Results 91 to 100 of about 12,572 (245)

Organolithium-Mediated Diversification of Peptide Thiazoles

, 2016
We report a one-step, racemization-free method for the diversification of peptide thiazoles via direct lithiation of the thiazole ring. The method is compatible with N-Boc, N-trityl, carboxylic ester, and carboxamide protecting groups and has been used ...
Jack Taunton (67759), Shaojiang Deng (2695228)   +1 more
core   +1 more source

Diethylene Glycol‐Linked Ring‐Fused Bis‐Azoles: Target‐Oriented Synthesis, In Silico Screening, and Antitumor Activity

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
A series of diethylene glycol‐linked cyclic derivatives with diversity in the heterocyclic motif have been synthesized and screened for antitumor activity. Two bis‐thiazolo[3,2‐a]pyrimidinone derivatives displayed moderate cytotoxicity, high selectivity against hepatocellular carcinoma cells, promising VEGFR2, and remarkable FGFR2 inhibitory activities
Sami A. Al‐Hussain, Abdulrahman S. Alharbi, Zeinab A. Muhammad, Alyaa S. Abdel Halim, Magdi E. A. Zaki, Mark C. Bagley, Refaie M. Kassab   +6 more
wiley   +1 more source

Thiazole Compounds

, 1967
Thiazole ...
J. Shukri, S. Alazawe
openaire   +2 more sources

One-pot synthesis of substituted steroidal thiazoles

, 2000
Steroid Research Laboratory, Department of Chemistry, Aligarh Muslim University, Aligarh-202 002, India Manuscript received 18 May 1999, revised 10 August 1999, accepted 13 September 1999 Substituted steroidal thiazoles (4-9) have been synthesized from
Shamsuzzaman, M. Jamaluddin, I. H. Siddiqui, Shafiullah, E. H. Khan   +4 more
core   +1 more source

Searching for Novel COVID19 Treatments: Towards Covalent TMPRSS2 Inhibitors

ChemMedChem, Volume 21, Issue 19, 14 October 2026.
We designed, synthesised, and evaluated new guanidine derivatives as potential covalent inhibitors of TMPRSS2, a key protease for SARS‐CoV‐2 entry. Computational studies showed that some compounds have improved binding over nafamostat. However, experimentally none effectively blocked viral entry in cell assays, indicating further optimisation is needed.
Marco Minneci, Barbara Farkaš, Adeyemi Rahman, Inga Nehlmeier, Amy Eichmann, Stefan Pöhlmann, Isabel Rozas   +6 more
wiley   +1 more source

A general synthesis of thiazoles. Part 3. Comparative evaluation of different functionalised thioureas as precursors

, 1979
N-Acyl-N'-monosubstituted thioureas (9) react with phenacyl bromide to produce thiazolines (10) and not thiazoles (4), as claimed. The addition products of N-arylbenzamidines and phenyl isothiocyanate react with phenacyl bromide to give 2-anilino-5 ...
Rajappa, Srinivasachari, Sreenivasan, Ramaswami, Desai, Jagdish A., Advani, Bhagwan G., Nair, Mohan D.   +4 more
core   +1 more source

Tackling Microbial Resistance with Isatin-Decorated Thiazole Derivatives: Design, Synthesis, and in vitro Evaluation of Antimicrobial and Antibiofilm Activity

Drug Design, Development and Therapy, 2022
Refaie M Kassab,1 Sami A Al-Hussain,2 Nooran S Elleboudy,3 Amgad Albohy,4 Magdi EA Zaki,2 Khaled AM Abouzid,5,6 Zeinab A Muhammad7 1Department of Chemistry, Faculty of Science, Cairo University, Giza, 12613, Egypt; 2Department of Chemistry, Faculty of ...
Kassab RM, Al-Hussain SA, Elleboudy NS, Albohy A, Zaki MEA, Abouzid KAM, Muhammad ZA   +6 more
doaj  

Synthesis and Biological Evaluation of Bisthiazoles and Polythiazoles

Molecules, 2018
Small heterocyclic compounds containing nitrogen and sulfur atoms, such as thiazole derivatives, represent a significant class of organic azoles that exhibit promising bioactivities and have a great potential in medicinal and agricultural fields.
Mohammed A. Al-Omair, Abdelwahed R. Sayed, Magdy M. Youssef   +2 more
doaj   +1 more source

Functionalization of thiazoles. selectivity in the reactions of 2-(dimethylamino)-1,3-thiazoles with electrophiles: Formation of Michael-type adducts and thiazolium salts

, 1981
The reactions of 2-(dimethylamino)-1,3-thiazoles with compounds cntaining an electron-poor double or triple bond are ...
MEDICI, Alessandro, C. VENTUROLI, PEDRINI, Paola, DONDONI, Alessandro   +3 more
core   +1 more source

Beyond the Active Site: First-In-Class Leishmania Infantum Trypanothione Reductase Dimerization Disruptors as Antileishmanial Leads. [PDF]

ChemMedChem
This review outlines a pioneering strategy to inhibit Leishmania infantum trypanothione reductase by disrupting its dimer interface. From peptides to small‐molecule proteomimetics, multiple chemotypes achieved potent enzymatic inhibition and notable cellular antileishmanial activity, highlighting a new therapeutic paradigm.
Camarasa MJ, Maldonado M, de la Cruz-Potenciano A, de Castro S.   +3 more
europepmc   +2 more sources