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Page 1
1H-Tetrazol-5-amine and 1,3-thiazolidin-4-one derivatives containing 3-(trifluoromethyl)phenyl scaffold: Synthesis, cytotoxic and anti-HIV studies.
Bielenica A, Szulczyk D, Olejarz W, Madeddu S, Giliberti G, Materek IB, Koziol AE, Struga M. Bielenica A, et al. Biomed Pharmacother. 2017 Oct;94:804-812. doi: 10.1016/j.biopha.2017.07.152. Epub 2017 Aug 10. Biomed Pharmacother. 2017. PMID: 28802233
On the basis of recently reported biologically active 3-(trifluoromethyl)phenylthioureas, a series of diaryl derivatives incorporating 1H-tetrazol-5-yl (1a-11a, 1a'-11a') and 1,3-thiazolidin-4-one (1b-11b) scaffolds were synthesized. ...The most promising N-(4-nitro …
On the basis of recently reported biologically active 3-(trifluoromethyl)phenylthioureas, a series of diaryl derivatives incorporatin …
Antimycobacterial activity of novel 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(sub)phenyl/pyridylthiourea compounds endowed with high activity toward multidrug-resistant Mycobacterium tuberculosis.
Sriram D, Yogeeswari P, Dinakaran M, Thirumurugan R. Sriram D, et al. J Antimicrob Chemother. 2007 Jun;59(6):1194-6. doi: 10.1093/jac/dkm085. Epub 2007 Apr 20. J Antimicrob Chemother. 2007. PMID: 17449482
OBJECTIVES: The objective of this work was to synthesize 15 new 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(sub)phenyl/pyridylthiourea compounds and evaluate their in vitro and in vivo antimycobacterial activities. ...RESULTS: Among the 15 compounds screened, 7 compo …
OBJECTIVES: The objective of this work was to synthesize 15 new 1-(5-cyclobutyl-1,3-oxazol-2-yl)-3-(sub)phenyl/pyridylt …
β-Stereoselective Mannosylation Using 2,6-Lactones.
Hashimoto Y, Tanikawa S, Saito R, Sasaki K. Hashimoto Y, et al. J Am Chem Soc. 2016 Nov 16;138(45):14840-14843. doi: 10.1021/jacs.6b08874. Epub 2016 Nov 4. J Am Chem Soc. 2016. PMID: 27782395
Owing to stereoelectronic effects, the reaction tends to proceed via an S(N)1 mechanism to afford alpha-glycosides. We found that the introduction of a 2,6-lactone bridge can circumvent the competing S(N)1 reaction, affording beta-glycosides with stereoinversion via …
Owing to stereoelectronic effects, the reaction tends to proceed via an S(N)1 mechanism to afford alpha-glycosides. We found that the …
Thiourea derivatives inhibit key diabetes-associated enzymes and advanced glycation end-product formation as a treatment for diabetes mellitus.
Ullah I, Hassan M, Khan KM, Sajid M, Umar M, Hassan S, Ullah A, El-Serehy HA, Charifi W, Yasmin H. Ullah I, et al. IUBMB Life. 2023 Feb;75(2):161-180. doi: 10.1002/iub.2699. Epub 2022 Dec 24. IUBMB Life. 2023. PMID: 36565478 Free article.
The data revealed the potency of five compounds, including E (1-(2,4-difluorophenyl)-3-(3,4-dimethyl phenyl) thiourea), AG (1-(2-methoxy-5-(trifluoromethyl) phenyl)-3-(3-methoxy phenyl) thiourea), AF (1-(2,4-dichlorop …
The data revealed the potency of five compounds, including E (1-(2,4-difluorophenyl)-3-(3,4-dimethyl phenyl) thiourea), …
Self-association promoted conformational transition of (3R,4S,8R,9R)-9-[(3,5-bis(trifluoromethyl)phenyl))-thiourea](9-deoxy)-epi-cinchonine.
Király P, Soós T, Varga S, Vakulya B, Tárkányi G. Király P, et al. Magn Reson Chem. 2010 Jan;48(1):13-9. doi: 10.1002/mrc.2531. Magn Reson Chem. 2010. PMID: 19862796
The conformational diversity of the (3R,4S,8R,9R)-9-[(3,5-bis(trifluoromethyl)phenyl))-thiourea](9-deoxy)-epi-cinchonine organocatalyst is discussed. ...The study is extended by a comparison with other members of the bifunctional amine-thiourea organoc …
The conformational diversity of the (3R,4S,8R,9R)-9-[(3,5-bis(trifluoromethyl)phenyl))-thiourea](9-deoxy)-epi-cinchonin …
Investigation of the Mechanisms of Cytotoxic Activity of 1,3-Disubstituted Thiourea Derivatives.
Strzyga-Łach P, Chrzanowska A, Podsadni K, Bielenica A. Strzyga-Łach P, et al. Pharmaceuticals (Basel). 2021 Oct 28;14(11):1097. doi: 10.3390/ph14111097. Pharmaceuticals (Basel). 2021. PMID: 34832881 Free PMC article.
Substituted thiourea derivatives possess confirmed cytotoxic activity towards cancer but also normal cells. ...The derivatives exerted better growth inhibitory profiles towards selected tumor cells than the reference cisplatin. Compounds incorporating 3,4-dichloro- (2) and …
Substituted thiourea derivatives possess confirmed cytotoxic activity towards cancer but also normal cells. ...The derivatives exerte …
Tetrahydroquinoline units in flexible heteroarotinoids (Flex-Hets) convey anti-cancer properties in A2780 ovarian cancer cells.
Gnanasekaran KK, Pouland T, Bunce RA, Darrell Berlin K, Abuskhuna S, Bhandari D, Mashayekhi M, Zhou DH, Benbrook DM. Gnanasekaran KK, et al. Bioorg Med Chem. 2020 Jan 1;28(1):115244. doi: 10.1016/j.bmc.2019.115244. Epub 2019 Dec 2. Bioorg Med Chem. 2020. PMID: 31831296
SHetA2 (NSC 721689), our lead Flex-Het anti-cancer agent, consists of a thiochroman (Ring A) and a 4-nitrophenyl (Ring B) linked by a thiourea bridge. In this work, several series of new analogs having a tetrahydroquinoline (THQ, Ring A) unit connected by a urea or thio …
SHetA2 (NSC 721689), our lead Flex-Het anti-cancer agent, consists of a thiochroman (Ring A) and a 4-nitrophenyl (Ring B) linked by a thi …
Synthesis, Structural Characterization and Biological Activity Evaluation of Novel Cu(II) Complexes with 3-(trifluoromethyl)phenylthiourea Derivatives.
Drzewiecka-Antonik A, Struga M, Głogowska A, Augustynowicz-Kopec E, Dobrzyńska K, Chrzanowska A, Wolska A, Rejmak P, Klepka MT, Wrzosek M, Bielenica A. Drzewiecka-Antonik A, et al. Int J Mol Sci. 2022 Dec 10;23(24):15694. doi: 10.3390/ijms232415694. Int J Mol Sci. 2022. PMID: 36555333 Free PMC article.
Copper complexes with 1,3-disubstituted thiourea derivatives, all containing 3-(trifluoromethyl)phenyl tail and 1-alkyl/halogen-phenyl substituent, were synthesized. ...The dimeric halogeno derivatives showed higher antimicrobial activity …
Copper complexes with 1,3-disubstituted thiourea derivatives, all containing 3-(trifluoromethyl)phenyl tail and …
Simple and Rapid Mechanochemical Synthesis of Lactide and 3S-(Isobutyl)morpholine-2,5-dione-Based Random Copolymers Using DBU and Thiourea.
Burton TF, Pinaud J, Pétry N, Lamaty F, Giani O. Burton TF, et al. ACS Macro Lett. 2021 Dec 21;10(12):1454-1459. doi: 10.1021/acsmacrolett.1c00617. Epub 2021 Nov 8. ACS Macro Lett. 2021. PMID: 35549138
In this study, the ring-opening (co)polymerization of leucine-derived 3S-(isobutyl)morpholine-2,5-dione (MD) and lactide (LA) was performed via ball-milling using a catalytic system composed of 1,8-diazabicyclo[5.4.0]undec-7-ene (DBU) and 3-[3,5-bis(trifluoromethyl) …
In this study, the ring-opening (co)polymerization of leucine-derived 3S-(isobutyl)morpholine-2,5-dione (MD) and lactide (LA) was performed …
Bis-Thiourea Chiral Sensor for the NMR Enantiodiscrimination of N-Acetyl and N-Trifluoroacetyl Amino Acid Derivatives.
Recchimurzo A, Balzano F, Uccello Barretta G, Gherardi L. Recchimurzo A, et al. J Org Chem. 2022 Sep 16;87(18):11968-11978. doi: 10.1021/acs.joc.2c00814. Epub 2022 Sep 5. J Org Chem. 2022. PMID: 36062357 Free PMC article.
A C2-symmetrical bis-thiourea chiral solvating agent (CSA), TFTDA, for NMR spectroscopy has been obtained by reacting (1R,2R)-1,2-bis(2-hydroxyphenyl)ethylenediamine and 3,5-bis(trifluoromethyl)phenyl isothiocyanate. TFTDA shows remarkable propensity t …
A C2-symmetrical bis-thiourea chiral solvating agent (CSA), TFTDA, for NMR spectroscopy has been obtained by reacting (1R,2R)-1 …
64 results