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Showing 1 to 12 of 1616 entries
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Small Molecule Docking Supports Broad and Narrow Spectrum Potential for the Inhibition of the Novel Antibiotic Target Bacterial Pth1.

Antibiotics (Basel, Switzerland)

Ferguson PP, Holloway WB, Setzer WN, McFeeters H, McFeeters RL.
PMID: 27171117
Antibiotics (Basel). 2016 May 10;5(2). doi: 10.3390/antibiotics5020016.

Peptidyl-tRNA hydrolases (Pths) play ancillary yet essential roles in protein biosynthesis by recycling peptidyl-tRNA. In E. coli, inhibition of bacterial Pth1 leads to accumulation of peptidyl-tRNA, depletion of aminoacyl-tRNA, and cell death. Eukaryotes have multiple Pths and Pth1 knock...

Total synthesis of (+)-lactacystin.

Angewandte Chemie (International ed. in English)

Panek JS, Masse CE.
PMID: 25138505
Angew Chem Int Ed Engl. 1999;38(8):1093-5. doi: 10.1002/(SICI)1521-3773(19990419)38:8<1093::AID-ANIE1093>3.0.CO;2-U.

A double stereodifferentiating crotylation between aldehyde 1 and silane (S)-2 to afford homoallylic alcohol 3 is the key diastereoselective step (anti:syn >30:1) in an efficient asymmetric synthesis of (+)-lactacystin. This compound is a metabolite isolated from Streptomyces sp. OM-6519...

Efficient Sialyltransferase Inhibitors Based on Transition-State Analogues of the Sialyl Donor.

Angewandte Chemie (International ed. in English)

Müller B, Schaub C, Schmidt RR.
PMID: 29711111
Angew Chem Int Ed Engl. 1998 Nov 02;37(20):2893-2897. doi: 10.1002/(SICI)1521-3773(19981102)37:20<2893::AID-ANIE2893>3.0.CO;2-W.

A 200- to 1000-fold higher affinity for sialyltransferase is shown by compounds 1 and 2 relative to the natural substrate. These inhibitors, which are derived from the transition state of S

From Cycloolefins to Linear C.

Angewandte Chemie (International ed. in English)

Armbruster J, Grabowski S, Ruch T, Prinzbach H.
PMID: 29711455
Angew Chem Int Ed Engl. 1998 Sep 04;37(16):2242-2245. doi: 10.1002/(SICI)1521-3773(19980904)37:16<2242::AID-ANIE2242>3.0.CO;2-0.

Technical olefins and azodicarbonic ester are the starting materials for C

Compounds from Terminalia mantaly L. (Combretaceae) Stem Bark Exhibit Potent Inhibition against Some Pathogenic Yeasts and Enzymes of Metabolic Significance.

Medicines (Basel, Switzerland)

Tchuente Tchuenmogne MA, Kammalac TN, Gohlke S, Kouipou RMT, Aslan A, Kuzu M, Comakli V, Demirdag R, Ngouela SA, Tsamo E, Sewald N, Lenta BN, Boyom FF.
PMID: 28930221
Medicines (Basel). 2017 Jan 24;4(1). doi: 10.3390/medicines4010006.

No abstract available.

2-Nitrobenzylarsonium Compounds That Photorelease Heavy-Atom Cholinergic Ligands for Time-Resolved Crystallographic Studies on Cholinesterases.

Angewandte Chemie (International ed. in English)

Peng L, Nachon F, Wirz J, Goeldner M.
PMID: 29711614
Angew Chem Int Ed Engl. 1998 Oct 16;37(19):2691-2693. doi: 10.1002/(SICI)1521-3773(19981016)37:19<2691::AID-ANIE2691>3.0.CO;2-7.

As heavy-atom analogues of caged cholinergic ligands, the arsonium compounds 1-3 were synthesized for potential time-resolved crystallographic studies on cholinesterases. Compounds 1 and 3 possess the desired properties for dynamic studies on the catalytic mechanism of cholinesterases: structural similarity...

Editorial: Chemical Insights Into the Synthetic Chemistry of Quinazolines and Quinazolinones: Recent Advances.

Frontiers in chemistry

Khan I, Ma Y, Saeed A.
PMID: 33614598
Front Chem. 2021 Feb 04;8:641321. doi: 10.3389/fchem.2020.641321. eCollection 2020.

No abstract available.

2-(2-Hydroxyethyl)piperazine derivatives as potent human carbonic anhydrase inhibitors: Synthesis, enzyme inhibition, computational studies and antiglaucoma activity.

European journal of medicinal chemistry

Chiaramonte N, Angeli A, Sgambellone S, Bonardi A, Nocentini A, Bartolucci G, Braconi L, Dei S, Lucarini L, Teodori E, Gratteri P, Wünsch B, Supuran CT, Romanelli MN.
PMID: 34920169
Eur J Med Chem. 2022 Jan 15;228:114026. doi: 10.1016/j.ejmech.2021.114026. Epub 2021 Dec 04.

Targeting Carbonic Anhydrases (CAs) represents a strategy to treat several diseases, from glaucoma to cancer. To widen the structure-activity relationships (SARs) of our series of piperazines endowed with potent human carbonic anhydrase (hCA) inhibition, a new series of chiral...

The Fellowship of Privileged Scaffolds-One Structure to Inhibit Them All.

Pharmaceuticals (Basel, Switzerland)

Skoreński M, Sieńczyk M.
PMID: 34832946
Pharmaceuticals (Basel). 2021 Nov 16;14(11). doi: 10.3390/ph14111164.

Over the past few years, the application of privileged structure has emerged as a powerful approach to the discovery of new biologically active molecules. Privileged structures are molecular scaffolds with binding properties to the range of different biological targets....

Size and Flexibility Define the Inhibition of the H3N2 Influenza Endonuclease Enzyme by Calix[n]arenes.

Antibiotics (Basel, Switzerland)

Tauran Y, Cerón-Carrasco JP, Rhimi M, Perret F, Kim B, Collard D, Coleman AW, Pérez-Sánchez H.
PMID: 31163674
Antibiotics (Basel). 2019 Jun 03;8(2). doi: 10.3390/antibiotics8020073.

Inhibition of H3N2 influenza PA endonuclease activity by a panel of anionic calix[n]arenes and β-cyclodextrin sulfate has been studied. The joint experimental and theoretical results reveal that the larger, more flexible and highly water-soluble sulfonato-calix[n]arenes have high inhibitory activity,...

Design, synthesis and biological evaluation of N-substituted indole-thiazolidinedione analogues as potential pancreatic lipase inhibitors.

Chemical biology & drug design

George G, Auti PS, Paul AT.
PMID: 33864339
Chem Biol Drug Des. 2021 Jul;98(1):49-59. doi: 10.1111/cbdd.13846. Epub 2021 May 02.

Pancreatic Lipase (PL) is a key enzyme responsible for the digestion of 50%-70% of dietary triglycerides, hence its inhibition is considered as a viable approach for the management of obesity. A series of indole-TZD hybrid analogues were synthesized, characterized...

Design and testing of selective inactivators against an antifungal enzyme target.

Drug development research

Friday SN, Cheng DW, Zagler SG, Zanella BS, Dietz JD, Calbat CN, Roach LT, Bagnal C, Faile IS, Halkides CJ, Viola RE.
PMID: 34469014
Drug Dev Res. 2021 Sep 01; doi: 10.1002/ddr.21875. Epub 2021 Sep 01.

Systemic infections from fungal organisms are becoming increasingly difficult to treat as drug resistance continues to emerge. To substantially expand the antifungal drug landscape new compounds must be identified and developed with novel modes of action against previously untested...

Showing 1 to 12 of 1616 entries