4.7 Article

Synthesis and biological evaluation of some novel cyclic-imides as hypoglycaemic, anti-hyperlipidemic agents

Journal

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 46, Issue 9, Pages 4324-4329

Publisher

ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.07.002

Keywords

Synthesis; Isoindolinediones; Tetrahydro-methyl-isoindolediones; Hypoglycaemic; Anti-hyperlipidemic agents

Funding

  1. King Saud University [RGP-VPP-037]

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Certain new halogenated cyclic-imides related to N-substituted phthalimide moiety were synthesized. Spacers of one or two carbon atom distances were inserted to connect the N-terminus of the cyclic-imide nuclei to the used heteroaryl groups to evaluate the effect of such alteration on biological activity. The synthesized compounds were subjected to hypoglycaemic and anti-hyperlipidemic evaluation. Some of the tested compounds proved to be more potent than the reference drugs glibenclamide and clofibrate. Compound Se remarkably reduced serum glucose level by 55%; while 5c, Se, 7d and 8e reduced total serum cholesterol by 58, 56, 54 and 53%, respectively. Those new cyclic-imides could be considered as useful template for future development to obtain more potent hypoglycaemic and anti-hyperlipidemic agents. (C) 2011 Elsevier Masson SAS. All rights reserved.

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Lipton, T. Liu, C. Madrid, K. Maeshima, C. Mantilla, D. Mason, P. McBride, P. Merkel, S. Mrenna, S. Nahn, J. Ngadiuba, D. Noonan, V. Papadimitriou, N. Pastika, K. Pedro, C. Pena, F. Ravera, A. Reinsvold Hall, L. Ristori, E. Sexton-Kennedy, N. Smith, A. Soha, L. Spiegel, S. Stoynev, J. Strait, L. Taylor, S. Tkaczyk, N. V. Tran, L. Uplegger, E. W. Vaandering, H. A. Weber, I. Zoi, P. Avery, D. Bourilkov, L. Cadamuro, V. Cherepanov, R. D. Field, D. Guerrero, M. Kim, E. Koenig, J. Konigsberg, A. Korytov, K. H. Lo, K. Matchev, N. Menendez, G. Mitselmakher, A. Muthirakalayil Madhu, N. Rawal, D. Rosenzweig, S. Rosenzweig, K. Shi, J. Wang, Z. Wu, T. Adams, A. Askew, R. Habibullah, V. Hagopian, T. Kolberg, G. Martinez, H. Prosper, C. Schiber, O. Viazlo, R. Yohay, J. Zhang, M. M. Baarmand, S. Butalla, T. Elkafrawy, M. Hohlmann, R. Kumar Verma, M. Rahmani, F. Yumiceva, M. R. Adams, H. Becerril Gonzalez, R. Cavanaugh, S. Dittmer, O. Evdokimov, C. E. Gerber, D. J. Hofman, D. S. Lemos, A. H. Merrit, C. Mills, G. Oh, T. Roy, S. Rudrabhatla, M. B. Tonjes, N. Varelas, X. Wang, Z. Ye, J. Yoo, M. Alhusseini, K. Dilsiz, L. Emediato, R. P. Gandrajula, G. Karaman, O. K. Koseyan, J. -P. Merlo, A. Mestvirishvili, J. Nachtman, O. Neogi, H. Ogul, Y. Onel, A. Penzo, C. Snyder, E. Tiras, O. Amram, B. Blumenfeld, L. Corcodilos, J. Davis, A. V. Gritsan, S. Kyriacou, P. Maksimovic, J. Roskes, S. Sekhar, M. Swartz, T. A. Vami, A. Abreu, L. F. Alcerro Alcerro, J. Anguiano, P. Baringer, A. Bean, Z. Flowers, T. Isidori, J. King, G. Krintiras, M. Lazarovits, C. Le Mahieu, C. Lindsey, J. Marquez, N. Minafra, M. Murray, M. Nickel, C. Rogan, C. Royon, R. Salvatico, S. Sanders, C. Smith, Q. Wang, J. Williams, G. Wilson, B. Allmond, S. Duric, A. Ivanov, K. Kaadze, D. Kim, Y. Maravin, T. Mitchell, A. Modak, K. Nam, D. Roy, F. Rebassoo, D. Wright, E. Adams, A. Baden, O. Baron, A. Belloni, A. Bethani, S. C. Eno, N. J. Hadley, S. Jabeen, R. G. Kellogg, T. Koeth, Y. Lai, S. Lascio, A. C. Mignerey, S. Nabili, C. Palmer, C. Papageorgakis, L. Wang, K. Wong, D. Abercrombie, W. Busza, I. A. Cali, Y. Chen, M. D'Alfonso, J. Eysermans, C. Freer, G. Gomez-Ceballos, M. Goncharov, P. Harris, M. Hu, D. Kovalskyi, J. Krupa, Y. -J. Lee, K. Long, C. Mironov, C. Paus, D. Rankin, C. Roland, G. Roland, Z. Shi, G. S. F. Stephans, J. Wang, Z. Wang, B. Wyslouch, T. J. Yang, R. M. Chatterjee, B. Crossman, A. Evans, J. Hiltbrand, Sh. Jain, B. M. Joshi, C. Kapsiak, M. Krohn, Y. Kubota, J. Mans, M. Revering, R. Rusack, R. Saradhy, N. Schroeder, N. Strobbe, M. A. Wadud, L. M. Cremaldi, K. Bloom, M. Bryson, D. R. Claes, C. Fangmeier, L. Finco, F. Golf, C. Joo, R. Kamalieddin, I. Kravchenko, I. Reed, J. E. Siado, G. R. Snow, W. Tabb, A. Wightman, F. Yan, A. G. Zecchinelli, G. Agarwal, H. Bandyopadhyay, L. Hay, I. Iashvili, A. Kharchilava, C. McLean, M. Morris, D. Nguyen, J. Pekkanen, S. Rappoccio, A. Williams, G. Alverson, E. Barberis, Y. Haddad, Y. Han, A. Krishna, J. Li, J. Lidrych, G. Madigan, B. Marzocchi, D. M. Morse, V. Nguyen, T. Orimoto, A. Parker, L. Skinnari, A. Tishelman-Charny, T. Wamorkar, B. Wang, A. Wisecarver, D. Wood, S. Bhattacharya, J. Bueghly, Z. Chen, A. Gilbert, K. A. Hahn, Y. Liu, N. Odell, M. H. Schmitt, M. Velasco, R. Band, R. Bucci, M. Cremonesi, A. Das, R. Goldouzian, M. Hildreth, K. Hurtado Anampa, C. Jessop, K. Lannon, J. Lawrence, N. Loukas, L. Lutton, J. Mariano, N. Marinelli, I. Mcalister, T. McCauley, C. Mcgrady, K. Mohrman, C. Moore, Y. Musienko, R. Ruchti, A. Townsend, M. Wayne, H. Yockey, M. Zarucki, L. Zygala, B. Bylsma, M. Carrigan, L. S. Durkin, B. Francis, C. Hill, M. Joyce, A. Lesauvage, M. Nunez Ornelas, K. Wei, B. L. Winer, B. R. Yates, F. M. Addesa, P. Das, G. Dezoort, P. Elmer, A. Frankenthal, B. Greenberg, N. Haubrich, S. Higginbotham, A. Kalogeropoulos, G. Kopp, S. Kwan, D. Lange, D. Marlow, K. Mei, I. Ojalvo, J. Olsen, D. Stickland, C. Tully, S. Malik, S. Norberg, A. S. Bakshi, V. E. Barnes, R. Chawla, S. Das, L. Gutay, M. Jones, A. W. Jung, D. Kondratyev, A. M. Koshy, M. Liu, G. Negro, N. Neumeister, G. Paspalaki, S. Piperov, A. Purohit, J. F. Schulte, M. Stojanovic, J. Thieman, F. Wang, R. Xiao, W. Xie, J. Dolen, N. Parashar, D. Acosta, A. Baty, T. Carnahan, M. Decaro, S. Dildick, K. M. Ecklund, P. J. Fernandez Manteca, S. Freed, P. Gardner, F. J. M. Geurts, A. Kumar, W. Li, B. P. Padley, R. Redjimi, J. Rotter, W. Shi, S. Yang, E. Yigitbasi, L. Zhang, Y. Zhang, A. Bodek, P. de Barbaro, R. Demina, J. L. Dulemba, C. Fallon, T. Ferbel, M. Galanti, A. Garcia-Bellido, O. Hindrichs, A. Khukhunaishvili, E. Ranken, R. Taus, G. P. Van Onsem, K. Goulianos, B. Chiarito, J. P. Chou, Y. Gershtein, E. Halkiadakis, A. Hart, M. Heindl, D. Jaroslawski, O. Karacheban, I. Laflotte, A. Lath, R. Montalvo, K. Nash, M. Osherson, H. Routray, S. Salur, S. Schnetzer, S. Somalwar, R. Stone, S. A. Thayil, S. Thomas, H. Wang, H. Acharya, A. G. Delannoy, S. Fiorendi, T. Holmes, E. Nibigira, S. Spanier, O. Bouhali, M. Dalchenko, A. Delgado, R. Eusebi, J. Gilmore, T. Huang, T. Kamon, H. Kim, S. Luo, S. Malhotra, R. Mueller, D. Overton, D. Rathjens, A. Safonov, N. Akchurin, J. Damgov, V. Hegde, K. Lamichhane, S. W. Lee, T. Mengke, S. Muthumuni, T. Peltola, I. Volobouev, A. Whitbeck, E. Appelt, S. Greene, A. Gurrola, W. Johns, A. Melo, F. Romeo, P. Sheldon, S. Tuo, J. Velkovska, J. Viinikainen, B. Cardwell, B. Cox, G. Cummings, J. Hakala, R. Hirosky, A. Ledovskoy, A. Li, C. Neu, C. E. Perez Lara, B. Tannenwald, P. E. Karchin, N. Poudyal, S. Banerjee, K. Black, T. Bose, S. Dasu, I. De Bruyn, P. Everaerts, C. Galloni, H. He, M. Herndon, A. Herve, C. K. Koraka, A. Lanaro, A. Loeliger, R. Loveless, J. Madhusudanan Sreekala, A. Mallampalli, A. Mohammadi, S. Mondal, G. Parida, D. Pinna, A. Savin, V. Shang, V. Sharma, W. H. Smith, D. Teague, H. F. Tsoi, W. Vetens, S. Afanasiev, V. Andreev, Yu. Andreev, T. Aushev, M. Azarkin, A. Babaev, A. Belyaev, V. Blinov, E. Boos, V. Borshch, D. Budkouski, V. Bunichev, V. Chekhovsky, R. Chistov, A. Dermenev, T. Dimova, I. Dremin, M. Dubinin, L. Dudko, V. Epshteyn, A. Ershov, G. Gavrilov, V. Gavrilov, S. Gninenko, V. Golovtcov, N. Golubev, I. Golutvin, I. Gorbunov, A. Gribushin, V. Ivanchenko, Y. Ivanov, V. Kachanov, L. Kardapoltsev, V. Karjavine, A. Karneyeu, V. Kim, M. Kirakosyan, D. Kirpichnikov, M. Kirsanov, V. Klyukhin, O. Kodolova, D. Konstantinov, V. Korenkov, A. Kozyrev, N. Krasnikov, E. Kuznetsova, A. Lanev, P. Levchenko, A. Litomin, N. Lychkovskaya, V. Makarenko, A. Malakhov, V. Matveev, V. Murzin, A. Nikitenko, S. Obraztsov, A. Oskin, I. Ovtin, V. Palichik, P. Parygin, V. Perelygin, S. Petrushanko, S. Polikarpov, V. Popov, E. Popova, O. Radchenko, M. Savina, V. Savrin, D. Selivanova, V. Shalaev, S. Shmatov, S. Shulha, Y. Skovpen, S. Slabospitskii, V. Smirnov, D. Sosnov, V. Sulimov, E. Tcherniaev, A. Terkulov, O. Teryaev, I. Tlisova, M. Toms, A. Toropin, L. Uvarov, A. Uzunian, E. Vlasov, A. Vorobyev, N. Voytishin, B. S. Yuldashev, A. Zarubin, I. Zhizhin, A. Zhokin

Summary: In this study, a search for vector-like T and B quark-antiquark pairs produced in proton-proton collisions was conducted using data collected by the CMS experiment at the CERN LHC. The analysis included single-lepton, same-sign charge dilepton, and multilepton channels to classify events. The results showed that the data are consistent with standard model background predictions, and the production of vector-like quark pairs is excluded for certain mass ranges.

JOURNAL OF HIGH ENERGY PHYSICS (2023)

Article Chemistry, Multidisciplinary

Discovery of new pyridine heterocyclic hybrids; design, synthesis, dynamic simulations, and in vitro and in vivo breast cancer biological assays

Menna M. Abdelshaheed, Hussein I. El Subbagh, Mohamed A. Tantawy, Reem T. Attia, Khairia M. Youssef, Iten M. Fawzy

Summary: Pyridine is a versatile nitrogen-containing heterocycle that shows a wide range of biological activities and has become a target of interest for medicinal chemistry researchers. In this study, novel pyridine derivatives were designed, synthesized, and evaluated for their anticancer abilities both in vitro and in vivo. The compounds exhibited significant cytotoxic activities against different human cancer cell lines and showed superior antiproliferative activities compared to Taxol. In addition, the most potent compounds were able to inhibit tubulin polymerization and molecular modeling studies confirmed their essential binding interactions.

RSC ADVANCES (2023)

Article Chemistry, Medicinal

Multi-targeted anti-Alzheimer's agents: Synthesis, biological evaluation, and molecular modeling study of some pyrazolopyridine hybrids

Omnia M. Waly, Selwan M. El-Sayed, Mariam A. Ghaly, Hussein I. El-Subbagh

Summary: A series of compounds with a pyrazolopyridine scaffold were synthesized as multi-targeted ligands for the treatment of Alzheimer's disease (AD). Compounds 49 and 51 exhibited potent inhibition against hAChE and hBuChE, as well as GSK3 beta. They also showed significant inhibition of tau protein aggregation and A beta(1-42) self-aggregation. Additionally, these compounds were able to chelate bio-metals and penetrate the blood-brain barrier. They could be considered as potential multi-targeted drugs for AD patients, and the substitution pattern obtained in this study could guide the development of new anti-Alzheimer's agents.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2023)

Article Chemistry, Medicinal

Highly potent dual-targeting angiotensin-converting enzyme 2 (ACE2) and Neuropilin-1 (NRP1) peptides: A promising broad-spectrum therapeutic strategy against SARS-CoV-2 infection

Shuang Mei, Su Jiang, Yuting Wang, Han Jing, Peng Yang, Miao-Miao Niu, Jindong Li, Kai Yuan, Yan Zhang

Summary: This study identifies a dual-targeting peptide, AP-1, that effectively inhibits variants of concern (VOCs) of SARS-CoV-2 without impairing host cell viability. The findings suggest that AP-1 could be a promising broad-spectrum agent for treating emerging VOCs of SARS-CoV-2.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

Discovery of proteolysis-targeting chimera targeting undruggable proteins using a covalent ligand screening approach

Hyeonjun Lee, Ju Yeon Lee, Hyunsoo Jang, Hye Young Cho, Minhee Kang, Sang Hyun Bae, Suin Kim, Eunji Kim, Jaebong Jang, Jin Young Kim, Young Ho Jeon

Summary: By using liquid chromatography-tandem mass spectrometry and nuclear magnetic resonance experiments, we identified new chemical moieties that bind to the target sites of the protein of interest, allowing for reversible binding and protein degradation. This method has the potential to expand the application of PROTAC technology.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

A pro-death autophagy-based nanoplatform for enhancing antitumour efficacy with improved immune responses

Yingying Li, Xiyou Du, Xinru Kong, Yuelin Fang, Zhijing He, Dongzhu Liu, Hang Wu, Jianbo Ji, Xiaoye Yang, Lei Ye, Guangxi Zhai

Summary: This study proposes a novel nanoplatform based on the autophagy cascade to overcome the obstacles in chemo-immunotherapy. The platform combines chemotherapy and starvation therapy to initiate pro-death autophagy and enhance antigen presentation, while also remodeling the immunosuppressive tumor microenvironment. Furthermore, the study discovers a new therapeutic direction for the respiration inhibitor 3-bromopyruvic acid (3BP) in cancer treatment. Overall, this study offers an opportunity to improve antitumor efficacy and boost immune responses.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

A novel scaffold long-acting selective estrogen receptor antagonist and degrader with superior preclinical profile against ER plus breast cancer

Bingsi Wang, Mingxu Ma, Yusen Dai, Pengfei Yu, Liang Ye, Wenyan Wang, Chunjie Sha, Huijie Yang, Yingjie Yang, Yunjing Zhu, Lin Dong, Shujuan Wei, Linlin Wang, Jingwei Tian, Hongbo Wang

Summary: Breast cancer is a common malignant tumor in women, and drug resistance remains a clinical challenge. In this study, a novel compound, G-5b, was developed with potent antagonistic and degradation activities comparable to the current drug fulvestrant. G-5b also showed improved stability and solubility. Mechanistically, G-5b engages the proteasome pathway to degrade ER, inhibiting the ER signaling pathway and inducing apoptosis and cell cycle arrest. In animal models, G-5b exhibited superior pharmacokinetics and pharmacodynamics properties. Overall, G-5b is a promising long-acting SERD worthy of further investigation and optimization.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

HDAC specificity and kinase off-targeting by purine-benzohydroxamate anti-hematological tumor agents

Karoline B. Waitman, Larissa C. de Almeida, Marina C. Primi, Jorge A. E. G. Carlos, Claudia Ruiz, Thales Kronenberger, Stefan Laufer, Marcia Ines Goettert, Antti Poso, Sandra V. Vassiliades, Vinicius A. M. de Souza, Monica F. Z. J. Toledo, Neuza M. A. Hassimotto, Michael D. Cameron, Thomas D. Bannister, Leticia Costa-Lotufo, Joa o A. Machado-Neto, Mauricio T. Tavares, Roberto Parise-Filho

Summary: A series of hybrid inhibitors combining pharmacophores of known kinase inhibitors and benzohydroxamate HDAC inhibitors were synthesized and evaluated for their anticancer activity and pharmacokinetic properties. Compounds 4d-f exhibited promising cytotoxicity against hematological cells and moderate activity against solid tumor models. Compound 4d showed potent inhibition of multiple kinase targets and had stable interactions with HDAC and members of the JAK family. These compounds showed selective cytotoxicity with minimal effects on non-tumorigenic cells and favorable pharmacokinetic profiles.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

Unexpected rearrangement of ivermectin in the synthesis of new derivatives with trypanocidal and antiplasmodial activities

Michal Sulik, Diana Fontinha, Dietmar Steverding, Szymon Sobczak, Michal Antoszczak, Miguel Prudencio, Adam Huczynski

Summary: This study describes the synthesis of the first-in-class ivermectin derivatives obtained through derivatization of the C13 position, along with the unexpected rearrangement of the macrolide ring. These derivatives show potential for antiparasitic activity and are important for the development of new antiparasitic agents.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

Novel ligustilide derivatives target quorum sensing system LasR/LasB and relieve inflammatory response against Pseudomonas aeruginosa infection

Jun Liu, Qiu-Xian Chen, Wen-Fu Wu, Dong Wang, Si -Yu Zhao, Jia-Hao Li, Yi-Qun Chang, Shao-Gao Zeng, Jia-Yi Hu, Yu-Jie Li, Jia-Xin Du, Shu-Meng Jiao, Hai-Chuan Xiao, Qiang Zhang, Jun Xu, Jian-Fu Zhao, Hai -Bo Zhou, Yong-Heng Wang, Jian Zou, Ping-Hua Sun

Summary: A new anti-infective drug strategy has been discovered to attenuate virulence and modulate inflammation caused by drug-resistant Pseudomonas aeruginosa infections. Compound 5f inhibits biofilm formation, macrophage migration, and inflammatory response induced by P. aeruginosa, showing potential as a novel candidate against drug-resistant infections.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

Design and synthesis of pterostilbene derivatives bearing triazole moiety that might treat DSS-induced colitis in mice through modulation of NF-KB/ MAPK signaling pathways

Liuzeng Chen, Ke Wang, Lingyun Wang, Wei Wang, Lifan Wang, Jia Li, Xiaohan Liu, Mengya Wang, Banfeng Ruan

Summary: In this study, a series of novel anti-inflammatory compounds were designed and synthesized based on the natural product pterostilbene skeleton. Among them, compound 8 showed the highest activity and exhibited its effects through inhibition of pro-inflammatory cytokines by blocking the NF-KB/MAPK signaling pathway. Compound 8 also demonstrated a good relieving effect on acute colitis in mice and showed good safety in acute toxicity experiments.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)

Article Chemistry, Medicinal

Discovery of 4-(N-dithiobenzyl piperazine)-1,8-naphthalimide as a potent multi-target antitumor agent with good efficacy, limited toxicity, and low resistance

Si-Min Liang, Gui-Bin Liang, Hui-Ling Wang, Hong Jiang, Xian-Li Ma, Jian-Hua Wei, Ri-Zhen Huang, Ye Zhang

Summary: A series of novel multi-target antitumor agents were designed, synthesized, and evaluated. Some compounds exhibited significant antitumor activity and one compound showed excellent efficacy, limited toxicity, and low resistance. Further mechanism studies revealed that the compound exerted antitumor effects through multiple pathways.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2024)