Results 11 to 20 of about 2,743 (163)

Modular Synthesis of Pyritide-Inspired Macrocycles Featuring Bipyridine Motifs. [PDF]

Angew Chem Int Ed Engl
A pyritide‐inspired build/couple/pair strategy yields a diverse macrocycle library. This approach expands chemical space and enables the discovery of 6paW, a potent anti‐ferroptotic agent. Abstract Macrocycles represent a promising class of drug‐like scaffolds with unique structural features and the ability to engage challenging targets such as protein–
Lee JH, Yi S, Bang J, Choi H, Park SB.
europepmc   +3 more sources

Crystal structure of endo-β-N-acetylglucosaminidase HSα. [PDF]

Acta Crystallogr F Struct Biol Commun
Structural analysis of the GH85 enzyme endo‐β‐N‐acetylglucosaminidase HSα reveals a novel domain that is potentially involved in complex N‐glycan recognition.The crystal structure of endo‐β‐N‐acetylglucosaminidase HSα (Endo HSα) was determined at 1.8 Å resolution, revealing that the enzyme is composed of five distinct domains.
Kurauchi I, Okura K, Hosokawa C, Ito K, Miyahara I.   +4 more
europepmc   +2 more sources

Antidiabetic Evaluation of New Pyrimidine-Thiazoline Hybrids Endorsed With Enzyme Kinetic Studies and Computational Analysis. [PDF]

Chem Biol Drug Des
We demonstrated the application of molecular hybridization in disclosing new pyrimidine‐thiazole molecular hybrids as potential α‐glucosidase and α‐amylase inhibitors and antioxidant agents. The representative compound of the series exhibited 3‐fold more potency than the standard drug acarbose against α‐glucosidase and 2‐fold greater potency than ...
Kumar G, Seboletswe P, Manhas N, Ghumran S, Gcabashe N, Bhargava G, Idris A, Islam MS, Singh P.   +8 more
europepmc   +2 more sources

Electrostatic potential as a reactivity scoring function in computer-assisted enzyme engineering. [PDF]

FEBS J
We present a computational metric that quantifies the electrostatic complementarity of enzymes to the charge distribution of substrates at the transition state. Implemented in BindScan, this metric accurately predicts functionally relevant mutations in glycoside hydrolases.
Vega A, Planas A, Biarnés X.
europepmc   +2 more sources

Thiazoline-related innate fear stimuli orchestrate hypothermia and anti-hypoxia via sensory TRPA1 activation

Nature Communications, 2021
Matsuo et al. report that thiazoline-related innate fear-eliciting compounds activate the spinal trigeminal nucleus (Sp5) and the nucleus of the solitary tract (NTS) via vagal/trigeminal TRPA1 to induce robust physiological alterations, enabling long ...
Tomohiko Matsuo, Tomoko Isosaka, Yuichiro Hayashi, Lijun Tang, Akihiro Doi, Aiko Yasuda, Mikio Hayashi, Chia-Ying Lee, Liqin Cao, Natsumaro Kutsuna, Sachihiro Matsunaga, Takeshi Matsuda, Ikuko Yao, Mitsuyoshi Setou, Dai Kanagawa, Koichiro Higasa, Masahito Ikawa, Qinghua Liu, Reiko Kobayakawa, Ko Kobayakawa   +19 more
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Synthesis and in silico ADMET evaluation of new thiazole and thiazolidine-4-one derivatives as non-ulcerogenic analgesic and anti-inflammatory agents [PDF]

Journal of the Serbian Chemical Society
A series of 1,3-thiazoline-4-one derivatives bearing 2-phenoxyphenyl moiety, were synthesized as potential new analgesic and anti-inflammatory agents. The structures were confirmed by FT-IR, NMR and mass spectra. The abdominal constriction (writing) test
Nassiri Koopaei Mansur, Monavari Mahshid, Vousooghi Nasim, Moshirabadi Sadaf, Assarzadeh Mohammad Javad, Amini Mohsen, Almasirad Ali   +6 more
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A Facile Synthesis of 2,4-Disubstituted Thiazoles Using MnO2

Molecules, 2009
Structurally diverse thiazoles with electron-donating and electron-withdrawing groups were conveniently synthesized through manganese dioxide (MnO2) oxidation of the corresponding thiazolines.
Bin Fu, Yan-Bo Yu, Hong-Liang Chen, Xin-Zheng Chen, Li-Yi Wang   +4 more
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2-Amino-1,3-thiazoline hydrochloride [PDF]

Acta Crystallographica Section B Structural Crystallography and Crystal Chemistry, 1981
C3H,N2S+. C1-2 M , = 138.62, monoclinic, P2,/c, a = 7.240 (7), b = 6.176 (2), c = 13.462 (8) A,8 = 100.10 (3)quot;, D, = 1.51, D, = 1.55 Mg m-3, Z =4, p = 7.619 mm-'. Final R = 0.110 for 657 observed reflections. The nonplanar thiazoline ring assumes an13; envelope conformation. The crystal structure is13; stabilized by NH . . .
B. M. Vedavathi, K. Vijayan
openaire   +1 more source

Two New Cholinesterase Inhibitory and Antioxidative Constituents from Syzygium cumini [PDF]

Iranian Journal of Chemistry & Chemical Engineering, 2023
Phytochemical investigation on dichloromethane (CH2Cl2) fraction from fruit seeds of Syzygium cumini provided two new esters Syzygioate A (1) and Syzygioate B (2), along with known compounds dipropyl succinate and dioctyl phthalate.
Neelam Sahab, Dilfaraz Khan, Hamid Ullah, Shumaila Kiran, Shafiullah Khan   +4 more
doaj   +1 more source

New Thiazoline-Tetralin Derivatives and Biological Activity Evaluation

Molecules, 2018
In this study, novel N′-(3-cyclohexyl/phenyl-4-(substituted phenyl)thiazole-2(3H)-ylidene)-2-[(5,6,7,8-tetrahydronaphthalen-2-yl)oxy]acetohydrazide (4a–4k) derivatives were synthesized and their anticancer potency were evaluated on human breast ...
Gülhan Turan-Zitouni, Leyla Yurttaş, Aouatef Tabbi, Gülşen Akalın Çiftçi, Halide Edip Temel, Zafer Asım Kaplancıklı   +5 more
doaj   +1 more source