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Future Medicinal Chemistry

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https://www.readbyqxmd.com/read/29145730/screening-and-evaluation-of-antioxidant-activity-of-some-1-2-4-triazolo-1-5-a-quinazoline-derivatives
#1
Rashad Al-Salahi, El-Hassane Anouar, Mohamed Marzouk, Hanan Aa Taie, Hatem A Abuelizz
AIM: The present study was carried out to assess a new series of triazoloquinazolines 1-40 for their antioxidant activities using 1,1-diphenyl-2-picryl hydrazyl radical scavenging, ferric reduction antioxidant power and reducing power capability assays. RESULTS: All triazoloquinazolines 1-40 exhibited antioxidant activity ranged from weak to moderate and high. The obtained findings revealed that the triazoloquinazolines 30, 36 and 38-40 have superiority among all compounds, demonstrating the highest capacity to deplete 1,1-diphenyl-2-picryl hydrazyl and free radicals, in relation to butylated hydroxyl toluene, as a synthetic antioxidant agent...
November 17, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29130348/tryptophan-containing-non-cationizable-opioid-peptides-a-new-chemotype-with-unusual-structure-and-in-vivo-activity
#2
Rossella De Marco, Luca Gentilucci
Recently, a new family of opioid peptides containing tryptophan came to the spotlight for the absence of the fundamental protonable tyramine 'message' pharmacophore. Structure-activity relationship investigations led to diverse compounds, characterized by different selectivity profiles and agonist or antagonist effects. Substitution at the indole of Trp clearly impacted peripheral/central antinociceptivity. These peculiarities prompted to gather all the compounds in a new class, and to coin the definition 'Tryptophan-Containing Non-Cationizable Opioid Peptides', in short 'TryCoNCOPs'...
November 13, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29120240/routes-to-drug-design-via-bioisosterism-of-carboxyl-and-sulfonamide-groups
#3
Alya A Arabi
AIM: The similarity in the biological function of the bioisosteric pair, carboxyl and sulfonamide functional groups, is studied using the quantitative tool, average electron density of the bioisosteric moiety in drug molecules and the qualitative tool, electrostatic potential. Results/methodology: Five different capping groups (methyl, phenyl, chlorine, hydrogen and amine) were considered to investigate the effect of the environment on the properties of the bioisosteres. The molecules were considered in their neutral and anionic forms to account for the change in pH depending on the medium of the drug-receptor interactions...
November 9, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29110537/novel-c-rgdyk-based-conjugates-of-popam-and-5-fluorouracil-for-integrin-targeted-cancer-therapy
#4
Savvas Thysiadis, Sotirios Katsamakas, Panagiotis Dalezis, Theodora Chatzisideri, Dimitrios Trafalis, Vasiliki Sarli
AIM: Alkylating agents and antimetabolites are cytotoxic drugs commonly used in cancer treatment. These medications are often associated with serious side effects on normal tissues and organs. METHODOLOGY: To improve the pharmacological profile of the alkylating agent POPAM and the antimetabolite 5-fluorouracil, novel integrin-targeted delivery systems based on c(RGDyK) were successfully synthesized. The new conjugates were tested in vitro against different cancer cells such as PC3, SKOV3, A549, MCF7 and MBA-MB-321...
November 7, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29098865/novel-quinazolinone-based-2-4-thiazolidinedione-3-acetic-acid-derivatives-as-potent-aldose-reductase-inhibitors
#5
Kamel Metwally, Harris Pratsinis, Dimitris Kletsas, Luca Quattrini, Vito Coviello, Concettina La Motta, Ahmed A El-Rashedy, Mahmoud Es Soliman
AIM: Targeting aldose reductase enzyme with 2,4-thiazolidinedione-3-acetic acid derivatives having a bulky hydrophobic 3-arylquinazolinone residue. MATERIALS & METHODS: All the target compounds were structurally characterized by different spectroscopic methods and microanalysis, their aldose reductase inhibitory activities were evaluated, and binding modes were studied by molecular modeling. RESULTS: All the synthesized compounds proved to inhibit the target enzyme potently, exhibiting IC50 values in the nanomolar/low nanomolar range...
November 3, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076773/targeting-protein-arginine-methyltransferase-5-in-disease
#6
André Richters
PRMT5 catalyzes the mono- and symmetric dimethylation of the arginine N-guanidine group of a wide variety of target proteins including histones, transcriptional elongation factors, kinases and tumor suppressors by utilizing the essential co-factor S-adenosylmethionine as methyl source. PRMT5 overexpression has been linked to the progression of various diseases, including cancer, and is oftentimes associated with a poor prognosis. Therefore, PRMT5 is promoted as a valuable target for drug discovery approaches and was a subject matter in recent endeavors aiming for the development of specific PRMT5 inhibitors...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076772/new-insights-for-the-use-of-quercetin-analogs-in-cancer-treatment
#7
Domenico Iacopetta, Fedora Grande, Anna Caruso, Roberta Alessandra Mordocco, Maria Rosaria Plutino, Luca Scrivano, Jessica Ceramella, Noemi Muià, Carmela Saturnino, Francesco Puoci, Camillo Rosano, Maria Stefania Sinicropi
AIM: Quercetin (Q1) is a flavonoid widely present in plants and endowed with several pharmacological properties mostly due to its antioxidant potential. Q1 shows anticancer activity and could be useful in cancer prevention. On the other hand, Q1 is poorly soluble in water and unstable in physiological systems, and its bioavailability is very low. METHODS: A small set of Q1 derivatives (Q2-Q9) has been synthesized following opportunely modified chemical procedures previously reported...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076769/%C3%AE-pyrones-and-their-hydroxylated-analogs-as-promising-scaffolds-against-mycobacterium-tuberculosis
#8
Zubair Shanib Bhat, Muzafar Ahmad Rather, Khalid Yousuf Syed, Zahoor Ahmad
Tuberculosis ranks as the leading cause of global human mortality from a single infectious agent. To address the uprising issues of drug resistance, intense research efforts have been directed towards drug discovery. However, it is a long and economically challenging process that is often associated with high failure rates. Therefore, it seems prudent to take forward the core scaffolds that have already acclaimed clinical relevance. In this direction, hydroxylated α-pyrone scaffold has received US FDA approval for human use against HIV...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076758/are-sigma-receptor-modulators-a-weapon-against-multiple-sclerosis-disease
#9
Simona Collina, Marta Rui, Silvia Stotani, Emanuele Bignardi, Daniela Rossi, Daniela Curti, Fabrizio Giordanetto, Alessio Malacrida, Arianna Scuteri, Guido Cavaletti
Effective therapies for multiple sclerosis (MS) are still missing. This neurological disease affects more than 2.5 million people worldwide. To date, biological immunomodulatory drugs are effective and safe during short-term treatment, but they are suitable only for parenteral administration and they are expensive. Accordingly, academic and industrial environments are still focusing their efforts toward the development of new MS drugs. Considering that neurodegeneration is a contributory factor in the onset of MS, herein we will focus on the crucial role played by sigma 1 receptors (S1Rs) in MS...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076756/virtual-screening-and-biological-evaluation-of-biofilm-inhibitors-on-dual-targets-in-quorum-sensing-system
#10
Yinqiu Xu, Xupeng Tong, Pinghua Sun, Leming Bi, Kejiang Lin
AIM: Resistance to conventional antibiotics has spurred interest in exploring new antimicrobial strategies. Suppressing quorum sensing within biofilm is a promising antimicrobial strategy. LasR in quorum sensing system of the Gram-negative bacteria, Pseudomonas aeruginosa, directly enhances virulence and antibiotic resistance, with QscR as its indirect suppressor, so targeting both of them can synergistically take the effect. METHODOLOGY/RESULTS: An in silico protocol combining pharmacophores with molecular docking was applied...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076753/can-small-molecule-inhibitors-of-glutaminyl-cyclase-be-used-as-a-therapeutic-for-alzheimer-s-disease
#11
Haiqiang Wu
Alzheimer's disease (AD) is a multifactorial and socioeconomically burdensome disease. In view of the failures of anti-AD candidates, we should try to rethink what we did before and what we should do next, in part at least. Research shows that the more neurotoxic factor, pyroglutamate-Aβs, and the more important inflammatory mediators, pyroglutamate-CCL2, both contribute to the initiation of AD specifically and the generation of N-terminal intramolecular cyclization catalyzed by glutaminyl cyclase quality control, the over-expression of which correlates positively with the severity of AD...
October 27, 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076761/cdk5-in-oncology-recent-advances-and-future-prospects
#12
Jimma Likisa Lenjisa, Solomon Tadesse, Nishat Zareen Khair, Malika Kumarasiri, Mingfeng Yu, Hugo Albrecht, Robert Milne, Shudong Wang
Selective abrogation of cyclin-dependent kinases (CDK) activity is a highly promising strategy in cancer treatment. The atypical CDK, CDK5 has long been known for its role in neurodegenerative diseases, and is becoming an attractive drug target for cancer therapy. Myriads of recent studies have uncovered that aberrant expression of CDK5 contributes to the oncogenic initiation and progression of multiple solid and hematological malignancies. CDK5 is also implicated in the regulation of cancer stem cell biology...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076755/discovery-of-a-cox-2-selective-inhibitor-hit-with-anti-inflammatory-activity-and-gastric-ulcer-protective-effect
#13
Mohamed A Abdelgawad, Rania B Bakr, Ahmed O El-Gendy, Gehan M Kamel, Amany A Azouz, Syed Nasir Abbas Bukhari
AIM: A novel series of 2-arylimino-5-arylidenethiazolidin-4-ones 12a-n were synthesized and all the target compounds were fully characterized by IR, (1)H NMR, (13)C NMR, mass spectroscopy and elemental analysis. Materials & methods: All the target compounds were evaluated for their COX inhibition by enzyme immunoassay kit and in vivo anti-inflammatory activity. RESULTS: Tested compounds were found more potent inhibitors of COX-2 (IC50 = 0.54-3.14 µM) than COX-1 (IC50 = 4...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076390/novel-rna-polymerase-inhibitor-found-in-soil-extracts-provides-hope-for-future-antibacterial-drugs
#14
Richard H Ebright
Richard H Ebright talks to Rachel Coleby, Commissioning Editor: Ebright is at Rutgers University (New Brunswick, NJ, USA), where he performs research on the structure, mechanism, and regulation of bacterial transcription and on antibacterial drug discovery targeting bacterial transcription. He has received research awards, including the Searle Scholar Award, the Walter J Johnson Prize, the Schering-Plough Award of the American Society for Biochemistry and Molecular Biology, the Waksman Award of the Theobold Smith Society, the MERIT Award of the National Institutes of Health, and membership in the American Academy of Arts and Science...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076351/activity-of-gallic-acid-and-its-ester-derivatives-in-caenorhabditis-elegans-and-zebrafish-danio-rerio-models
#15
Junya de Lacorte Singulani, Liliana Scorzoni, Paulo César Gomes, Ana Carolina Nazaré, Carlos Roberto Polaquini, Luis Octávio Regasini, Ana Marisa Fusco-Almeida, Maria José Soares Mendes-Giannini
AIM: Gallic acid and its ester derivatives have shown antifungal activity in vitro. This study was performed to investigate their activity against Candida albicans and their toxicity in the animal models Caenorhabditis elegans and zebrafish embryos. RESULTS: The compounds protected worms from C. albicans infection. The dodecyl gallate was the most effective. In zebrafish embryo, gallic acid and dodecyl gallate were the least toxic. CONCLUSION: Gallic acid and its ester derivatives have potential for in vivo use against C...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076350/the-derivatization-and-antitumor-mechanisms-of-polysaccharides
#16
Gangliang Huang, Hualiang Huang
At present, the polysaccharide antitumor research is focused on how to further improve the antitumor activity of polysaccharides. The structural modification of polysaccharides can enhance their antitumor activity to a certain extent. The antitumor mechanisms of polysaccharide derivatives mainly contain the inducing apoptosis of tumor cells, effecting on the cycle of tumor cells, enhancing the antioxidant activity of organism, activating the body's immune response and inhibiting the tumor angiogenesis. Herein, the common methods of polysaccharide modification, such as sulfation, carboxymethylation, phosphorylation and acetylation, were summarized...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076349/the-therapeutic-potential-of-targeting-the-kir1-1-renal-outer-medullary-k-channel
#17
Birgit T Priest, Alexander Pasternak
Kir1.1 (renal outer medullary K(+)) channels are potassium channels expressed almost exclusively in the kidney and play a role in the body's electrolyte and water balance. Potassium efflux through Kir1.1 compliments the role of transporters and sodium channels that are the targets of known diuretics. Consequently, loss-of-function mutations in men and rodents are associated with salt wasting and low blood pressure. On this basis, Kir1.1 inhibitors may have value in the treatment of hypertension and heart failure...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29076348/synthesis-and-evaluation-of-xanthone-derivatives-as-acid-sphingomyelinase-inhibitors-potential-treatment-for-uv-induced-skin-damage
#18
Kan Yang, Biao Gao, Xianjun Ming, Zhipeng Huang, Minghui Wang, Jibin Dong, Jinxin Wang
AIM: ASM, which hydrolyzes sphingomyelin into ceramide, is recognized as a therapeutic target for UV-induced skin damage. Direct inhibitors for this enzyme are rare. Here we synthesized several series of 1,3,6,7-tetrahydroxy-xanthone derivatives as novel ASM inhibitors. RESULTS: Several compounds were more potent than the lead compound, among which 5b was found competitively inhibiting the enzyme and dose-dependently reducing ceramide generation. Furthermore, 5b and 5c showed excellent protective effect to skin keratinocytes against UV...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29064290/quercetin-oleic-acid-based-g-protein-coupled-receptor-40%C3%A2-ligands-as-new-insulin-secretion-modulators
#19
Mariateresa Badolato, Gabriele Carullo, Mariarita Perri, Erika Cione, Fabrizio Manetti, Maria Luisa Di Gioia, Antonella Brizzi, Maria Cristina Caroleo, Francesca Aiello
AIM: Management of Type 2 diabetes mellitus by diet is achievable at the early stage of the disease; patients usually underestimate this approach and an appropriate drug therapy is required. RESULTS: Starting from quercetin and oleic acid, that have effect on insulin secretion, a small set of hybrid molecules was synthesized. Insulin secretion was evaluated in both in vitro and ex vivo models.  AV1  was able to enhance insulin secretion dose dependently, behaving as a conceivable agonist of G-protein-coupled receptor 40...
October 2017: Future Medicinal Chemistry
https://www.readbyqxmd.com/read/29028366/synthesis-modeling-and-biological-evaluation-of-hybrids-from-pyrazolo-1-5c-pyrimidine-as-antileishmanial-agents
#20
Kamal Fahmy Mohamed Atta, Tamer Mohamed Ibrahim, Omaima Osman Mahmoud Farahat, Tareq Qasem Al-Shargabi, Mohamed Gaber Marei, Adnan Ahmed Bekhit, El Sayed Helmy El Ashry
AIM: A new series of pyrazolo[1,5-c]pyrimidines were synthesized by different hybridization strategies. METHODOLOGY: All structures were confirmed by IR, (1)H, (13)C, (1)H-(13)C heteronuclear multiple-quantum correlation (HMQC) spectra and microanalysis. They were evaluated for their in vitro antileishmanial activity against miltefosine and amphotericin B deoxycholate as reference drugs. RESULTS: The most active compounds 2a and 9a demonstrated superior potencies to miltefosine by ten- and six-fold, respectively, for the promastigote form, and by 5...
October 2017: Future Medicinal Chemistry
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