journal
https://read.qxmd.com/read/38523542/trends-in-the-synthesis-of-antimicrobial-derivatives-by-using-the-gewald-strecker-and-groebke-blackburn-bienaym%C3%A3-gbb-reactions
#1
JOURNAL ARTICLE
Kaushal Naithani, Subhendu Bhowmik
BACKGROUND: Multicomponent reactions are highly useful in synthesizing natural products and bioactive molecules. Out of several MCRs, although utilized widely, some remain neglected in review articles. The Gewald and Groebke-Blackburn-Bienaymé (GBB) reactions are two such reactions. This comprehensive review assimilates applications of Gewald and Groebke-Blackburn- Bienayme reactions in synthesizing novel antimicrobial agents. It presents the antimicrobial properties of the synthesized molecules, providing an overview of their potential druggability...
March 20, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38468522/predicting-the-efficacy-of-novel-synthetic-compounds-in-the-treatment-of-osteosarcoma-via-anti-receptor-activator-of-nuclear-factor-%C3%AE%C2%BAb-ligand-rankl-receptor-activator-of-nuclear-factor-%C3%AE%C2%BAb-rank-targets
#2
JOURNAL ARTICLE
Wenhua Zhang, Siping Xu, Peng Liu, Xusheng Li, Xinyuan Yu, Bing Kang
BACKGROUND: Osteosarcoma (OS) currently demonstrates a rising incidence, ranking as the predominant primary malignant tumor in the adolescent demographic. Notwithstanding this trend, the pharmaceutical landscape lacks therapeutic agents that deliver satisfactory efficacy against OS. OBJECTIVE: This study aimed to authenticate the outcomes of prior research employing the HM and GEP algorithms, endeavoring to expedite the formulation of efficacious therapeutics for osteosarcoma...
March 11, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38425108/biochemical-and-in-silico-studies-on-triazole-derivatives-as-tyrosinase-inhibitors-potential-treatment-of-hyperpigmentation-related-skin-disorders
#3
JOURNAL ARTICLE
Yusra Choudhary, Atia-Tul- Wahab, Humaira Zafar, Salman Siddiqui, Majid Khan, Khalid M Khan, Amer H Asseri, M Iqbal Choudhary, Atta-Ur- Rahman
INTRODUCTION: Tyrosinase is a versatile, glycosylated copper-containing oxidase enzyme that mainly catalyzes the biosynthesis of melanin in mammals. Its overexpression leads to the formation of excess melanin, resulting in hyperpigmentary skin disorders, such as dark spots, melasma, freckles, etc. Therefore, inhibition of tyrosinase is a therapeutic approach for the treatment of hyperpigmentation. METHOD: The current study focused on evaluating tyrosinase inhibitory activities of triazole derivatives 1-20, bearing different substituents on the phenyl ring...
February 29, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38351695/synthesis-antimicrobial-evaluation-and-interaction-of-emodin-alkyl-azoles-with-dna-and-hsa
#4
JOURNAL ARTICLE
Yu-Hang Zhou, Ying Wang, Hui-Zhen Zhang
OBJECTIVE: This study aimed to overcome the growing antibiotic resistance. Moreover, the new series of emodin alkyl azoles were synthesized. METHOD: The novel emodin alkyl azoles were synthesized using commercial emodin and azoles by alkylation. The NMR and HRMS spectra were employed to confirm the structures of novel prepared compounds. The in vitro antibacterial and antifungal activities of the prepared emodin compounds were studied by the 96-well plate method...
February 13, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38347768/pharmacochemical-study-of-multitarget-amino-acids-hybrids-design-synthesis-in-vitro-and-in-silico-studies
#5
JOURNAL ARTICLE
Dimitra Hadjipavlou-Litina, Ioannis Fotopoulos, Eleni Pontiki
Neuro-inflammation is a complex phenomenon resulting in several disorders. ALOX-5, COX-2, pro-inflammatory enzymes, and amino acid neurotransmitters are tightly correlated to neuro- inflammatory pathologies. Developing drugs that interfere with these targets will offer treatment for various diseases. Herein, we extend our previous research by synthesizing a series of multitarget hybrids of cinnamic acids with amino acids recognized as neurotransmitters. The synthesis was based on an in silico study of a library of cinnamic amide hybrids with glycine, γ- aminobutyric, and L - glutamic acids...
February 9, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38333980/heterocyclic-based-analogues-against-sarcine-ricin-loop-rna-from-escherichia-coli-in-silico-molecular-docking-study-and-machine-learning-classifiers
#6
JOURNAL ARTICLE
Shivangi Sharma, Rahul Choubey, Manish Gupta, Shivendra Singh
BACKGROUND: Heterocyclic-based drugs have strong bioactivities, are active pharmacophores, and are used to design several antibacterial drugs. Due to the diverse biodynamic properties of well-known heterocyclic cores, such as quinoline, indole, and its derivatives, they have a special place in the chemistry of nitrogen-containing heterocyclic molecules. OBJECTIVE: The objective of this study is to analyze the interaction of several heterocyclic molecules using molecular docking and machine learning approaches to find out the possible antibacterial drugs...
February 7, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38333979/new-analogues-of-the-nicotinamide-phosphoribosyltransferase-inhibitor-fk866-as-potential-anti-pancreatic-cancer-agents
#7
JOURNAL ARTICLE
Irene Conforti, Andrea Benzi, Irene Caffa, Santina Bruzzone, Alessio Nencioni, Alberto Marra
BACKGROUND: During the past two decades, many nicotinamide phosphoribosyltransferase (NAMPT) inhibitors were prepared and tested because this enzyme is overexpressed in pancreatic cancer. Although FK866 is a well-known, strong NAMPT inhibitor, it suffers severe drawbacks. OBJECTIVE: Our work aimed to synthesize efficient NAMPT inhibitors featuring better pharmacokinetic properties than the pyridine-containing FK866. To this aim, the new anticancer agents were based on benzene, pyridazine, or benzothiazole moieties as a cap group instead of the pyridine unit found in FK866 and other NAMPT inhibitors...
February 7, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38299297/structure-activity-relationship-studies-on-vegfr2-tyrosine-kinase-inhibitors-for-identification-of-potential-natural-anticancer-compounds
#8
JOURNAL ARTICLE
Meenakshi Verma, Inamul Hasan, Feroz Khan, Prema G Vasudev
BACKGROUND: Over-expression of vascular endothelial growth factor receptors (VEGFRs) leads to the hyperactivation of oncogenes. For inhibition of this hyperactivation, the USA Food Drug Administration (FDA) has approved many drugs that show adverse effects, such as hypertension, hypothyroidism, etc. There is a need to discover potent natural compounds that show minimal side effects. In the present study, we have taken structurally diverse known VEGFR2 inhibitors to develop a quantitative structure-activity relationship (QSAR) model and used this model to predict the inhibitory activity of natural compounds for VEGFR2...
January 29, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38279758/oxadiazole-derivatives-of-diclofenac-as-an-anti-proliferative-agent-for-b-cell-non-hodgkin-lymphoma-an-in-vitro-and-in-silico-studies
#9
JOURNAL ARTICLE
Shaista Qayyum, Almas Jabeen, Sajda Ashraf, Faiza Seraj, Khalid Mohammad Khan, Rafat Ali Siddiqui, Zaheer Ul-Haq
BACKGROUND: Non-Hodgkin lymphoma of B cell origin is the common type of lymphoma- related malignancy with poor response rate with conventional front-line therapies. AIM: The aim of the present study was to investigate the potential of new anti-inflammatory oxadiazole derivatives of Diclofenac as an anti-lymphoma agent through in vitro and in silico approaches. METHOD: The compound (II) showed anti-lymphoma activity against both follicular and Burkitt's lymphoma cells, whereas compound (V) inhibited follicular lymphoma cells only...
January 25, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38317467/systematic-review-on-major-antiviral-phytocompounds-from-common-medicinal-plants-against-sars-cov-2
#10
JOURNAL ARTICLE
Suvendu Ghosh, Partha Singha, Lakshmi Kanta Das, Debosree Ghosh
UNLABELLED: Viral infections are rising around the globe and with evolving virus types and increasing varieties of viral invasions; the human body is developing antimicrobial resistance continuously. This is making the fight of mankind against viruses weak and unsecured. On the other hand, changing lifestyle, globalization and human activities adversely affecting the environment are opening up risks for new viral predominance on human race. In this context the world has witnessed the pandemic of the human Coronavirus disease (COVID-19) recently...
January 24, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38279757/recent-advances-in-nitrogen-containing-heterocyclic-scaffolds-as-antiviral-agents
#11
JOURNAL ARTICLE
Kanupriya, Ravi K Mittal, Vikram Sharma, Tanya Biswas, Isha Mishra
This study aims to provide a thorough analysis of nitrogen-containing heterocycles, focusing on their therapeutic implications for the development of targeted and effective antiviral drugs. To better understand how nitrogen-containing heterocycles can be used to create antiviral drugs, this review adopts a systematic literature review strategy to compile and analyze pertinent research studies. It combines information from various fields to understand better the compounds' mode of action and their therapeutic potential...
January 24, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38279756/synthesis-characterization-and-investigation-of-doxorubicin-drug-release-properties-of-poly-acrylamide-co-acrylic-acid-maleic-acid-hydroxyapatite-composite-hydrogel
#12
JOURNAL ARTICLE
Birnur Akkaya, Recep Akkaya
BACKGROUND: Hydroxyapatite and its derivatives have been used for a lot of applications. One of them is drug release studies. Due to its low adhesion strength and lack of the strength and durability required for load-carrying applications, there is a need to improve the properties of hydroxyapatite. For this aim, the most important factors are increasing pH sensitivity and preventing coagulation. Mixing it with multifunctional polymers is the best solution. OBJECTIVES: The main objectives are: 1- preparing poly(acrylamide-co-acrylic acid/maleic acid)- hydroxyapatite (PAm-co-PAA/PMA-HApt), 2- assessment of (PAm-co-PAA/PMA-HApt) and dox-loaded poly(acrylamide-co-acrylic acid/maleic acid) (Dox-(PAm-co-PAA/PMA-HApt)) composite hydrogels, and 3- elucidating the difference in behavior of drug release studies between hydroxyapatite (HApt) and poly(acrylamide-co-acrylic acid/maleic acid) composite hydrogels...
January 24, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38275074/a-review-on-the-development-of-novel-heterocycles-as-%C3%AE-glucosidase-inhibitors-for-the-treatment-of-type-2-diabetes-mellitus
#13
JOURNAL ARTICLE
Prexa Patel, Drashti Shah, Tushar Bambharoliya, Vidhi Patel, Mehul Patel, Dharti Patel, Vashisth Bhavsar, Shantilal Padhiyar, Bhavesh Patel, Anjali Mahavar, Riddhisiddhi Patel, Ashish Patel
One 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 simple and small heterocyclic scaffolds that work as excellent α-glucosidase inhibitors...
January 24, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38265379/a-review-of-antidiabetic-medicinal-plants-as-a-novel-source-of-phosphodiesterase-inhibitors-future-perspective-of-new-challenges-against-diabetes-mellitus
#14
JOURNAL ARTICLE
Hayat Ouassou, Nour Elhouda Daoudi, Saliha Bouknana, Rhizlan Abdenim, Mohamed Bnouham
Intracellular 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 effects...
January 23, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38204279/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
#15
JOURNAL ARTICLE
Timoteo Delgado-Maldonado, Luis Donaldo Gonzalez-Morales, Alfredo Juarez-Saldivar, Edgar E Lara-Ramírez, Guadalupe Rojas-Verde, Adriana Rodriguez-Moreno, Debasish Bandyopadhyay, Gildardo Rivera
BACKGROUND: In the last years, severe acute respiratory syndrome coronavirus 2 (SARS-CoV-2) caused more than 760 million infections and 6.9 million deaths. Currently, remains a public health problem with limited pharmacological treatments. Among the virus drug targets, the SARS-CoV-2 spike protein attracts the development of new anti-SARS-CoV-2 agents. OBJECTIVE: The aim of this work was to identify new compounds derived from natural products (BIOFACQUIM and Selleckchem databases) as potential inhibitors of the spike receptor binding domain (RBD)-ACE2h binding complex...
January 9, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38192146/design-and-synthesis-of-6-amido-3-carboxypyridazine-derivatives-as-potent-t3ss-inhibitors-of-salmonella-enterica-serovar-typhimurium
#16
JOURNAL ARTICLE
Zhenyu Li, Zhiyong Liu, Yuemao Shen, Chengwu Shen
BACKGROUND: Salmonella enterica (S. enterica) serovar Typhimurium, an anaerobic enteric pathogene, could cause human and animal diseases ranging from mild gastroenteritis to whole body serious infections. OBJECTIVE: The goal of this paper was to synthesize new 6-amido-3-carboxypyridazine derivatives with different lengths of side chains with the aim of getting potent antibacterial agents. METHODS: Synthesized compounds were analyzed by analytical techniques, such as 1H NMR, 13C NMR spectra, and mass spectrometry...
January 8, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38192145/s-dihydrodaidzein-and-3-1-3-benzoxazol-2-yl-benzamide-two-new-potential-%C3%AE-estrogen-receptor-ligands-with-anti-adipogenic-activity
#17
JOURNAL ARTICLE
María F Torres-Rojas, Gilberto Mandujano-Lazaro, Cesar Lopez-Camarillo, Esther Ramirez-Moreno, Domingo Mendez-Alvarez, Gildardo Rivera, Laurence A Marchat
BACKGROUND: The elucidation of molecular pathways associated with adipogenesis has evidenced the relevance of estrogen and estrogen receptor beta (ERβ). The positive effects of ERβ ligands on adipogenesis, energy expenditure, lipolysis, food intake, and weight loss, make ERβ an attractive target for obesity control. From ligand-based virtual screening, molecular docking, and molecular dynamic simulations, six new likely ERβ ligands (C1 to C6) have been reported with potential for pharmacological obesity treatment...
January 8, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38192144/triple-action-of-lignosulfonic-acid-sodium-anti-protease-antioxidant-and-anti-inflammatory-effects-of-a-polymeric-heparin-mimetic
#18
JOURNAL ARTICLE
Rami A Al-Horani, Kholoud F Aliter
BACKGROUND: Heparins are sulfated glycosaminoglycans that are used as anticoagulants to treat thrombosis. Heparins exhibit other potential therapeutic effects, such as anti-inflammatory, anti-viral, and anti-malarial effects. However, the strong anticoagulant activity of heparins poses a risk of life-threatening bleeding, limiting their therapeutic use for other diseases beyond thrombosis. To exploit the other effects of heparins and eliminate the bleeding risk, we explored an alternative polymer called lignosulfonic acid sodium (LSAS), which acts as a sulfonated heparin mimetic...
January 8, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38192143/nitrogen-fused-heterocycles-empowering-anticancer-drug-discovery
#19
JOURNAL ARTICLE
Tanya Biswas, Ravi K Mittal, Vikram Sharma, Kanupriya, Isha Mishra
The worldwide impact of cancer is further compounded by the constraints of current anticancer medications, which frequently exhibit a lack of selectivity, raise safety apprehensions, result in significant adverse reactions, and encounter resistance mechanisms. The current situation highlights the pressing need to develop novel and more precise anticancer agents that prioritize safety and target specificity. Remarkably, more than 85% of drugs with physiological activity contain heterocyclic structures or at least one heteroatom...
January 8, 2024: Medicinal Chemistry
https://read.qxmd.com/read/38173200/exploring-the-therapeutic-marvels-a-comprehensive-review-on-the-biological-potential-of-quinoline-5-8-dione
#20
JOURNAL ARTICLE
Neetu Agrawal, Dimple Bansal, Shilpi Pathak
Quinoline-5,8-diones, also referred to as 5,8-quinolinediones or quinolinequinones, have been researched extensively for their antiproliferative effects, where they displayed great results. Other than anticancer, they exhibit multiple activities such as antimalarial, antiviral, antibacterial, and antifungal activities. Natural quinolinequinones have also been known for their significant activities. The review highlights the diverse biological activities exhibited by synthetic quinoline- 5,8-diones over the past two decades...
January 3, 2024: Medicinal Chemistry
journal
journal
40990
1
2
Fetch more papers »
Fetching more papers... Fetching...
Remove bar
Read by QxMD icon Read
×

Save your favorite articles in one place with a free QxMD account.

×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"

We want to hear from doctors like you!

Take a second to answer a survey question.