D1R ligand identified from these studies (K_i at D1R = 30 nM; 6-fold selectivity versus D5R). Further functional activity assessments indicate that 15a functions as a D1R antagonist towards cAMP-mediated signaling. The predicted drug-like properties of 15a are encouraging for further pharmacological assessments on the compound. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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10 pages, 2453 KiB

Open AccessArticle

Targeting Carbohydrate Mimetics of Tetrahydrofuran-Containing Acetogenins to Prostate Cancer

by Patricia Gonzalez Periche, Jacky Lin, Naga V. S. D. K. Bhupathiraju, Teja Kalidindi, Delissa S. Johnson, Nagavarakishore Pillarsetty and David R. Mootoo

Molecules 2023, 28(7), 2884; https://doi.org/10.3390/molecules28072884 - 23 Mar 2023

Viewed by 1297

Abstract

The high potency of the tetrahydrofuran-containing acetogenins (THF-ACGs) against a broad range of human cancer cell lines has stimulated interest in structurally simpler mimetics. In this context, we have previously reported THF-ACG mimetics in which the THF and butenolide moieties of a mono-THF-ACG were replaced with carbohydrate and thiophene residues, respectively. In the present study, towards the targeting of these carbohydrate analogues to prostate cancer (PCa), we synthesized prodrugs in which a parent thiophene or butenolide congener was conjugated through a self-immolative linker to 2-[3-(1,3-dicarboxypropyl)ureido] pentanedioic acid (DUPA), a highly specific ligand for prostate-specific membrane antigen (PSMA), which is overexpressed on prostate tumors. Both prodrugs were found to be more active against receptor positive LNCaP than receptor-negative PC-3 cells, with 2.5 and 12 times greater selectivity for the more potent thiophene analog and the less active butenolide congener, respectively. This selectivity for LNCaP over PC-3 contrasted with the behavior of the parent drugs, which showed similar or significantly higher activity for PC-3 compared to LNCaP. These data support the notion that higher activity of these DUPA-derived prodrugs against LNCaP cells is connected to their binding to PSMA and suggest that the conjugation of PSMA ligands to this family of cytotoxic agents may be effective for targeting them to PCa. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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19 pages, 4074 KiB

Open AccessArticle

Synthesis of 4-Amino-N-[2 (diethylamino)Ethyl]Benzamide Tetraphenylborate Ion-Associate Complex: Characterization, Antibacterial and Computational Study

by Gamal A. E. Mostafa, Ahmed H. Bakheit, Mohamed H. Al-Agamy, Rashad Al-Salahi, Essam A. Ali and Haitham Alrabiah

Molecules 2023, 28(5), 2256; https://doi.org/10.3390/molecules28052256 - 28 Feb 2023

Cited by 5 | Viewed by 1599

Abstract

The 4-amino-N-[2 (diethylamino) ethyl] benzamide (procainamide)-tetraphenylborate complex was synthesized by reacting sodium tetraphenyl borate with 4-amino-N-[2 (diethylamino) ethyl] benzamide, chloride salt, and procainamide in deionized water at room temperature through an ion-associate reaction (green chemistry) at room temperature, and characterized by several physicochemical methods. The formation of ion-associate complex between bio-active molecules and/or organic molecules is crucial to comprehending the relationships between bioactive molecules and receptor interactions. The solid complex was characterized by infrared spectra, NMR, elemental analysis, and mass spectrometry, indicating the formation of ion-associate or ion-pair complex. The complex under study was examined for antibacterial activity. The ground state electronic characteristics of the S1 and S2 complex configurations were computed using the density functional theory (DFT) approach, using B3LYP level 6-311 G(d,p) basis sets. R² = 0.9765 and 0.9556, respectively, indicate a strong correlation between the observed and theoretical ¹H-NMR, and the relative error of vibrational frequencies for both configurations was acceptable, as well. HOMO and LUMO frontier molecular orbitals and molecular electrostatics using the optimized were used to obtain a potential map of the chemical. The n → π* UV absorption peak of the UV cutoff edge was detected for both configurations of the complex. Spectroscopic methods were structures used to characterize the structure (FT-IR and 1HNMR). In the ground state, DFT/B3LYP/6-311G(d,p) basis sets were used to determine the electrical and geometric properties of the S1 and S2 configurations of the title complex. Comparing the observed and calculated values for the S1 and S2 forms, the HOMO-LUMO energy gap of compounds was 3182 and 3231 eV, respectively. The small energy gap between HOMO and LUMO indicated that the compound was stable. In addition, the MEP reveals that positive potential sites were around the PR molecule, whereas negative potential sites were surrounding the TPB site of atoms. The UV absorption of both arrangements is comparable to the experimental UV spectrum. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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27 pages, 17743 KiB

Open AccessArticle

Synthesis, DFT Studies, Molecular Docking and Biological Activity Evaluation of Thiazole-Sulfonamide Derivatives as Potent Alzheimer’s Inhibitors

by Shoaib Khan, Hayat Ullah, Muhammad Taha, Fazal Rahim, Maliha Sarfraz, Rashid Iqbal, Naveed Iqbal, Rafaqat Hussain, Syed Adnan Ali Shah, Khurshid Ayub, Marzough Aziz Albalawi, Mahmoud A. Abdelaziz, Fatema Suliman Alatawi and Khalid Mohammed Khan

Molecules 2023, 28(2), 559; https://doi.org/10.3390/molecules28020559 - 05 Jan 2023

Cited by 29 | Viewed by 2640

Abstract

Alzheimer’s disease is a major public brain condition that has resulted in many deaths, as revealed by the World Health Organization (WHO). Conventional Alzheimer’s treatments such as chemotherapy, surgery, and radiotherapy are not very effective and are usually associated with several adverse effects. Therefore, it is necessary to find a new therapeutic approach that completely treats Alzheimer’s disease without many side effects. In this research project, we report the synthesis and biological activities of some new thiazole-bearing sulfonamide analogs (1–21) as potent anti-Alzheimer’s agents. Suitable characterization techniques were employed, and the density functional theory (DFT) computational approach, as well as in-silico molecular modeling, has been employed to assess the electronic properties and anti-Alzheimer’s potency of the analogs. All analogs exhibited a varied degree of inhibitory potential, but analog 1 was found to have excellent potency (IC₅₀ = 0.10 ± 0.05 µM for AChE) and (IC₅₀ = 0.20 ± 0.050 µM for BuChE) as compared to the reference drug donepezil (IC₅₀ = 2.16 ± 0.12 µM and 4.5 ± 0.11 µM). The structure-activity relationship was established, and it mainly depends upon the nature, position, number, and electron-donating/-withdrawing effects of the substituent/s on the phenyl rings. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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17 pages, 819 KiB

Open AccessArticle

Evaluation of the Local Anesthetic Activity, Acute Toxicity, and Structure–Toxicity Relationship in Series of Synthesized 1-Aryltetrahydroisoquinoline Alkaloid Derivatives In Vivo and In Silico

by Azizbek A. Azamatov, Sherzod N. Zhurakulov, Valentina I. Vinogradova, Firuza Tursunkhodzhaeva, Roaa M. Khinkar, Rania T. Malatani, Mohammed M. Aldurdunji, Antonio Tiezzi and Nilufar Z. Mamadalieva

Molecules 2023, 28(2), 477; https://doi.org/10.3390/molecules28020477 - 04 Jan 2023

Cited by 4 | Viewed by 1562

Abstract

Isoquinoline alkaloids constitute one of the most common classes of alkaloids that have shown a pronounced role in curing various diseases. Finding ways to reduce the toxicity of these molecules and to increase their therapeutic margin is an urgent matter. Here, a one-step method for the synthesis of a series of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines was performed in 85–98% yield by the Pictet–Spengler reaction. This was accomplished using the reaction between 3,4-dimethoxyphenylethylamine and substituted benzaldehydes boiling in trifluoroacetic acid. Furthermore, 1-(3′-amino-, 4′-aminophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines were obtained in 94% and 97% yield by reduction in 1-(3′-nitro-, 4′-nitrophenyl)-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines with SnCl₂ × 2H₂O. The structures of the substances obtained were confirmed by infrared (IR) and nuclear magnetic resonance (¹H and ¹³C NMR) spectra. ADMET/TOPKAT in silico study concluded that the synthesized compounds exhibited acceptable pharmacodynamic and pharmacokinetic properties without carcinogenic or mutagenic potential but with variable hepatotoxicity. The acute toxicity and structure–toxicity relationship (STR) in the series of 20 derivatives of 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolines (3a–r, 4a, b) was studied via determination of acute toxicity and resorptive action in white mice employing intragastric step-by-step administration. The first compound, 1-phenyl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3a), showed the highest toxicity with LD₅₀ of 280 mg/kg in contrast to 1-(3′-bromo -4′-hydroxyphenyl)-6,7-methylenedioxy-1,2,3,4-tetrahydroisoquinoline hydrochloride (3e) which proved to be the safest of the compounds studied. Its toxicity was 13.75 times lower than that of the parent compound 3a. All compounds investigated showed high local anesthetic activity on rabbit eyes in the concentrations studied. Only 3r, 3n, and 4a caused eye irritation and redness. All investigated derivatives (except 4b) in 1% concentration were more active than lidocaine, providing longer duration of complete anesthesia. Therefore, based on the obtained results of in silico tests, local anesthesia, and acute toxicity, a conclusion can be drawn that the experimental compounds need further extensive future investigations and possible modifications so that they can act as promising drug candidates. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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10 pages, 619 KiB

Open AccessCommunication

Benzochromenopyrimidines: Synthesis, Antiproliferative Activity against Colorectal Cancer and Physicochemical Properties

by Emna Choura, Fares Elghali, Paul J. Bernard, Dhouha Msalbi, José Marco-Contelles, Sami Aifa, Lhassane Ismaili and Fakher Chabchoub

Molecules 2022, 27(22), 7878; https://doi.org/10.3390/molecules27227878 - 15 Nov 2022

Cited by 3 | Viewed by 1170

Abstract

Ten new differently substituted 3-benzyl-5-aryl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidin-4,6,11-triones 3 were synthesized by a simple and cost-efficient procedure in a one-pot, three-component reaction from readily available ethyl 2-amino-4-aryl-5,10-dioxo-5,10-dihydro-4H-benzo[g]chromene-3-carboxylates, benzylamine and triethyl orthoformate under solvent- and catalyst-free conditions. All the new compounds were screened for their antiproliferative activity against two colorectal-cancer-cell lines. The results showed that the compounds 3-benzyl-5-phenyl-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3a) and 3-benzyl-5-(3-hydroxyphenyl)-3,5-dihydro-4H-benzo[6,7]chromeno[2,3-d]pyrimidine-4,6,11-trione (3g) exhibited the most potent balanced inhibitory activity against human LoVo and HCT-116 cancer cells. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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29 pages, 5830 KiB

Open AccessArticle

Synthesis and Cytotoxic Activity of 1,2,4-Triazolo-Linked Bis-Indolyl Conjugates as Dual Inhibitors of Tankyrase and PI3K

by Prasanna A. Yakkala, Samir R. Panda, Syed Shafi, V. G. M. Naidu, M. Shahar Yar, Philemon N. Ubanako, Samson A. Adeyemi, Pradeep Kumar, Yahya E. Choonara, Eugene V. Radchenko, Vladimir A. Palyulin and Ahmed Kamal

Molecules 2022, 27(21), 7642; https://doi.org/10.3390/molecules27217642 - 07 Nov 2022

Cited by 8 | Viewed by 1721

Abstract

A series of new 1,2,4-triazolo-linked bis-indolyl conjugates (15a–r) were prepared by multistep synthesis and evaluated for their cytotoxic activity against various human cancer cell lines. It was observed that they were more susceptible to colon and breast cancer cells. Conjugates 15o (IC₅₀ = 2.04 μM) and 15r (IC₅₀ = 0.85 μM) illustrated promising cytotoxicity compared to 5-fluorouracil (5-FU, IC₅₀ = 5.31 μM) against the HT-29 cell line. Interestingly, 15o and 15r induced cell cycle arrest at the G₀/G₁ phase and disrupted the mitochondrial membrane potential. Moreover, these conjugates led to apoptosis in HT-29 at 2 μM and 1 μM, respectively, and also enhanced the total ROS production as well as the mitochondrial-generated ROS. Immunofluorescence and Western blot assays revealed that these conjugates reduced the expression levels of the PI3K-P85, β-catenin, TAB-182, β-actin, AXIN-2, and NF-κB markers that are involved in the β-catenin pathway of colorectal cancer. The results of the in silico docking studies of 15r and 15o further support their dual inhibitory behaviour against PI3K and tankyrase. Interestingly, the conjugates have adequate ADME-toxicity parameters based on the calculated results of the molecular dynamic simulations, as we found that these inhibitors (15r) influenced the conformational flexibility of the 4OA7 and 3L54 proteins. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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17 pages, 5539 KiB

Open AccessArticle

Structure and Computational Studies of New Sulfonamide Compound: {(4-nitrophenyl)sulfonyl}tryptophan

by Florence Uchenna Eze, Chigozie Julius Ezeorah, Blessing Chinweotito Ogboo, Obinna Chibueze Okpareke, Lydia Rhyman, Ponnadurai Ramasami, Sunday Nwankwo Okafor, Groutso Tania, Simeon Atiga, Thomas Ugochukwu Ejiyi, Mirabel Chinasa Ugwu, Chiamaka Peace Uzoewulu, Jude Ikechukwu Ayogu, Ogechi Chinelo Ekoh and David Izuchukwu Ugwu

Molecules 2022, 27(21), 7400; https://doi.org/10.3390/molecules27217400 - 31 Oct 2022

Cited by 1 | Viewed by 2544

Abstract

Synthesis of sulfonamide through an indirect method that avoids contamination of the product with no need for purification has been carried out using the indirect process. Here, we report the synthesis of a novel sulfonamide compound, ({4-nitrophenyl}sulfonyl)tryptophan (DNSPA) from 4-nitrobenzenesulphonylchloride and L-tryptophan precursors. The slow evaporation method was used to form single crystals of the named compound from methanolic solution. The compound was characterized by X-ray crystallographic analysis and spectroscopic methods (NMR, IR, mass spectrometry, and UV-vis). The sulfonamide N-H NMR signal at 8.07–8.09 ppm and S-N stretching vibration at 931 cm⁻¹ indicate the formation of the target compound. The compound crystallized in the monoclinic crystal system and P2₁ space group with four molecules of the compound in the asymmetric unit. Molecular aggregation in the crystal structure revealed a 12-molecule aggregate synthon sustained by O-H⋯O hydrogen bonds and stabilised by N-H⋯O intermolecular contacts. Experimental studies were complemented by DFT calculations at the B3LYP/6-311++G(d,p) level of theory. The computed structural and spectroscopic data are in good agreement with those obtained experimentally. The energies of interactions between the units making up the molecule were calculated. Molecular docking studies showed that DNSPA has a binding energy of −6.37 kcal/mol for E. coli DNA gyrase (5MMN) and −6.35 kcal/mol for COVID-19 main protease (6LU7). Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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9 pages, 1421 KiB

Open AccessArticle

Synthesis of Novel α-Trifluorothioanisole Derivatives Containing Phenylpyridine Moieties with Herbicidal Activity

by Zengfei Cai, Wenliang Zhang, Zhongjie Yan and Xiaohua Du

Molecules 2022, 27(18), 5879; https://doi.org/10.3390/molecules27185879 - 10 Sep 2022

Cited by 1 | Viewed by 1262

Abstract

To discover novel herbicidal compounds with favorable activity, a range of phenylpyridine-moiety-containing α-trifluorothioanisole derivatives were designed, synthesized, and identified via NMR and HRMS. Preliminary screening of greenhouse-based herbicidal activity revealed that compound 5a exhibited >85% inhibitory activity against broadleaf weeds Amaranthus retroflexus, Abutilon theophrasti, and Eclipta prostrate at 37.5 g a.i./hm², which was slightly superior to that of fomesafen. The current study suggests that compound 5a could be further optimized as an herbicide candidate to control various broadleaf weeds. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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Review

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31 pages, 3456 KiB

Open AccessReview

A Review of Biologically Active Oxime Ethers

by Tomasz Kosmalski, Daria Kupczyk, Szymon Baumgart, Renata Paprocka and Renata Studzińska

Molecules 2023, 28(13), 5041; https://doi.org/10.3390/molecules28135041 - 28 Jun 2023

Cited by 3 | Viewed by 1356

Abstract

Oxime ethers are a class of compounds containing the >C=N-O-R moiety. The presence of this moiety affects the biological activity of the compounds. In this review, the structures of oxime ethers with specific biological activity have been collected and presented, and bactericidal, fungicidal, antidepressant, anticancer and herbicidal activities, among others, are described. The review includes both those substances that are currently used as drugs (e.g., fluvoxamine, mayzent, ridogrel, oxiconazole), as well as non-drug structures for which various biological activity studies have been conducted. To the best of our knowledge, this is the first review of the biological activity of compounds containing such a moiety. The authors hope that this review will inspire scientists to take a greater interest in this group of compounds, as it constitutes an interesting research area. Full article

(This article belongs to the Special Issue Design, Synthesis and Biological Activity of Organic Compounds)

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