Article
Chemistry, Medicinal
Rashmika Moodley, Chakes Mashaba, Goitsemodimo H. Rakodi, Nomagugu B. Ncube, Mabuatsela Maphoru, Mohammed O. Balogun, Audrey Jordan, Digby F. Warner, Rene Khan, Matshawandile Tukulula
Summary: A series of new benzothiazole-urea-quinoline hybrid compounds were successfully synthesized and evaluated for their anti-tuberculosis activity. Some of the compounds showed promising activity and low cytotoxicity. The results indicate that these compounds could serve as valuable starting points for the development of new anti-Mycobacterium tuberculosis agents.
Article
Biochemistry & Molecular Biology
Nisheeth C. Desai, Ghanshyam M. Kotadiya, Krunalsinh A. Jadeja, Keyur N. Shah, Alimamad H. Malani, Vijjulatha Manga, Tamalapakula Vani
Summary: By synthesizing quinoline bearing dihydropyrimidine analogues, promising results have been achieved in terms of structure determination and molecular properties prediction, with compound 5m showing excellent anti-tubercular activity and drug-likeness.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Stefano Zoroddu, Paola Corona, Luca Sanna, Federica Borghi, Valentina Bordoni, Battistina Asproni, Gerard A. Pinna, Luigi Bagella, Gabriele Murineddu
Summary: A library of novel 1,3,4-oxadiazole bioisosteres was synthesized and evaluated for their cytotoxic activity. Several of the new compounds showed potent anticancer activity, surpassing the previously synthesized oxadiazole compound. The nature of the selenadiazole and thiadiazole rings may play a crucial role in the antitumor activity. These compounds exhibited strong cytotoxic effects in tumor cells compared to human primary cells.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Nisheeth C. Desai, Kandarp Bhatt, Jahnvi Monapara, Unnat Pandit, Vijay M. Khedkar
Summary: Microwave-assisted organic reaction enhancement (MORE) is becoming increasingly important in synthetic organic chemistry for efficient resource utilization. The microwave-assisted synthesis method allows for quicker synthesis with higher yields and better quality compounds compared to traditional methods.
Article
Biochemistry & Molecular Biology
Bin-Long Sun, Ying-Ying Wang, Sen Yang, Min-Ting Tu, Ying-Ying Shao, Yi Hua, Yi Zhou, Cheng-Xia Tan
Summary: New compounds with high fungicidal activity were designed and synthesized, and their biological activities were evaluated. These compounds showed excellent inhibitory activity against fungi, surpassing the activity of existing fungicides. Furthermore, their fungicidal activity against the target fungi was better than that of existing fungicides, and one of the compounds exhibited low toxicity.
Article
Chemistry, Physical
Shaikh Faazil, M. Shaheer Malik, Saleh A. Ahmed, Qazi Mohammad Sajid Jamal, Shaikh Thoukhir Basha, Munirah M. Al-Rooqi, Rami J. Obaid, Jihan Qurban, Iqbal N. Shaikh, Basim H. Asghar, Ahmed Kamal
Summary: This study reports the design and synthesis of a series of new quinoline-thiolactone conjugates as potential antitubercular and antibacterial agents. Two of the conjugates showed good antitubercular activity, while two others exhibited decent antibacterial activity. Docking studies confirmed their good binding affinity towards the target proteins.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Ana Flavia Borsoi, Laura Manzoli Alice, Nathalia Sperotto, Alessandro Silva Ramos, Bruno Lopes Abbadi, Fernanda Souza Macchi Hopf, Adilio da Silva Dadda, Raoni S. Rambo, Rodrigo Braccini Madeira Silva, Josiane Delgado Paz, Kenia Pissinate, Mauro Neves Muniz, Christiano Ev Neves, Luiza Galina, Laura Calle Gonzalez, Marcia Alberton Perello, Alexia de Matos Czeczot, Mariana Leyser, Silvia Dias de Oliveira, Graziela de Araujo Lock, Bibiana Verlindo de Araujo, Teresa Dalla Costa, Cristiano Valim Bizarro, Luiz Augusto Basso, Pablo Machado
Summary: A novel series of 2-(quinoline-4-yloxy)acetamides were synthesized and evaluated as inhibitors of Mycobacterium tuberculosis (Mtb) growth. The compounds showed selective and potent antitubercular activity against drug-sensitive and drug-resistant Mtb strains. They targeted the cytochrome bc(1) complex and inhibited Mtb growth in a macrophage model. The leading compound demonstrated good stability, solubility, permeability, and a promising pharmacokinetic profile after oral administration in mice.
ACS MEDICINAL CHEMISTRY LETTERS
(2022)
Article
Chemistry, Medicinal
Tamer M. Ibrahim, Ghada Abada, Marcel Dammann, Raed M. Maklad, Wagdy M. Eldehna, Rofaida Salem, Marwa M. Abdelaziz, Ramadan A. El-domany, Adnan A. Bekhit, Frank M. Beockler
Summary: Derivatives with tetrahydrobenzo[h]quinoline chemotype were synthesized and evaluated for their antileishmanial, antimalarial and antitubercular activities. These compounds were designed to possess antileishmanial activity through antifolate mechanism, targeting Leishmania major pteridine reductase 1 (Lm-PTR1). They showed promising in vitro activity against Leishmania parasites, Plasmodium berghei, and Mycobacterium tuberculosis. Molecular docking and simulations supported their mechanisms of action. This work introduces a potential solution for treating Neglected Tropical Diseases with drug resistance issues.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Biochemistry & Molecular Biology
Mashooq A. Bhat, Ahmed M. Naglah, Siddique Akber Ansari, Hanaa M. Al-Tuwajiria, Abdullah Al-Dhfyan
Summary: This study developed an environmentally friendly method using A ChCl: Gly (DESs) to synthesize xanthene analogues from aryl aldehydes and dimedone, showcasing excellent antimycobacterial activity. The compounds showed significant antitubercular activity with low toxicity against various cell lines, confirming their potential as new drug candidates for tuberculosis treatment.
Review
Chemistry, Medicinal
Vladimir Finger, Martin Kufa, Ondrej Soukup, Daniele Castagnolo, Jaroslav Roh, Jan Korabecny
Summary: This review provides an overview of recent advances in the hit-to-lead drug discovery studies of pyrimidine-containing compounds with antitubercular activity, focusing on their structural diversity. The review discusses the targets and structure-activity relationships of different pyrimidine families in the first part and categorizes unexplored or speculative targets of antitubercular pyrimidine derivatives based on their structural types in the second part.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Review
Chemistry, Medicinal
Atukuri Dorababu
Summary: Although most heterocycles have significant pharmacological activities, only a few quinoline derivatives exhibit the best biological activities, including anticancer, anti-inflammatory, antibacterial, antiviral, and antifungal activities. Therefore, designing more efficient antimicrobial drugs is a priority to prevent malevolent microbial diseases.
ARCHIV DER PHARMAZIE
(2021)
Article
Biochemistry & Molecular Biology
Robert Murnane, Mire Zloh, Sangeeta Tanna, Renee Allen, Felipe Santana-Gomez, Tanya Parish, Federico Brucoli
Summary: A library of 4-substituted quinolines was synthesized based on the structure of 4-(benzylthio)-6-methoxy-2-methylquinoline scaffold, which have shown effective anti-tuberculosis activity. The novel quinoline analogues exhibited significant growth inhibitory activity against wild-type MTB and depleted intracellular ATP. The cytochrome bc1 oxidase complex was identified as the molecular target. Interestingly, a new quinoline derivative showed increased selectivity for a specific mutant strain.
BIOORGANIC CHEMISTRY
(2023)
Article
Chemistry, Physical
B. Gandhi, M. Jhansi, S. S. Deshpande, T. Vinay, S. Misra, Shiva Shanker Kaki
Summary: A series of 1,3,4-oxadiazole based 1-monoacylglycerol derivatives were synthesized and evaluated for their antimicrobial and anticancer activity. The derivatives showed noticeable inhibition on selected bacterial and fungal strains as well as broad spectrum cytotoxicity against various cell lines. These lipidic oxadiazole derivatives hold potential as promising antitumor agents and further studies can be conducted to design analogs with improved therapeutic effects.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Apeng Wang, Shijie Xu, Yun Chai, Guimin Xia, Bin Wang, Kai Lv, Dan Wang, Xiaoyu Qin, Bin Jiang, Wenhao Wu, Mingliang Liu, Yu Lu
Summary: The structure-activity relationship study of novel nitrofuran-1,3,4-oxadiazole hybrids as anti-TB agents showed that linkers and substituents greatly influence the activity, with substituted benzenes being more favored. The optimal compound in series 2 demonstrated strong activity against both MTB strains and low toxicity, indicating its potential as a lead compound for further development.
BIOORGANIC & MEDICINAL CHEMISTRY
(2022)
Article
Biochemistry & Molecular Biology
Elmas Begum Cakmak, Belma Zengin Kurt, Dilek Ozturk Civelek, Andrea Angeli, Atilla Akdemir, Fatih Sonmez, Claudiu T. Supuran, Mustafa Kucukislamoglu
Summary: Carbonic anhydrase (CA) IX and XII isoforms are highly expressed in various human tissues and cancers, with CA IX being a prominent target due to its overexpression in hypoxic tumors. A study synthesized and characterized twenty-seven novel compounds with inhibitory activities against CA I, CA II, CA IX, and CA XII isoforms, among which compound 2m showed the highest inhibition against hCA IX. Furthermore, compounds 3a, 3e, and 3f exhibited the most cytotoxic effects across different cell lines.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Medicinal
Shibin Zhao, Julian Maceren, Mia Chung, Samantha Stone, Raphael Geiben, Melissa L. Boby, Bradley S. Sherborne, Derek S. Tan
Summary: Antibiotic resistance is a major threat to public health, with Gram-negative bacteria presenting unique challenges due to their low permeability and efflux pumps. Limited understanding of the chemical rules for overcoming these barriers hinders antibacterial drug discovery. Efforts to address this issue, such as screening compound libraries and using cheminformatic analysis, have led to the design of sulfamidoadenosines with diverse substituents, showing potential utility in accumulation in Escherichia coli.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Jichun Li, Qing Li, Shuai Xia, Jiahuang Tu, Longbo Zheng, Qian Wang, Shibo Jiang, Chao Wang
Summary: This study successfully developed a short peptide mimetic as a MERS-CoV fusion inhibitor by reproducing the key recognition features of the HR2 helix. The resulting 23-mer lipopeptide showed comparable inhibitory effect to the 36-mer HR2 peptide HR2P-M2. This has important implications for developing short peptide-based antiviral agents to treat MERS-CoV infection.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Krista Jaunsleine, Linda Supe, Jana Spura, Sten van Beek, Anna Sandstrom, Jessica Olsen, Carina Halleskog, Tore Bengtsson, Ilga Mutule, Benjamin Pelcman
Summary: Beta(2)-adrenergic receptor agonists can stimulate glucose uptake by skeletal muscle cells and are therefore potential treatments for type 2 diabetes. The chirality of compounds has a significant impact on the activity of these agonists. This study found that certain synthesized compounds showed higher glucose uptake activity. These findings provide important information for the design of novel beta(2)AR agonists for T2D treatment.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Xin Xu, Jia Chen, Guan Wang, Xiaojuan Zhang, Qiang Li, Xiaobo Zhou, Fengying Guo, Min Li
Summary: The study focuses on EZH2, a promising therapeutic target for various types of cancers. Researchers designed and synthesized a series of novel derivatives aiming to enhance the EZH2 inhibition activity. Among them, compound 28 displayed potent EZH2 inhibition activity and showed high anti-proliferative effects in lymphoma cell lines and xenograft mouse models. The study suggests that compound 28 has potential as a therapeutic candidate for EZH2-associated cancers.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Wei Zhang, Wei Liu, Ya-Dong Zhao, Li-Zi Xing, Ji Xu, Rui-Jun Li, Yun-Xiao Zhang
Summary: This study developed a series of aromatic amide derivatives based on Rhein and investigated their inhibitory activity against alpha-Syn aggregation. Two of these compounds showed promising potential in treating Parkinson's disease by stabilizing alpha-Syn's conformation and disassembling alpha-Syn oligomers and fibrils.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)
Article
Chemistry, Medicinal
Mani Sharma, S. S. S. S. Sudha Ambadipudi, Neeraj Kumar Chouhan, V. Lakshma Nayak, Srihari Pabbaraja, Sai Balaji Andugulapati, Ramakrishna Sistla
Summary: Therapeutically active lipids in drug delivery systems can enhance the safety and efficacy of treatment. The liposome formulation created using synthesized biologically active lipids showed additive anti-cancer effects and reduced tumorigenic potential.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2024)