Article
Chemistry, Multidisciplinary
Geraldo Jose da Silva Neto, Leandro Rocha Silva, Rafael Jorge Melo de Omena, Anna Caroline Campos Aguiar, Yasmin Annunciato, Barbara Santos Rossetto, Marcos Leoni Gazarini, Luana Heimfarth, Lucindo Jose Quintans-Junior, Edeildo Ferreira da Silva-Junior, Mario Roberto Meneghetti
Summary: Although current drugs are available for malaria treatment, the development of resistant strains of the parasite calls for the need of new drugs. This study synthesized four dual pharmaceutical compounds with potential antimalarial and anti-inflammatory activities, with DEQ showing the highest activity and IBUCEQ and TOQ being the most promising candidates.
NEW JOURNAL OF CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Bishnu Prasad Raiguru, Jasmine Panda, Seetaram Mohapatra, Sabita Nayak
Summary: Malaria continues to be a global burden in the 21st century, causing significant economic troubles to disease-endemic nations. Developing novel antimalarial drugs has become an urgent need in order to control and eradicate malaria. This review summarizes the developments of hybrid antimalarial agents from 2017 to the present, highlighting their synthesis and evaluation to identify the most potent hybrids. It provides valuable information for the scientific community in the development of new antimalarial drugs to combat malaria.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Medicinal
Thomas Tremblay, Catherine Bergeron, Dominic Gagnon, Christopher Berube, Normand Voyer, Dave Richard, Denis Giguere
Summary: A series of squaramide tethered chloroquine, clindamycin, and mortiamide D hybrids were synthesized and tested for their in vitro antiplasmodial activity against Plasmodium falciparum strains. The most active compound, a chloroquine analogue, showed low nanomolar IC50 values against both strains. Hybrids incorporating the hydroxychloroquine scaffold exhibited potent activities, with a chloroquine dimer as the most promising hit. These findings provide valuable insights for further optimization in the development of antimalarial drugs.
ACS MEDICINAL CHEMISTRY LETTERS
(2023)
Article
Multidisciplinary Sciences
Arne Alder, Cecilia P. Sanchez, Matthew R. G. Russell, Lucy M. Collinson, Michael Lanzer, Michael J. Blackman, Tim-Wolf Gilberger, Joachim M. Matz
Summary: Malaria parasites use a complex to acidify the digestive vacuole and degrade host erythrocyte hemoglobin, which is essential for their survival in the human bloodstream.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Plant Sciences
Emmanuel O. Adeyoju, Clement O. Ajayi, Awodayo O. Adepiti, Anthony A. Elujoba
Summary: This study compared the antimalarial activity of methanol and water extracts of MAMA Powder against Plasmodium berghei-infected mice, finding that the water extract exhibited higher efficacy and can be optimized for chloroquine-resistant malaria, aiding in the production of various dosage forms.
JOURNAL OF ETHNOPHARMACOLOGY
(2022)
Article
Chemistry, Multidisciplinary
Benita Kapuku, Fadi Baakdah, Elias Georges, D. Scott Bohle
Summary: The synthesis and characterization of new chloroquine derivatives and their antimalarial activity were investigated. The results showed that 4-substituted chloroquine derivatives with electron-withdrawing groups have the lowest IC50 values and exhibit good activity against resistant strains. Among them, the 4-chlorobenzamido-chloroquine derivative was selected as a potential lead compound for combination therapy.
CANADIAN JOURNAL OF CHEMISTRY
(2023)
Article
Pharmacology & Pharmacy
Anne Cristine Almeida, Anna Beatriz Ribeiro Elias, Maria Paula Marques, Gisely Cardoso de Melo, Allyson Guimaraes da Costa, Erick Frota Gomes Figueiredo, Larissa Wanderley Brasil, Fernanda Rodrigues-Soares, Wuelton Marcelo Monteiro, Marcus Vinicius Guimaraes de Lacerda, Vera Lucia Lanchote, Guilherme Suarez-Kurtz
Summary: The study investigated the impact of Plasmodium vivax malaria and chloroquine-primaquine chemotherapy on CYP2D6 and CYP2C19 activity in patients from the Brazilian Amazon. Results showed alterations in CYP2D6 and CYP2C19 metabolic phenotypes, potentially due to changes in pharmacokinetics and cytokine levels during different stages of vivax malaria illness and treatment.
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY
(2021)
Article
Chemistry, Medicinal
Chhuttan L. Meena, Tejashri Hingamire, Tanya Gupta, Bhagyashree Deshmukh, Krishanpal Karmodiya, Rakesh Joshi, Dhanasekaran Shanmugam, Gangadhar J. Sanjayan
Summary: We synthesized peptide-histidinal conjugated drug scaffolds that can target falcipain-2/3 hemoglobin-degrading proteases from the malaria parasite. Various substitutions were tested and compounds 8g, 8h, and 15 showed strong antimalarial activity. Docking studies revealed that these compounds interacted strongly with the binding sites of falcipain-2/3. ADME studies showed that the molecules of interest had good drug-likeness properties. These findings provide a starting point for the development of potential antimalarial drug candidates.
Article
Infectious Diseases
Laurent Dembele, Yaw Aniweh, Nouhoum Diallo, Fanta Sogore, Cheick Papa Oumar Sangare, Aboubecrin Sedhigh Haidara, Aliou Traore, Seidina A. S. Diakite, Mahamadou Diakite, Brice Campo, Gordon A. Awandare, Abdoulaye A. Djimde
Summary: The study found that P. malariae showed reduced ex vivo susceptibility to chloroquine, lumefantrine, and artemether, while exhibiting strong inhibition with piperaquine exposure. Additionally, new antimalarial compounds such as imidazolopiperazines and the PI4K-specific inhibitor showed promising inhibitory effects against P. malariae.
JOURNAL OF ANTIMICROBIAL CHEMOTHERAPY
(2021)
Review
Chemistry, Medicinal
Loeki Enggar Fitri, Aulia Rahmi Pawestri, Nuning Winaris, Agustina Tri Endharti, Alif Raudhah Husnul Khotimah, Hafshah Yasmina Abidah, John Thomas Rayhan Huwae
Summary: Malaria elimination is targeted to be achieved by 2030 in Indonesia, but the development and spread of antimalarial resistance poses a significant risk to the national malaria control programs. Resistance has been reported in two human species of Plasmodium, P. falciparum and P. vivax. Understanding the mechanisms of antimalarial drugs and their development of resistance could provide insights for designing future treatment guidelines and control programs in Indonesia.
DRUG DESIGN DEVELOPMENT AND THERAPY
(2023)
Article
Rheumatology
Ziyi Jin, Fan Wang, Wenyou Pan, Lin Liu, Min Wu, Huaixia Hu, Xiang Ding, Hua Wei, Yaohong Zou, Xian Qian, Meimei Wang, Jian Wu, Juan Tao, Jun Tan, Zhanyun Da, Miaojia Zhang, Jing Li, Xuebing Feng, Lingyun Sun
Summary: The study showed that antimalarial drugs were associated with a lower mortality risk in SLE patients, especially in cases of renal insufficiency and other organ involvement-related deaths. The protective effects on survival may be enhanced by adherence to and full dosage of these drugs.
Article
Integrative & Complementary Medicine
Mihret Ayalew, Azmeraw Bekele
Summary: This study evaluated the antimalarial activity of crude extract of Eucalyptus globulus Labill. leaf in Plasmodium berghei-infected mice. The results demonstrated that the extract significantly suppressed parasitemia, increased survival time, and prevented body weight loss and decrease in packed cell volume. The findings support the traditional use and in vitro test results of the plant.
EVIDENCE-BASED COMPLEMENTARY AND ALTERNATIVE MEDICINE
(2021)
Article
Pharmacology & Pharmacy
Pawan Sharma, Kielan D. McAlinden, Saeid Ghavami, Deepak A. Deshpande
Summary: The usage of chloroquine and its derivatives, known for their safety profile, in the treatment of COVID-19 has the potential to open up a new therapeutic approach. However, further clinical studies are needed to validate their efficacy in this regard.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Amad Uddin, Meenal Chawla, Iram Irfan, Shubhra Mahajan, Shailja Singh, Mohammad Abid
Summary: Resistance of traditional antimalarial drugs remains a challenge, leading to the search for novel lead molecules. Artemisinin-based combination therapy is the WHO-recommended first-line treatment, while hybrid molecules offer a new strategy for the development of next-generation antimalarial drugs.
RSC MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Sewan Theeramunkong, Artitiya Thiengsusuk, Opa Vajragupta, Phunuch Muhamad
Summary: This study presents the synthesis of novel decorated isoquinolines as potential antimalarial agents and evaluates their activity against resistant and sensitive strains of P. falciparum. Compound 6 and compound 15 showed promising antiplasmodial activity, with compound 15 being particularly effective against the resistant strain. These results contribute to further lead discovery and modification in rational drug design.
MEDICINAL CHEMISTRY RESEARCH
(2021)
Article
Biochemistry & Molecular Biology
F. Stanly Pradeep, M. Palaniswamy, S. Ravi, A. Thangamani, B. V. Pradeep
PROCESS BIOCHEMISTRY
(2015)
Article
Chemistry, Medicinal
Sulaiman Ali Muhammad, Subban Ravi, Arumugam Thangamani
MEDICINAL CHEMISTRY RESEARCH
(2016)
Article
Chemistry, Applied
Raju Sripathi, Dharani Jayagopal, Subban Ravi
NATURAL PRODUCT RESEARCH
(2018)
Article
Chemistry, Multidisciplinary
Sulaiman Ali Muhammad, Subban Ravi, Arumugam Thangamani, Balakumar Chandrasekaran, M. Ramesh
RESEARCH ON CHEMICAL INTERMEDIATES
(2017)
Article
Chemistry, Multidisciplinary
Sulaiman Ali Muhammad, Arumgam Thangamani, Subban Ravi
RESEARCH ON CHEMICAL INTERMEDIATES
(2017)
Article
Biochemistry & Molecular Biology
K. R. Jayanthi, K. Hemapriya, Subban Ravi
Summary: In an attempt to challenge COVID-19, molecular docking was used to study the association between cinnamoylated chloroquine compounds and the main protease enzyme of SARS-CoV-2. Compound 5 showed stable interactions with the protein and has potential as a starting point for drug discovery.
ORIENTAL JOURNAL OF CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
K. R. Jayanthi, S. Ravi
Summary: This study presents a two-step synthesis method for target compounds and evaluates their anticancer activity against breast cancer cell lines. Certain compounds exhibit potent anticancer activity and are non-toxic to normal cells.
ORIENTAL JOURNAL OF CHEMISTRY
(2022)
Article
Chemistry, Organic
Velliangiri Prabhu, Subban Ravi
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY
(2017)
Article
Chemistry, Organic
Srinivasan Govindarajapuram Varadarajan, Vijayan Kochukarattu Krishnan, Ravi Subban
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY
(2017)
Article
Pharmacology & Pharmacy
Kathirvel Poonkodi, Subban Ravi
BANGLADESH JOURNAL OF PHARMACOLOGY
(2016)
Article
Multidisciplinary Sciences
Stephen Kumar Celestina, Kaveri Sundaram, Subban Ravi
RESEARCH JOURNAL OF PHARMACEUTICAL BIOLOGICAL AND CHEMICAL SCIENCES
(2015)
Article
Biochemistry & Molecular Biology
G. M. V. N. A. R. Ravi Kumar, Thangamani Arumugam, Venkata Reddy Gayam, Ravi Subban
ORIENTAL JOURNAL OF CHEMISTRY
(2017)
Article
Pharmacology & Pharmacy
Palanisamy Chella Perumal, Sundaram Sowmya, Prabhakaran Pratibha, Balasubramanian Vidya, Palanirajan Anusooriya, Thangarajan Starlin, Subban Ravi, Velliyur Kanniappan Gopalakrishnan
PHARMACOGNOSY RESEARCH
(2015)
Article
Chemistry, Medicinal
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
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
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
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
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
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
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
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
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)