Results 31 to 40 of about 35,216 (249)

Breakthrough Design of Highly Potent Antivirals Against Wild‐Type HIV‐1 and Lenacapavir‐Resistant M66I Variant

Angewandte Chemie, EarlyView.
Lenacapavir, the first‐in‐class drug targeting HIV‐1 capsid, is a breakthrough drug in HIV‐1 treatment and prophylaxis. However, a single M66I mutation confers complete viral resistance to lenacapavir. We report herein the design and synthesis of innovative R2 analogs demonstrating low nM potency against HIV‐1 M66I and excellent pharmacokinetics in ...
Nicolas Jamey, D. M. Nirosh Udayanga, Huanchun Zhang, Roshan Katekar, Wei Xie, Shreya M. Ravichandran, Xinyong Cai, Zachary C. Lorson, William M. McFadden, Won Hee Ryu, Jiashu Xie, Karen A. Kirby, Stefan G. Sarafianos, Zhengqiang Wang   +13 more
wiley   +2 more sources

Chiral versus achiral crystal structures of 4-benzyl-1H-pyrazole and its 3,5-diamino derivative

Acta Crystallographica Section E: Crystallographic Communications
The crystal structures of 4-benzyl-1H-pyrazole (C10H10N2, 1) and 3,5-diamino-4-benzyl-1H-pyrazole (C10H12N4, 2) were measured at 150 K. Although its different conformers and atropenantiomers easily interconvert in solution by annular tautomerism and/or ...
Emily R. Hayward, Matthias Zeller, Gellert Mezei   +2 more
doaj   +1 more source

Chemistry and biomedical relevance of pyrazole derivatives: An integrated review [PDF]

EPJ Web of Conferences
Over the past decades, the interest in the synthesis and applications of different pyrazole derivatives has been increased dramatically. Pyrazole is well known five-member ring found to be present in many plants and microorganisms.
Dubal Gaurang, Joshi Kaushik, Talaviya Rahul   +2 more
doaj   +1 more source

A de‐novo Approach Towards Divergent [3+2π/σ] Photocycloadditions of Nitrones via Assembly‐Controlled Kinetic Electron Transfer Gating

Angewandte Chemie, EarlyView.
A metal‐free photocatalytic platform converts nitrones into 4‐isoxazolines and oxa–aza–bicycloheptanes through divergent [3+2π/σ] cycloadditions. Assembly‐controlled kinetic electron transfer gating dictates substrate activation, enabling selective reactivity beyond thermodynamic expectations.
Nayan Saha, Rajesh Kancherla, Jorge Escorihuela, Shana Chandran, Mrinal K. Bera, Magnus Rueping, Burkhard König   +6 more
wiley   +2 more sources

DataSheet1_Synthesis, antioxidant, and antimicrobial evaluation of novel 2,3-dihydro-1H-pyrazole-4-carbonitrile derivatives using K2CO3/glycerol as a green deep eutectic solvent.PDF

, 2023
Providing green methods for the synthesis of new heterocyclic compounds with biological properties is interesting for scientists. Through the multi-component reaction of aldehyde derivatives, methyl 2-cyanoacetate, and phenylhydrazine using K2CO3, and ...
Benien M. Ridha (16499580), Ali Alsalamy (16499583), Mustafa Kahtan (16499568), Enas Abdulgader Hassan (16499574), Mohammed Asiri (16499577), Ali A. Zwain (16499562), Atheer Khdyair Hamad (16499571), Rasha Khalaf Jebur Ali (16499565), Irfan Ahmad (194014)   +8 more
core   +1 more source

Choline chloride/urea as a green and efficient deep eutectic solvent in three-component and four-component synthesis of novel pyrazole and pyrano[2,3-c] pyrazole derivatives with antibacterial and antifungal activity

Frontiers in Chemistry
In this study, choline chloride/urea was used as a green deep eutectic solvent in the three-component reaction of hydrazine/phenylhydrazine, malononitrile, and aromatic aldehydes for synthesizing pyrazole derivatives, and in the four-component reaction ...
Israa Habeeb Naser, Hassan Thoulfikar A. Alamir, Ali Hisham Al-Shukarji, Batool Ali Ahmed, Talal Aziz Qassem, Maher Kamal, Tahani M. Almeleebia, Enas R. Alwaily, Eftikhaar Hasan Kadhum, Ahmed Alawadi, Ahmed Alawadi, Ahmed Alawadi, Ali Alsalamy   +12 more
doaj   +1 more source

{2,6-Bis[(2,6-diisopropylphosphanyl)oxy]-4-fluorophenyl-κ3P,C1,P′}(1H-pyrazole-κN2)nickel(II) hexafluorophosphate

Acta Crystallographica Section E, 2012
The title compound, [Ni(C18H30FO2P2)(C3H4N2)]PF6, was prepared by halide abstraction with TlPF6 in the presence of CH3CN in CDCl3 from the respective neutral pincer chlorido analogue followed by addition of pyrazole.
Man-Lung Kwan, Sara J. Conry, Charles S. Carfagna, Loren P. Press, Oleg V. Ozerov, Norris W. Hoffman, Richard E. Sykora   +6 more
doaj   +1 more source

Recent Advancement in Drug Design and Discovery of Pyrazole Biomolecules as Cancer and Inflammation Therapeutics

Molecules, 2022
Pyrazole, an important pharmacophore and a privileged scaffold of immense significance, is a five-membered heterocyclic moiety with an extensive therapeutic profile, viz., anti-inflammatory, anti-microbial, anti-anxiety, anticancer, analgesic ...
Md. Jahangir Alam, Ozair Alam, Mohd. Javed Naim, Farah Nawaz, Ajay Manaithiya, Mohd Imran, Hamdy Khamees Thabet, Sultan Alshehri, Mohammed M. Ghoneim, Prawez Alam, Faiyaz Shakeel   +10 more
doaj   +1 more source

Flavin Catalysts in Organic Synthesis

Angewandte Chemie, EarlyView.
Flavins and their congeners are potent catalysts for organic synthesis inspired by enzymatic transformations. In addition to catalysis in the flavin ground state via covalent intermediates, the excited singlet and triplet states unlock applications including photooxidation, photoreduction, and energy transfer via sensitization.
Jan Freudenberg, Golo Storch
wiley   +2 more sources

2,6-Bis(1-isopropyl-5-phenyl-1H-pyrazol-3-yl)pyridine

Acta Crystallographica Section E, 2008
In the title compound, C29H29N5, the central pyridine ring and the two pyrazole rings are approximately coplanar, the dihedral angles between the pyridine and pyrazole rings being 3.94 (12) and 14.84 (12)°.
Ping Liu, Yong-Bo Zhou, Min-Guo Li, Cai-Xia An   +3 more
doaj   +1 more source