New Analogues of the Nicotinamide Phosphoribosyltransferase Inhibitor FK866 as Potential Anti-Pancreatic Cancer Agents
CONCLUSION: The positive results observed for some newly synthesized molecules, particularly those carrying a thiophene unit as a tail group, indicate that they could act as in vivo anti-pancreatic cancer agents.PMID:38333979 | DOI:10.2174/0115734064289584240121142405 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - February 9, 2024 Category: Chemistry Authors: Irene Conforti Andrea Benzi Irene Caffa Santina Bruzzone Alessio Nencioni Alberto Marra Source Type: research
Heterocyclic-Based Analogues against Sarcine-Ricin Loop RNA from Escherichia coli: In Silico Molecular Docking Study and Machine Learning Classifiers
CONCLUSION: The dataset from the molecular docking study was used for additional optimum analysis, and the molecular descriptors were classified using a variety of machine learning classifiers, including the GB Classifier, CB Classifier, RF Classifier, SV Classifier, KNN Classifier, and Voting Classifier. The research presented here showed that heterocyclic derivatives may operate as potent antibacterial agents when combined with other compounds to produce highly efficient antibacterial agents.PMID:38333980 | DOI:10.2174/0115734064266329231228050535 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - February 9, 2024 Category: Chemistry Authors: Shivangi Sharma Rahul Choubey Manish Gupta Shivendra Singh Source Type: research
Systematic Review On Major Antiviral Phytocompounds from Common Medicinal Plants Against SARS-CoV-2
CONCLUSION: The best advantage is that these phytocompounds being derived from nature in most of the cases, come with minimum or no side effects compared to that of chemically synthesized conventional bioactive compounds and are indigenously available hence are the source of cost effective drug formulations with strong therapeutic potentials.PMID:38317467 | DOI:10.2174/0115734064262843231120051452 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - February 6, 2024 Category: Chemistry Authors: Suvendu Ghosh Partha Singha Lakshmi Kanta Das Debosree Ghosh Source Type: research
Structure-activity Relationship Studies on VEGFR2 Tyrosine Kinase Inhibitors for Identification of Potential Natural Anticancer Compounds
CONCLUSION: The developed QSAR model has identified 5 conserved activity-inducing physiochemical properties, which have been found to be correlated with the anticancer activity of the nonidentical ligand molecules bound with the VEGFR2 kinase. Lavendustin_A, 3’-O-acetylhamaudol, and arctigenin have been obtained as possible lead natural compounds against the VEGFR2 kinase.PMID:38299297 | DOI:10.2174/0115734064247526231129080415 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - February 1, 2024 Category: Chemistry Authors: Meenakshi Verma Aqib Sarfraz Inamul Hasan Prema Gauri Vasudev Feroz Khan Source Type: research
Synthesis, Characterization, and Investigation of Doxorubicin Drug Release Properties of Poly(acrylamide-co-acrylic Acid/Maleic Acid)- Hydroxyapatite Composite Hydrogel
CONCLUSION: It should be inferred that the drug release profile was improved at pH 4.5 by the newly produced pH-sensitive composite hydrogel.PMID:38279756 | DOI:10.2174/0115734064268726231203164405 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 27, 2024 Category: Chemistry Authors: Birnur Akkaya Recep Akkaya Source Type: research
Recent Advances in Nitrogen-Containing Heterocyclic Scaffolds as Antiviral Agents
In conclusion, nitrogen-containing heterocycles are shown to be of utmost importance in the field of medicinal chemistry, as emphasized by the review paper. It emphasizes the central importance of chemical insights and pharmacological potential in developing novel and effective antiviral medicines by bringing them together.PMID:38279757 | DOI:10.2174/0115734064280150231212113012 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 27, 2024 Category: Chemistry Authors: None Kanupriya Ravi K Mittal Vikram Sharma Tanya Biswas Isha Mishra Source Type: research
Oxadiazole Derivatives of Diclofenac as an Anti-proliferative Agent for B-cell Non-Hodgkin Lymphoma: An In vitro and In Silico Studies
CONCLUSION: The compound (II) can be a potential therapeutic candidate for B-cell non-Hodgkin lymphoma and deserves further development as a novel anti-lymphoma agent.PMID:38279758 | DOI:10.2174/0115734064290905231228110023 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 27, 2024 Category: Chemistry Authors: Shaista Qayyum Almas Jabeen Sajda Ashraf Faiza Seraj Khalid Mohammad Khan Rafat Ali Siddiqui None Zaheer Ul-Haq Source Type: research
A Review on the Development of Novel Heterocycles as α-Glucosidase Inhibitors for the Treatment of Type-2 Diabetes Mellitus
Med Chem. 2024 Jan 24. doi: 10.2174/0115734064264591231031065639. Online ahead of print.ABSTRACTOne of the most effective therapeutic decencies in the treatment of Type 2 Diabetes Mellitus is the inhibition of α-glucosidase enzyme, which is present at the brush border of the intestine and plays an important role in carbohydrate digestion to form mono-, di-, and polysaccharides. Acarbose, Voglibose, Miglitol, and Erniglitate have been well-known α-glucosidase inhibitors in science since 1990. However, the long synthetic route and side effects of these inhibitors forced the researchers to move their focus to innovate simpl...
Source: Medicinal Chemistry - January 26, 2024 Category: Chemistry Authors: Prexa Patel Drashti Shah Tushar Bambharoliya Vidhi Patel Mehul Patel Dharti Patel Vashisth Bhavsar Shantilal Padhiyar Bhavesh Patel Anjali Mahavar Riddhisiddhi Patel Ashish Patel Source Type: research
A Review of Antidiabetic Medicinal Plants as a Novel Source of Phosphodiesterase Inhibitors: Future Perspective of New Challenges Against Diabetes Mellitus
Med Chem. 2024 Jan 23. doi: 10.2174/0115734064255060231116192839. Online ahead of print.ABSTRACTIntracellular glucose concentration plays a crucial role in initiating the molecular secretory process of pancreatic β-cells through multiple messengers and signaling pathways. Cyclic nucleotides are key physiological regulators that modulate pathway interactions in β-cells. An increase of cyclic nucleotides is controled by hydrolysed phosphodiesterases (PDEs), which degrades cyclic nucleotides into inactive metabolites. Despite the undeniable therapeutic potential of PDE inhibitors, they are associated with several side effec...
Source: Medicinal Chemistry - January 24, 2024 Category: Chemistry Authors: Hayat Ouassou Nour Elhouda Daoudi Saliha Bouknana Rhizlan Abdenim Mohamed Bnouham Source Type: research
Structure-based Virtual Screening from Natural Products as Inhibitors of SARS-CoV-2 Spike Protein and ACE2-h Receptor Binding and their Biological Evaluation In vitro
CONCLUSION: Compound B-8 can be used as a scaffold to develop new and more efficient antiviral drugs.PMID:38204279 | DOI:10.2174/0115734064279323231206091314 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 11, 2024 Category: Chemistry Authors: Timoteo Delgado-Maldonado Luis Donaldo Gonzalez-Morales Alfredo Juarez-Saldivar Edgar E Lara-Ram írez Guadalupe Rojas-Verde Adriana Rodriguez-Moreno Debasish Bandyopadhyay Gildardo Rivera Source Type: research
Nitrogen-fused Heterocycles: Empowering Anticancer Drug Discovery
This article explores the medicinal chemistry behind these molecules, highlighting their potential as game-changing possibilities for anticancer medication development. The analysis highlights the inherent structural variety in nitrogen-containing heterocycles, revealing their potential to be customized for creating personalized anticancer medications. It also emphasizes the importance of computational techniques and studies on the relationships between structure and activity, providing a road map for rational medication design and optimization. Nitrogen-containing heterocycles are a promising new area of study in the figh...
Source: Medicinal Chemistry - January 9, 2024 Category: Chemistry Authors: Tanya Biswas Ravi K Mittal Vikram Sharma None Kanupriya Isha Mishra Source Type: research
Triple Action of Lignosulfonic Acid Sodium: Anti-protease, Antioxidant, and Anti-inflammatory Effects of a Polymeric Heparin Mimetic
CONCLUSION: Based on these findings, LSAS is put forward as a polymeric heparin mimetic with multiple functions, serving as a potential platform for developing novel therapeutics to treat complex pathologies.PMID:38192144 | DOI:10.2174/0115734064275120231222111145 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 9, 2024 Category: Chemistry Authors: Rami A Al-Horani Kholoud F Aliter Source Type: research
S-Dihydrodaidzein and 3-(1,3-benzoxazol-2-yl)-benzamide, Two New Potential β-estrogen Receptor Ligands with Anti-adipogenic Activity
CONCLUSION: Altogether, these results show the two new potential β-estrogen receptor ligands, C1 and C2, to exhibit anti-adipogenic activity. They could further be used as lead structures for the development of more efficient drugs for obesity control.PMID:38192145 | DOI:10.2174/0115734064285786231230185457 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 9, 2024 Category: Chemistry Authors: Mar ía F Torres-Rojas Gilberto Mandujano-Lazaro Cesar Lopez-Camarillo Esther Ramirez-Moreno Domingo Mendez-Alvarez Gildardo Rivera Laurence A Marchat Source Type: research
Design and Synthesis of 6-amido-3-carboxypyridazine Derivatives as Potent T3SS Inhibitors of Salmonella Enterica Serovar Typhimurium
CONCLUSION: The novel synthetic 6-amido-3-carboxypyridazines could act as potent leads for the development of novel antibacterial agents.PMID:38192146 | DOI:10.2174/0115734064252833231129062005 (Source: Medicinal Chemistry)
Source: Medicinal Chemistry - January 9, 2024 Category: Chemistry Authors: Zhenyu Li Zhiyong Liu Yuemao Shen Chengwu Shen Source Type: research
Nitrogen-fused Heterocycles: Empowering Anticancer Drug Discovery
This article explores the medicinal chemistry behind these molecules, highlighting their potential as game-changing possibilities for anticancer medication development. The analysis highlights the inherent structural variety in nitrogen-containing heterocycles, revealing their potential to be customized for creating personalized anticancer medications. It also emphasizes the importance of computational techniques and studies on the relationships between structure and activity, providing a road map for rational medication design and optimization. Nitrogen-containing heterocycles are a promising new area of study in the figh...
Source: Medicinal Chemistry - January 9, 2024 Category: Chemistry Authors: Tanya Biswas Ravi K Mittal Vikram Sharma None Kanupriya Isha Mishra Source Type: research
