Results 21 to 30 of about 12,612 (175)

iNOS/PGE₂ inhibitors as a novel template for analgesic/anti-inflammatory activity: Design, synthesis, in vitro biological activity and docking studies. [PDF]

Arch Pharm (Weinheim)
Using published studies, pharmacophore groups of anti‐inflammatory agents with 1,3,4‐oxadiazole and 1,2,4‐triazole nuclei were determined. Docking studies of identified pharmacophore groups on inducible nitric oxide synthase (iNOS) were performed to identify potent derivatives. New 1,3,4‐oxadiazoles (3a–f, 4a–f) and their cyclized 1,2,4‐triazolo[3,4‐b][
Erdogan A, Ozhan Y, Sipahi H, Gurdal EE, Sippl W, Koksal M.   +5 more
europepmc   +2 more sources

Recent Synthetic Advances in C-H/N-H Functionalization of 1H-Pyrazoles: Diverse Strategies Across Variously Substituted Scaffolds. [PDF]

Chem Rec
Systematic overview of pyrazole functionalization reactions from C‐5 to N−H. It covers different strategies, from traditional cross‐coupling of prefunctionalized pyrazoles to more efficient direct functionalizations. This review briefly and systematically overviews C–H and N–H functionalization reactions of pyrazoles, aimed at creating new CC and C ...
Dzedulionytė Müldür K, Žukauskaitė A, Šačkus A, Arbačiauskienė E.   +3 more
europepmc   +2 more sources

Integrative Insights Into DYRK1A From Molecular Function to Therapeutic Advancement. [PDF]

Chem Biol Drug Des
At the center the 3D structure of DYRK1A has been displayed. The dual‐function of DYRK1A involved in cancer and neurodegeneration, i.e., its overexpression drives Down syndrome, neurodegenerative disease etc., and underexpression causes intellectual disability, seizures, etc.
Paul S, Dubey S, Tiwari P.
europepmc   +2 more sources

Synthesis and molecular docking studies of novel tricyclic and angular tetracyclic benzothiadiazines via sp3‐C‐H activation as potential colon cancer inhibitors

Journal of Heterocyclic Chemistry, Volume 60, Issue 10, Page 1738-1759, October 2023., 2023
Substituted tricyclic and tetracyclic benzothiadiazines were synthesized in this paper, were synthesized via metal‐free intramolecular N‐iodosuccinimide (NIS)‐mediated radical oxidative sp3‐C‐H activation aminative cyclization. Docking studies of the tricyclic and angular tetracyclic 1,2,4‐benzothiadizine dioxides 26–34 and intermediates were carried ...
Sherif O. Kolade, Oluwafemi S. Aina, Allen T. Gordon, Eric C. Hosten, Idris A. Olasupo, Adeniyi S. Ogunlaja, Olayinka T. Asekun, Oluwole B. Familoni   +7 more
wiley   +1 more source

Design, Synthesis, in vitro and in silico Characterization of 2‐Quinolone‐L‐alaninate‐1,2,3‐triazoles as Antimicrobial Agents

ChemMedChem, Volume 17, Issue 5, March 4, 2022., 2022
Antibiotics that click: Inspired by the broad antibacterial activities of various heterocyclic compounds such as 2‐quinolone derivatives, we designed and synthesized new methyl‐(2‐oxo‐1,2‐dihydroquinolin‐4‐yl)‐L‐alaninate‐1,2,3‐triazole derivatives via 1,3‐dipolar cycloaddition reaction of 1‐propargyl‐2‐quinolone‐L‐alaninate with appropriate azide ...
Oussama Moussaoui, Rajendra Bhadane, Riham Sghyar, Janez Ilaš, El Mestafa El Hadrami, Said Chakroune, Outi M. H. Salo‐Ahen   +6 more
wiley   +1 more source

Inverse Electron-Demand Aza-DielsAlder Reaction of ,-Unsaturated Thioesters with In Situ-Generated 1,2-Diaza-1,3-dienes for the Synthesis of 1,3,4-Thiadiazines

, 2022
A highly regioselective inverse electron-demand aza-Diels–Alder reaction of α,β-unsaturated thioesters with 1,2-diaza-1,3-dienes generated in situ from α-halogeno hydrazones was developed.
Yong You, Yan-Ping Zhang, Yong You (28100), Zhen-Hua Wang (435746), Li-Wen Shen, Wei-Cheng Yuan, Wei-Cheng Yuan (1457101), Jian-Qiang Zhao (706458), Jian-Qiang Zhao, Li-Wen Shen (8681013), Yan-Ping Zhang (432349), Zhen-Hua Wang   +11 more
core   +1 more source

Synthesis and Biological Activity of Some Novel Derivatives of 4-Amino-3-(D-galactopentitol-1-yl)-5-mercapto-1,2,4-triazole

Molecules, 2007
To discover new 1,2,4-triazole derivatives which may possess significant biological activities, we synthesized a series of novel 6-aryl-3-(D-galactopentitol-1-yl)- 7H-1,2,4-triazolo[3,4-b][1,3,4]thiadiazines and 4-(arylmethylidene)amino-5-(D ...
Jiang-Hai Zhu, Xin-Xiang Lei, An-jiang Zhang, Li-xue Zhang, Jian-yu Jin   +4 more
doaj   +1 more source

Pharmacologic Evaluation of Antidepressant Activity and Synthesis of 2-Morpholino-5-phenyl-6H-1,3,4-thiadiazine Hydrobromide

Pharmaceuticals, 2016
Substituted thiadiazines exert a reliable therapeutic effect in treating stress, and a schematic description of their ability to influence all aspects of a stress response has been depicted. This study was conducted to pharmacologically evaluate compound
Alexey P. Sarapultsev, Oleg N. Chupakhin, Petr A. Sarapultsev, Larisa P. Sidorova, Tatiana A. Tseitler   +4 more
doaj   +1 more source

Synthesis and Antiviral Activity of Novel 1,3,4-Thiadiazine Derivatives

Chemical and Pharmaceutical Bulletin, 2011
A series of novel 1,3,4-thiadiazine derivatives were synthesized via chemical optimization on phthiobuzone. Their anti-herpes simplex virus (HSV) activities in vitro were also tested. Several compounds exhibited more highly potent anti-HSV activity and much higher selectivity index (SI) values than those of phthiobuzone.
Yang, Yajun, Feng, Ziming, Jiang, Jianshuang, Yang, Yanan, Pan, Xiandao, Zhang, Peicheng   +5 more
openaire   +3 more sources

Computational Study of Ignored Pericyclic Reactions: Rearrangements of 1,2‐Bis(Diazo)Alkanes to 1,2,3,4‐Tetrazines and Subsequent Fragmentations

Angewandte Chemie, Volume 137, Issue 45, November 3, 2025.
DFT calculations of the 8π‐electrocyclization of 1,2‐bis(diazo)alkanes and of other bis‐1,3‐dipoles reveal that this process can establish a so far ignored route to heterocycles such as 1,2,3,4‐tetrazines. Alternative reaction channels via carbenes or nitrenes leading to fragmentation products are discussed.
Hans‐Ulrich Reissig, Ernst‐Ulrich Würthwein   +1 more
wiley   +2 more sources