Article
Chemistry, Physical
Sabrina Halit, Amina Benazzouz-Touami, Malika Makhloufi-Chebli, Souhila Terrachet Bouaziz, Karima Ighilahriz, Anthony Robert, Carine Machado-Rodrigues
Summary: A new series of compounds with antioxidant and antifungal activities were synthesized. Compounds 3d and 3e showed promising antifungal activity, with 3e exhibiting potential inhibitory activity against Aspergillus niger. Molecular docking studies suggested that compound 3e may act as a potential antifungal agent.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Infectious Diseases
Carmen Molina-Torres, Carlos Pedraza-Rodriguez, Lucio Vera-Cabrera, Jorge Ocampo-Candiani, Catalina Rivas-Morales, Ezequiel Viveros-Valdez
Summary: Tuberculosis (TB) is still a major global health problem, with antibiotic-resistant strains posing the greatest challenge to its treatment. Additionally, the prevalence of non-tuberculous mycobacteria (NTM) in humans has significantly increased in recent years. This study aims to investigate the antimycobacterial effects of extracts and major compounds from Hedeoma drummondii on both clinical isolates of Mycobacterium tuberculosis and NTM strains. The methanolic extract exhibited the best activity against M. tuberculosis, inhibiting 10 out of 12 strains at a concentration < 2500 mu g/mL, while the hexanic extract showed the best activity against NTM, inhibiting 8 out of 10 strains at <= 625 mu g/mL. Furthermore, there was a strong positive correlation between the antimycobacterial activity of pulegone and the hexanic extract against NTM strains, suggesting its potential as a predictive marker for these microorganisms.
Article
Chemistry, Medicinal
Daria Elzbieta Nawrot, Ghada Bouz, Ondrsi Jandourek, Klara Konecna, Pavla Paterova, Pavel Barta, Martin Novak, Radim Kucera, Julia Zemanova, Martin Forbak, Jana Kordulakova, Oto Pavlis, Pavla Kubickova, Martin Dolezal, Jan Zitko
Summary: Tuberculosis, caused by Mycobacterium tuberculosis (Mtb), is the leading cause of death among infectious diseases caused by a single microbe. With the emergence of antimicrobial resistance, the success rate of treating this infection is decreasing, and there is an urgent need for novel treatments. In this study, a novel series of compounds inspired by combining fragments from first-line and second-line agents for tuberculosis were synthesized and evaluated. Compound 10c from the second series showed selective and potent antimycobacterial activity against both drug-sensitive and drug-resistant Mtb strains, with no cytotoxicity. The compound targeted methionine metabolism rather than the folate pathway and had a long half-life, overcoming the limitations of current drugs for tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Multidisciplinary
Esmeralda Ivonne Nino-Padilla, Clara Espitia, Carlos Velazquez, Efrain Alday, Erika Silva-Campa, Alexel Burgara-Estrella, Jose Antonio Enciso-Moreno, Olivia Valenzuela, Humberto Astiazaran-Garcia, Adriana Garibay-Escobar
Summary: This study evaluated the potential antibiofilm activity of Rhynchosia precatoria compounds against Mycobacterium bovis BCG. The compound precatorin A (PreA) showed the strongest biofilm inhibitory activity, preventing the formation of biofilms by BCG. However, neither PreA nor the extract showed bactericidal effects.
Article
Biochemistry & Molecular Biology
Boddupalli Venkata Siva Kumar, Yogesh Mahadu Khetmalis, Adinarayana Nandikolla, Banoth Karan Kumar, Kevin Van Calster, Sankaranarayanan Murugesan, Davie Cappoen, Kondapalli Venkata Gowri Chandra Sekhar
Summary: A series of novel 2-substituted-5,7-dichloro-1,2,3,4-tetrahydroisoquinoline-6-carbohydrazide derivatives were synthesized and evaluated for their anti-mycobacterial activity against Mycobacterium tuberculosis. Compound 10A25 containing biphenyl moiety exhibited significant inhibition with IC50 4.7 μM, while compound 10A19 with an electron-withdrawing Iodo group showed significant anti-tubercular activity with IC50 8.8 μM. Molecular docking study of the active compound 10A25 was performed to determine its binding position at the active site of the selected target proteins.
CHEMISTRY & BIODIVERSITY
(2023)
Article
Biophysics
Sandra Montalvo-Quiros, Sergio Gomez-Grana, Maria Vallet-Regi, Rafael C. Prados-Rosales, Blanca Gonzalez, Jose L. Luque-Garcia
Summary: Tuberculosis remains a major public health issue with a lack of effective vaccine and the emergence of highly antibiotic-resistant strains of Mycobacterium tuberculosis. Silver nanoparticles show high bactericidal efficacy, but their relatively high toxicity calls for the design of nanocarriers for safe delivery. Mesoporous silica nanoparticles have been used as carriers for silver nanoparticles as antimycobacterial agents, demonstrating good capability against Mtb with different synthetic approaches.
COLLOIDS AND SURFACES B-BIOINTERFACES
(2021)
Article
Biochemistry & Molecular Biology
Ting Li, Chaoyue Yang, Houkang Cao, Siyi Mo, Bo Li, Zhipeng Huang, Ruobing Zhang, Jianzhao Wu, Kefeng Zhang, Ya Gao
Summary: Bergenin (BER) can alleviate liver injury induced by isonicotinic acid hydrazide (INH) and rifampicin (RIF) by regulating drug metabolism enzymes, bile acid metabolism, Nrf2 pathway, and TLR4 pathway.
Article
Biotechnology & Applied Microbiology
M. E. F. A. G. Oliveira, Y. J. A. Silva, L. A. Azevedo, L. A. Linhares, L. M. L. Montenegro, S. Alves Jr, R. V. S. Amorim
Summary: The study investigated the adjuvant effect of chitosan with the drug ethambutol as a compound, demonstrating a promising composite against strains Mtb H37Rv and multidrug resistant tuberculosis. The CS-EMB compound showed increased antibacterial activity and cytotoxicity compared to the isolated EMB, making it a potential therapeutic option for drug-resistant tuberculosis.
APPLIED MICROBIOLOGY AND BIOTECHNOLOGY
(2021)
Article
Plant Sciences
Frederikke D. Andersen, Katja D. Pedersen, Dennis Wilkens Juhl, Tobias Mygind, Paul Chopin, Esben B. Svenningsen, Thomas B. Poulsen, Marie Braad Lund, Andreas Schramm, Charlotte H. Gotfredsen, Thomas Torring
Summary: This study reveals that triculamin and alboverticillin, two natural products with potent and specific activity against mycobacteria, are actually the same lasso peptide. By determining the structure using 2D NMR spectroscopy and exploring the bioactivity, we found that their precursor peptides have a follower instead of a leader peptide, which is different from known lasso peptides.
JOURNAL OF NATURAL PRODUCTS
(2022)
Article
Chemistry, Multidisciplinary
Mohamed H. Assaleh, Snezana K. Bjelogrlic, Nevena Prlainovic, Ilija Cvijetic, Aleksandra Bozic, Irena Arandjelovic, Dragana Vukovic, Aleksandar Marinkovic
Summary: A series of novel hybrids of cinnamic acid and thiocarbohydrazones were synthesized and evaluated for their impact against Mycobacterium tuberculosis (Mtb) and cancer cells. Compound 3 demonstrated strong anti-Mtb activity while not affecting HepG-2 cells. Compounds 2a and 3b showed different inductions of apoptosis and cellular mobility in cancer cells.
ARABIAN JOURNAL OF CHEMISTRY
(2022)
Review
Biochemistry & Molecular Biology
Ali A. Rabaan, Saad Alhumaid, Hawra Albayat, Mohammed Alsaeed, Fadwa S. Alofi, Mawaheb H. Al-Howaidi, Safaa A. Turkistani, Salah M. Alhajri, Hejji E. Alahmed, Abdulwahab B. Alzahrani, Mutaib M. Mashraqi, Sara Alwarthan, Mashael Alhajri, Fatimah S. Alshahrani, Souad A. Almuthree, Roua A. Alsubki, Abdulmonem A. Abuzaid, Mubarak Alfaresi, Mona A. Al Fares, Abbas Al Mutair
Summary: Tuberculosis (TB) caused by Mycobacterium tuberculosis (Mtb) is a bacterial disease that has caused billions of deaths in the past two centuries. Drug resistance has become a major obstacle in the eradication of TB, highlighting the need for new drugs. Small molecule-based treatments, such as flavonoids, show potential in overcoming drug resistance and inhibiting non-tubercular mycobacterial organisms.
Article
Infectious Diseases
Sorasak Intorasoot, Amornrat Intorasoot, Arocha Tawteamwong, Bordin Butr-Indr, Ponrut Phunpae, Chayada Sitthidet Tharinjaroen, Usanee Wattananandkul, Sirikwan Sangboonruang, Jiaranai Khantipongse
Summary: D-hLF 1-11 exhibits antimycobacterial activity against drug-sensitive and drug-resistant Mycobacterium tuberculosis strains, showing potential as a novel treatment option for tuberculosis infections in the future.
Article
Chemistry, Medicinal
Pengfei Geng, Xiaoqiao Hong, Xueyuan Li, Dianmo Ni, Gang Liu
Summary: This study successfully developed a new fluorescent probe through structure-fluorescence relationships investigation, which can specifically label and detect live Mycobacterium tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2022)
Article
Chemistry, Medicinal
Sh A. Shomurotov, O. R. Akhmedov, A. S. Turaev, G. Kh Mamadullaev
Summary: The newly prepared conjugate containing isonicotinic acid hydrazide and ethambutol exhibited pronounced antituberculosis activity in vitro and in vivo, with the active substances persisting longer in blood compared to their low-molecular-mass analogs, indicating a prolonged antituberculosis effect.
PHARMACEUTICAL CHEMISTRY JOURNAL
(2021)
Article
Chemistry, Medicinal
Bhaiyyasaheb Harale, Saqib Kidwai, Divya Ojha, Manisha Singh, Dwarika Kumar Chouhan, Ramandeep Singh, Vijay Khedkar, Ambadas B. Rode
Summary: Riboflavin derivatives showed promising antimycobacterial activity, with compound 5a being a lead candidate due to its potency and low toxicity. These compounds may exert their antimycobacterial effects through inhibition of riboflavin biosynthesis pathway via FMN riboswitch.
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2021)
Article
Chemistry, Organic
Sivanandhan Karunanidhi, Rajshekhar Karpoormath, Milan Bera, Rajesh A. Rane, Mahesh B. Palkar
JOURNAL OF HETEROCYCLIC CHEMISTRY
(2016)
Review
Biochemistry & Molecular Biology
Girish A. Hampannavar, Rajshekhar Karpoormath, Mahesh B. Palkar, Mahamadhanif S. Shaikh
BIOORGANIC & MEDICINAL CHEMISTRY
(2016)
Article
Chemistry, Medicinal
Girish A. Hampannavar, Rajshekhar Karpoormath, Mahesh B. Palkar, Mahamadhanif S. Shaikh, Balakumar Chandrasekaran
ACS MEDICINAL CHEMISTRY LETTERS
(2016)
Article
Food Science & Technology
Malleswara R. Peram, Sunil S. Jalalpure, Mahesh B. Palkar, Prakash V. Diwan
FOOD SCIENCE AND BIOTECHNOLOGY
(2017)
Article
Biochemical Research Methods
Malleswara Rao Peram, Sunil S. Jalalpure, Sumit A. Joshi, Mahesh B. Palkar, Prakash V. Diwan
JOURNAL OF LIQUID CHROMATOGRAPHY & RELATED TECHNOLOGIES
(2017)
Article
Chemistry, Medicinal
Mahesh B. Palkar, Aniket Patil, Girish A. Hampannavar, Mahamadhanif S. Shaikh, Harun M. Patel, Ashish M. Kanhed, Mange Ram Yadav, Rajshekhar V. Karpoormath
MEDICINAL CHEMISTRY RESEARCH
(2017)
Article
Chemistry, Multidisciplinary
Rajesh A. Rane, Mukesh Nandave, Suresh Nayak, Anushri Naik, Dhwani Shah, Wesam S. Alwan, Niteshkumar U. Sahu, Shital S. Naphade, Mahesh B. Palkar, Sivanandhan Karunanidhi, Neeta Thapliyal, Rajshekhar Karpoormath
ARABIAN JOURNAL OF CHEMISTRY
(2017)
Article
Chemistry, Medicinal
Mahesh B. Palkar, D. M. Praveen, Pradeepkumar M. Ronad, A. H. M. Viswanathswamy, Rajesh A. Rane, Harun M. Patel, Mahamadhanif S. Shaikh, Girish A. Hampannavar, Kavita S. Jain, Rajshekhar Karpoormath
MEDICINAL CHEMISTRY RESEARCH
(2015)
Article
Chemistry, Medicinal
Mahamadhanif S. Shaikh, Ashish M. Kanhed, Balakumar Chandrasekaran, Mahesh B. Palkar, Nikhil Agrawar, Christian Lherbet, Girish A. Hampannavar, Rajshekhar Karpoormath
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
(2019)
Article
Biochemistry & Molecular Biology
Mahamadhanif S. Shaikh, Balakumar Chandrasekaran, Mahesh B. Palkar, Ashish M. Kanhed, Afsana Kajee, Koleka P. Mlisana, Parvesh Singh, Meenu Ghai, Mavela Cleopus Mahlalela, Rajshekhar Karpoormath
CHEMISTRY & BIODIVERSITY
(2020)
Article
Biochemistry & Molecular Biology
Harun M. Patel, Mahesh Palkar, Rajshekhar Karpoormath
CHEMISTRY & BIODIVERSITY
(2020)
Article
Chemistry, Physical
Girish Bolakatti, Mahesh Palkar, Manjunatha Katagi, Girish Hampannavar, Rajshekhar Karpoormath, Shilpa Ninganagouda, Arvind Badiger
Summary: A novel series of benzo[d]thiazolyl substituted-2-quinolone hybrids were synthesized, showing significant cytotoxicity against cancer cells, especially compound 8f. Docking studies revealed important binding interactions of compounds 8f and 7f with EGFR tyrosine kinase. Additionally, compounds 7e, 7f, 8e, and 8f exhibited antibacterial activity, particularly against E. coli.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Review
Chemistry, Medicinal
Pankaj S. Girase, Sanjeev Dhawan, Vishal Kumar, Suraj R. Shinde, Mahesh B. Palkar, Rajshekhar Karpoormath
Summary: Piperazine, a nitrogen-containing heterocyclic compound, is widely used in medicinal chemistry for its diverse pharmacological activities, particularly in the development of anti-TB molecules. Studies have shown that molecules containing piperazine subunits exhibit potential activity against drug-resistant strains of Mycobacterium tuberculosis.
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
(2021)
Review
Chemistry, Organic
Suraj R. Shinde, Pankaj Girase, Sanjeev Dhawan, Shaukatali N. Inamdar, Vishal Kumar, Chandrakant Pawar, Mahesh B. Palkar, Mahadev Shinde, Rajshekhar Karpoormath
Summary: 1,3-Oxazole is an important class of heterocyclic compounds with wide-ranging applications. In recent years, there has been an increase in research articles exploring the synthesis and applications of 1,3-oxazole derivatives. However, there is currently no specific review on this topic. This review aims to comprehensively interpret the literature on metal catalytic strategies for 1,3-oxazole derivatives and assist organic chemists in overcoming challenges in the methods.
SYNTHETIC COMMUNICATIONS
(2022)
Article
Chemistry, Organic
Alisha Dream Soares, Shivalingrao N. Mamle Desai, Priyanka Tiwari, Mahesh B. Palkar, Sunil G. Shingade, Bheemanagouda Biradar
INDIAN JOURNAL OF CHEMISTRY SECTION B-ORGANIC CHEMISTRY INCLUDING MEDICINAL CHEMISTRY
(2019)
