Showing papers in "Bioorganic & Medicinal Chemistry in 2017"

TL;DR: An overview of the peptide therapeutic landscape is provided, including historical perspectives, molecular characteristics, regulatory benchmarks, and a therapeutic area breakdown, which includes over 150 peptides in active development today.

TL;DR: This review examines recent publications relating the structures of pyrazoles with their corresponding biological activities and approved pyrazole-containing drugs.

TL;DR: The prospects for venom-derived peptides look very optimistic, as proteomic and transcriptomic approaches continue to identify new sequences and the potential of venom- derived peptides to find applications as therapeutics, cosmetics and insecticides grows accordingly.

TL;DR: This review summarizes the progress in the field since 2005 regarding the isolation of new phenazine natural products, new insights in their biological function, and particularly the now almost completely understood biosynthesis.

TL;DR: This review discusses the recent discoveries, engineering, and applications of biocatalysts for the synthesis of pharmaceuticals and pharmaceutical intermediates.

TL;DR: Recently reported NIR emitting organic/inorganic fluorophores that targets and accumulates in organelle/organs specifically for molecular imaging of cancerous cells are reviewed.

TL;DR: The effects of N-methylation of cyclic peptides in strategies to optimize bioavailabilities is reviewed, of which N-alkylation is probably the most common.

TL;DR: Biocatalytic processes are described for the synthesis of key chiral intermediates for development pharmaceuticals, providing products in high yields and purity.

TL;DR: The article concludes highlighting the early stage of this research field and its still unveiled potential and that more explicatory PK/PD studies are required in order to achieve the translation from preclinical to the clinical development phase.

TL;DR: The focus will be, on the various approaches for the synthesis of tryptanthrins and its derivatives along with the biological activities.

TL;DR: Current clinical trials using neoantigen targeting cancer vaccines, including in combination with checkpoint blockade monoclonal antibodies, have demonstrated potent T-cell responses against those neoantigens accompanied by antitumor effects in patients.

TL;DR: An accurate analysis is proposed for a review article an accurate analysis of PZQ and OXA medicinal properties and uses, focusing on the pharmacochemical aspects of both drugs through 178 bibliographic references.

TL;DR: Structural-guided saturation mutagenesis and its iterative form have emerged as the method of choice for evolving stereo- and regioselective mutant enzymes needed in the asymmetric synthesis of chiral intermediates.

TL;DR: This review aims to offer a view on tumor targeting peptides that are either derived from natural peptide ligands or identified using phage display screening, including examples of peptides targeting the high-grade malignant tumors of the central nervous system as an example of the complex therapeutic management due to the tumor's location.

TL;DR: The synthesis, characterization and biological activities of 1,2,4-triazole and 1,3, 4-oxadiazole analogues (SS 1-SS 10) were reported, and enzyme inhibition efficacy against the receptor Pf-DHFR computationally as well as in vitro to prove their candidature as lead dihydrofolate reductase inhibitors.

TL;DR: A series of novel quinazoline-4(3H)-one-sulfonylurea hybrids were designed and synthesized as dual PPARγ and SUR agonists, evaluating their in vivo anti-hyperglycemic activities against STZ-induced hyperglycemic rats and their in vitro binding affinities and insulin-secreting abilities.

TL;DR: Synthesis of analogs of SLC-0111, both of the sulfanilamide and metanilamides series, which possess diverse substitution patterns at the terminal ureido-phenyl moiety, are reported, thus including one or more halogens, trifluoromethyl, perchloro-/perfluorophenyl groups instead of the 4-fluor phenyl groups present in SLC -0111.

TL;DR: In this review, innovative solutions for the multistep preparation of complex molecules such as APIs (Active Pharmaceutical Ingredients) in a telescoped manner are summarized, in order to benefit chemists aiming to exploit flow chemistry systems for the synthesis of biologically active molecules.

TL;DR: Results indicate specific biodistribution to the spleen, which can be blocked by co-administration of excess nivolumab, and distribution to other organs is consistent with elimination pathways of antibodies, with primary clearance through the liver.

TL;DR: In this article, a series of homoisoflavonoid Mannich base derivatives were designed, synthesized and evaluated as multifunctional agents against Alzheimer's disease, and it demonstrated that most of the derivatives were selective AChE and MAO-B dual inhibitors.

TL;DR: The results suggest that the developed SVR model is highly predictive and provides medicinal chemists a useful in silico tool to facilitate design and synthesis of novel compounds with optimal drug-like properties, and thus accelerate the lead optimization in drug discovery.

TL;DR: The pharmacological activities of CA and FA, and their hybrids as multi-target-directed ligands (MTDLs) against AD are summarized, hoping to provide beneficial information for the development of CA- and FA-based MTDLs against AD.

TL;DR: Coumarin-chalcone hybrids 2a-c have demonstrated the most promising activity against both cancer cell lines with IC50 values of 0.65-2.02μM, and Interestingly, the acrylohydrazide hybrid 4c showed the highest cytotoxic activity against the leukemia cell line (K562), thus indicating selectivity toward the tumor cells.

TL;DR: The 1,3-dipolar cycloadditions of an azomethine ylide generated from isatin and thiazolidinecarboxylic acid to a series of 2,6-bis[(E)-arylmethylidene]cyclohexanones afforded new di-spiro heterocycles incorporating pyrrolidine and oxindole rings in quantitative yields and chemo- regio- and stereoselectively.

TL;DR: A series of indole-2-carboxamides are synthesized that inhibit MmpL3 and have potent pan-activity against mycobacterial species and are suggested to be strong contenders for further preclinical testing as NTM therapeutics.

TL;DR: In this article, hydroxamic acid derivatives of olaparib were constructed as dual PARP and HDAC inhibitors, which showed potent inhibitory activities against PARP1/2 and HAC1/6 with IC50 values in the nanomolar range.

TL;DR: In this review, some of the most recently described peptide-based optical probes are reviewed with a special emphasis on their in vivo use and potential application in a clinical setting.

TL;DR: The quinazolinone derivatives identified in this work were potentially promising candidates for developing as novel anti-diabetic agents and docking results showed that BQ was less active than CQ against α-glucosidase because of its weaker interaction with the enzyme.

TL;DR: A highly optimized and environmentally conscious continuous-flow synthesis of two APIs identified as essential medicines by the World Health Organization, namely diazepam and atropine is reported.

TL;DR: The synthesis, characterization and biological activities of benzothiazole analogues (J 1-J 10) were reported and computational and in vitro studies were carried out to examine their candidatures as lead dihydrofolate reductase inhibitors.