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Medicinal Chemistry

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https://www.readbyqxmd.com/read/29788895/synthesis-of-nucleosides-and-non-nucleosides-based-4-6-disubstituted-2-oxo-dihydropyridine-3-carbonitriles-as-antiviral-agents
#1
Tarek S Ibrahim, Hassan A El-Sayed, Maan T Khayat, Amany M M Al-Mahmoudy, Ahmed H Moustafa, Ayat K Saad El-Deen, Sherif A F Rostom, Siva S Panda
BACKGROUND: Viral diseases are considered main threats that face the humanity worldwide. The emergence of new viruses like influenza viruses emphasizes the significance of designing novel antiviral drugs. METHOD: The aim of this work is to synthesize a new set of nucleoside and non-nucleoside cyanopyridine, characterized and evaluated for their in vitro antiviral properties against various strains. CONCLUSION: More than compounds showed variable antiviral potential against a panel of eighteen DNA and RNA viruses...
May 22, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29737262/design-of-bactericidal-peptides-against-escherichia-coli-o157-h7-pseudomonas-aeruginosa-and-methicillin-resistant-staphylococcus-aureus
#2
Jenniffer Cruz, Paola Rondon, Rodrigo Torres, Mauricio Urquiza, Fanny Guzman, Claudio Alvarez, Maria Angeles Abengozar, Daniel A Sierra, Luis Rivas, Roberto Fernandez-Lafuente, Claudia Ortiz
BACKGROUND: Antimicrobial peptides are on the first line of defense against pathogenic microorganisms of many living beings. These compounds are considered natural antibiotics that can overcome bacterial resistance to conventional antibiotics. Due to this characteristic, new peptides with improved properties are quite appealing for designing new strategies for fighting pathogenic bacteria Methods: Sixteen designed peptides were synthesized using Fmoc chemistry; five of them are new cationic antimicrobial peptides (CAMPs) designed using a genetic algorithm that optimizes the antibacterial activity based on selected physicochemical descriptors and 11 analog peptides derived from these five peptides were designed and constructed by single amino acid substitutions...
May 8, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29669503/evaluation-of-trypanocidal-and-antioxidant-activities-of-a-selected-series-of-3-amidocoumarins
#3
Mauricio Moncada-Basualto, Michel Lapier, Juan Diego Maya, Betty Matsuhiro, Claudio Olea-Azar, Giovanna L Delogu, Eugenio Uriarte, Lourdes Santana, Maria Joao Matose
BACKGROUND: Neglected diseases are becoming more prevalent due to globalization. This has inspired active research in the development of new drugs for the treatment of parasitic diseases such as Chagas disease. OBJECTIVES: With the aim of finding new trypanocidal agents, we report the in vitro evaluation of a new series of 3-amidocoumarins with or without hydroxyl substituents at position 4 of the coumarin ring. METHODS: Electrochemical and biological assays were performed in order to assess the antioxidant and trypanocidal potential of these compounds, and to better understand the mechanisms involved in their activity...
April 18, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29669502/synthetic-diethyl-2-6-dimethyl-1-4-dihydropyridine-3-5-dicarboxylates-induce-apoptosis
#4
Seunghyun Ahn, Youngshim Lee, Jihyun Park, Junho Lee, Soon Young-Shin, Young Han Lee, Dongsoo Koh, Yoongho Lim
BACKGROUND: The Hantzsch ester, diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate, has been used as a hydride donor and its various biological effects have been reported. To identify chemotherapeutic agents with apoptotic effects, 21 diethyl 2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates were designed and synthesized; they have not been reported as apoptosis inducers thus far. Their structure-cytotoxicity relationships were investigated. Further biological experiments were performed on the title compound...
April 18, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29663896/molecular-interaction-and-computational-analytical-studies-of-pinocembrin-for-its-antiangiogenic-potential-targeting-vegfr-2-a-persuader-of-metastasis
#5
Neha Sharma, Mala Sharma, Eram Shakeel, Qazi M Sajid Jamal, Mohammad A Kamal, Usman Sayeed, Mohammad K A Khan, Mohammad H Siddiqui, Jamal M Arif, Salman Akhtar
BACKGROUND: Designing a novel antagonist against VEGFR-2 is being applied currently to inhibit cancer growth and metastasis. Because of the unexpected side effects incurred by the contemporary anticancer medications, the focus has been laid towards identifying natural compounds that might carry the potential to inhibit tumor progression. VEGR-2 remains an important target for anticancer drug development as it is the master regulator of vascular growth. OBJECTIVE: The study focuses on virtual screening of compounds from plants of Asteraceae family that bears antiangiogenic potential and thus, inhibiting VEGFR-2 using a computational approach...
April 16, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29663895/synthesis-and-antibacterial-activity-against-mrsa-of-pleuromutilin-derivatives-possessing-a-mercaptoethylamine-linker
#6
Zhao-Sheng Zhang, Yun-Zhen Huang, Jian Luo, Bing-Feng Wang, Zhen Jin, Ya-Hong Liu, You-Zhi Tang
BACKGROUND: Methicillin resistant Staphylococcus aureus (MRSA) usually invalidate powerful antibiotics in the clinic. Pleuromutilin derivatives have been reported possess antibacterial activity against MRSA. OBJECTIVE: The antibacterial activities against MRSA of a series of thirteen synthetic pleuromutilin derivatives were investigated through in vitro models. METHODS: A series of novel thioehter pleuromutilin derivatives incorporating various aromatic substituents into the C14 side chain have been reported...
April 16, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29651943/benzoin-schiff-bases-design-synthesis-and-biological-evaluation-as-potential-antitumor-agents
#7
Dima A Sabbah, Fatima Al-Tarawneh, Wamidh H Talib, Kamal Sweidan, Sanaa K Bardaweel, Eveen Al-Shalabi, Haizhen A Zhong, Ghassan Abu Sheikha, Reema Abu Khalaf, Mohammad S Mubarak
BACKGROUND: Phosphoinositide 3-kinase α (PI3Kα) is an attractive target for anticancer drug design. OBJECTIVES: Target compounds were designed to probe the significance of alcohol and imine moieties tailored on a benzoin scaffold to better understand the structure activity relation (SAR) and improve their biological activity as anticancer compounds. METHODS: Chemical synthesis of the targeted compounds, biological evaluation tests against human colon adenocarcinoma (HCT-116), breast adenocarcinoma (MCF-7), and breast carcinoma (T47D) cell lines, as well as Glide docking studies were employed in this investigation...
April 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29651942/an-expedient-synthesis-of-cmf-019-s-5-methyl-3-1-pentan-3-yl-2-thiophen-2-ylmethyl-1h-benzo-d-imidazole-5-carboxamido-hexanoic-acid-a-potent-apelin-receptor-apj-agonist
#8
Lena Trifonov, Michal Afri, Krzysztof Palczewski, Edward E Korshin, Arie Gruzman
BACKGROUND: Apelin receptor (APJ) is a G protein-coupled receptor (GPCR) activated by the endogenous peptide apelin. The apelin-APJ system has emerged as an important regulator of cardiovascular homeostasis. Recently, a potent benzimidazole-derived apelin peptidomimetic, CMF-019, was patented but without a comprehensive description of its synthesis and a complete spectroscopic characterization of the intermediates. OBJECTIVE: Here, a detailed preparation of CMF-019 through a modified and improved synthetic pathway is described...
April 12, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29564982/towards-in-silico-design-of-new-hsp90-inhibitors-molecular-docking-and-3d-qsar-comfa-studies-of-tetrahydropyrido-4-3-d-pyrimidine-derivatives-as-hsp90-inhibitors
#9
Bakhtyar Sepehri, Raouf Ghavami
BACKGROUND: HSP90 is necessary for the conformational maturation of proteins, proteins disaggregation, folding new synthesized peptides and the refolding of denatured proteins. The inhibition of HSP90 leads to proteasomal degradations of client proteins that finally kill cancer cells. METHODS: In this research, molecular docking and comparative molecular field analysis (CoMFA) were used to investigate the interactions of tetrahydropyrido[4,3-d]pyrimidine derivatives with the N-terminal domain binding site of the HSP90 and predicting their inhibitory activities Results: A CoMFA model with five components and q2 of 0...
March 21, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29564981/synthesis-cyclooxygenase-2-inhibition-anti-inflammatory-evaluation-and-docking-study-of-substituted-n-3-4-5-trimethoxyphenyl-benzo-d-oxazole-derivatives
#10
Avneet Kaur, Sharad Wakode, Dharam Pal Pathak, Vidushi Sharma, Ashok K Shakya
BACKGROUND: Non-steroidal anti-inflammatory drugs are widely used for many years, but the chronic use of NSAID's leads to gastric side effects, ulceration and kidney problems. These side effects are due to non-selective inhibition of COX-2 along with COX-1. Therefore, it is imperative to develop novel and selective COX-2 inhibitors Objective: In this paper wehave synthesized a series of novel hybrids comprising of substituted-N-(3,4,5-trimethoxyphenyl)-benzo[d]oxazole derivatives and screened for the treatment of inflammation...
March 21, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29564980/diclofenac-1-3-4-oxadiazole-derivatives-biology-oriented-drug-synthesis-biods-in-search-of-better-non-steroidal-non-acid-antiinflammatory-agents
#11
Shazia Shah, Arshia, Nida Siraj Kazmi, Almas Jabeen, Aisha Faheem, Nida Dastagir, Tariq Ahmed, Khalid Mohammed Khan, Shakil Ahmed, Abeer Raza, Shahnaz Perveen
BACKGROUND: Inflammation is defined as the response of immune system cells to damaged or injured tissues The major symptoms of inflammation include increased blood flow, cellular influx, edema, elevated cellular metabolism, reactive oxygen species (ROS) nitric oxide (NO) and vasodilation. This normally protective mechanism against harmful agents when this normal mechanism becomes dysregulated that can cause serious illnesses including ulcerative colitis, Crohn's disease, rheumatoid arthritis, osteoarthritis, sepsis, and chronic pulmonary inflammation ...
March 21, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29521194/synthesis-of-a-tyr-tyr-dipeptide-library-and-evaluation-against-tumor-cells
#12
Stanley Ns Vasconcelos, Juliana M Sciani, Nicole Mambeli Lisboa, Helio A Stefani
BACKGROUND: Structural component of proteins and peptides, amino acids have been used as building blocks in the synthesis of more complex molecules with antitumor activity against several types of cancer. OBJECTIVE: The search for new anticancer compounds is ongoing, especially for cancers that are very aggressive and have poor prognoses, such as leukemia. METHOD: Here, we report a method to synthesize Tyr-Tyr dipeptides via sonochemistry reactions followed by functionalization of these Tyr-Tyr dipeptides with Suzuki-Miyaura and Sonogashira cross-coupling reactions in good yields...
March 9, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29493459/anti-diabetic-phenolic-compounds-of-black-carrot-daucus-carota-subspecies-sativus-var-atrorubens-alef-inhibit-enzymes-of-glucose-metabolism-an-in-silico-and-in-vitro-validation
#13
Suhas Gorakh Karkute, Tanmay Kumar Koley, Bijen Kumar Yengkhom, Ajay Tripathi, Shivani Srivastava, Arti Maurya, Bijendra Singh
BACKGROUND: Black carrot is known to be effective against Type 2 diabetes. The phenolic compounds present in black carrot are responsible for this property, but limited information was available about the mechanism of action and target enzymes. OBJECTIVE: The present study aims at understanding molecular interactions of phenolic compounds of black carrot with enzymes involved in glucose metabolism in human to identify the potential inhibitor that can be used as candidate drug molecule to control diabetes...
February 28, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29485004/design-synthesis-and-biological-evaluation-of-7-arylbenzo-c-acridine-5-6-diones-as-potential-anti-leishmanial-and-anti-trypanosomal-agents
#14
Shivani Mahajan, Shabana Khan, Babu Tekwani, Ikhlas Khan, Inder Pal Singh
Herein we report the anti-leishmanial and anti-trypanosomal activities of a series of thirty three newly synthesized 7-arylbenzo[c]acridine-5,6-diones. Of the tested, seven compounds (14, 17, 19, 26, 27, 38 and 39) were found to exhibit excellent anti-parasitic activities. Compound 14 was identified as the most potent compound against L. donovani promastigotes while compound 27 showed most significant inhibition activity against amastigotes. The synthesized analogs were also tested in human macrophage cell line (THP) infected with L...
February 26, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29485003/activity-of-diosgenyl-2-amino-2-deoxy-%C3%AE-d-glucopyranoside-its-hydrochloride-and-n-n-dialkyl-derivatives-against-non-albicans-candida-isolates
#15
Malgorzata Anna Dawgul, Daria Grzywacz, Beata Liberek, Wojciech Kamysz, Henryk Myszka
BACKGROUND: Candida albicans belongs to the most common fungal pathogens in humans, but recently an increased proliferation of strains called non-albicans Candida has been report-ed. Species belonging to this group are often characterised by a reduced susceptibility to anti-fungal agents. OBJECTIVE: In view of the emergence of non-albicans Candida and their resistance to available antifungals, an attempt has been made to develop novel effective agents. Biological activities of the N,N-dialkyl diosgenyl glycosides, which were previously synthesized, were determined...
February 26, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29485002/emerging-roles-of-purinergic-signaling-in-diabetes
#16
Carmen Fotino, Diego Dal Ben, Elena Adinolfi
BACKGROUND: Purinergic signaling accounts for a complex network of receptors and extracellular enzymes responsible for the generation, recognition and degradation of extracellular ATP and adenosine. The main actors of this system include P2X, P2Y and Adenosine Receptors, ectonucleotidases CD39 and CD73 and Adenosine Deaminase. The purinergic network recently emerged as a central player in several physiopathological conditions particularly those linked to immune system regulation including type 1 and type 2 diabetes...
February 26, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29485001/design-and-synthesis-of-3-4-diarylpyrrole-analogues-as-potent-topoisomerase-inhibitors
#17
Qiang Zhao, Wang Chen, Xu He, Zili Feng, Qi Liang
BACKGROUND: The natural products containing a common 3,4-diarylpyrrole skeleton have attracted considerable attention due to their unique structures and multiplex biological activities. In our previous study, lycogarubin C was synthesized and showed cytotoxicity against MDA-MB-231, A549, PC3 and HeLa cell lines and topoisomerase II inhibitory activities. OBJECTIVE: We present the design, synthesis and antitumor studies of 3,4-diarylprrole derivatives. Their antitumor activities and inhibitory activities against Topo I and Topo IIα of these compounds were assayed...
February 26, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29473521/synthesis-of-oleanolic-acid-analogues-and-their-cytotoxic-effects-on-3t3-cell-line
#18
Salih Tuncay, Halil Senol, Eray Metin Guler, Nuket Ocal, Hasan Secen, Abdurrahim Kocyigit, Gulacti Topcu
BACKGROUND: Oleanolic acid (OA) is a known natural compound with many important biological activities. Thirteen oleanolic acid derivatives linked at C-3 and C-28 were synthesized and their structures were confirmed by 1H- and 13C NMR and mass spectral analyses. Among them, compounds 4, 6, 8-10, 12, 13 were synthesized for the first time. They were evaluated for their cytotoxic activity. They showed proliferative effect at low concentrations while cytotoxic effect was observed at high concentrations in a dose dependent manner...
February 21, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29473520/synthesis-and-biological-evaluation-of-12n-substituted-tricyclic-matrinic-derivatives-as-a-novel-family-of-anti-influenza-agents
#19
Sheng Tang, Yu-Huan Li, Xin-Yue Cheng, Jin-Qiu Yin, Ying-Hong Li, Dan-Qing Song, Yan-Xiang Wang, Zhan-Dong Liu
BACKGROUND: Influenza is still a serious threat to human health with significant morbidity and mortality, so it is desirable to develop novel anti-flu drug agents with novel structures. OBJECTIVE: The main purpose of this research was to explore broad-spectrum anti-flu agents and provide antiviral stockpiles in response to potential future influenza pandemics. METHODS: Fifteen novel 12N-substituted tricyclic matrinic derivatives were synthesized and evaluated for their anti-influenza activities against H1N1 subtype taking 12N-p-cyanobenzenesulfonyl matrinane (1) as the lead...
February 21, 2018: Medicinal Chemistry
https://www.readbyqxmd.com/read/29473519/identification-of-new-chromenone-derivatives-as-cholinesterase-inhibitors-and-molecular-docking-studies
#20
Jamshed Iqbal, Muhammad Shakeel Ahmad Abbasi, Sumera Zaib, Saifullah Afridi, Norbert Furtmann, Jurgen Bajorath, Peter Langer
BACKGROUND: Alzheimer's disease (AD) is the leading cause of dementia among aging population. This devastating disorder is generally associated with the gradual memory loss, specified by decrease of acetylcholine level in the cortex hippocampus of the brain due to hyper-activation of cholinesterases (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)). OBJECTIVE: Therefore, inactivation of AChE and BChE by inhibitors can increase the acetylcholine level and hence may be an encouraging strategy for the treatment of AD and related neurological problems...
February 21, 2018: Medicinal Chemistry
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