Design, synthesis and biological activities of 1,2,4-triazolo[1,5-a]pyrimidine-7-amine derivatives bearing 1,2,4-oxadiazole motif

Article Chemistry, Organic

Synthesis and biological evaluation of novel 2-arylquinoline-3-fused thiazolo[2,3-c]1,2,4-triazole heterocycles as potential antiproliferative and antimicrobial agents

Ramulu Dhanavath et al.

Summary: A series of novel compounds were synthesized efficiently and characterized, with some of them showing significant antiproliferative and antimicrobial activities.

JOURNAL OF HETEROCYCLIC CHEMISTRY (2022)

Add to Collection

Article Biochemistry & Molecular Biology

Synthesis, structural, spectral, antioxidant, bioactivity and molecular docking investigations of a novel triazole derivative

Can Alasalvar et al.

Summary: The structural, spectroscopic and electronic properties of a triazole compound were analyzed both theoretically and experimentally, and its radical scavenging activities were evaluated and compared with standard compounds.

JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS (2022)

Add to Collection

Article Chemistry, Multidisciplinary

Design, Synthesis, and Anti-Proliferative Activity of Quinoxaline Linked 1,2,4-Oxadiazole Hybrids

Vinitha Badithapuram et al.

Summary: This study presents the synthesis of new quinoxaline-1,2,4-oxadiazole derivatives and examines their in vitro anti-cancer activity against four human cancer cell lines. The results reveal promising anti-cancer activity for four of the tested products, with one product showing higher activity than the standard drug etoposide against all tested cell lines. Molecular docking studies suggest that the most potent compound strongly binds to the EGFR protein. Two compounds also exhibit promising inhibitory activity of the tyrosine kinase EGFR.

RUSSIAN JOURNAL OF GENERAL CHEMISTRY (2022)

Add to Collection

Article Chemistry, Multidisciplinary

Novel 1,2,4-oxadiazole/pyrrolidine hybrids as DNA gyrase and topoisomerase IV inhibitors with potential antibacterial activity

Firas Obaid Arhema Frejat et al.

Summary: DNA gyrase is a promising target for antibacterial agents. A small library of 1,2,4-oxadiazole/pyrrolidine hybrids has been designed with high inhibitory and potent antibacterial activities against DNA gyrase and topoisomerase IV. Compound 16 has shown the highest inhibitory activity and is more potent than novobiocin.

ARABIAN JOURNAL OF CHEMISTRY (2022)

Add to Collection

Article Engineering, Chemical

Synthesis, insecticidal activities and DFT study of pyrimidin-4-amine derivatives containing the 1,2,4-oxadiazole motif

Yong-Hui Wen et al.

Summary: Twenty six novel pyrimidin-4-amine derivatives containing the 1,2,4-oxadiazole motif were synthesized and their chemical structures were confirmed. Some of these compounds showed excellent insecticidal activity against Mythimna separate, but were inactive against Aphis medicagini and Tetranychus cinnabarinus. The study discussed the structure-insecticidal activity relationships and suggested the potential use of density functional theory analysis for designing more active compounds. These findings provide valuable information for further optimization of insecticides.

FRONTIERS OF CHEMICAL SCIENCE AND ENGINEERING (2022)

Add to Collection

Article Agriculture, Multidisciplinary

Novel Dioxolane Ring Compounds for the Management of Phytopathogen Diseases as Ergosterol Biosynthesis Inhibitors :Synthesis, Biological Activities, and Molecular Docking

Li-Jing Min et al.

Summary: In this study, thirty novel dioxolane ring compounds were designed and synthesized. Their chemical structures were confirmed, and bioassays showed that these compounds exhibited excellent fungicidal and herbicidal activity. The study also revealed their target in plants and the mechanism of enzyme inhibition. The structure-activity relationships were discussed, providing useful information for designing more active compounds.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY (2022)

Add to Collection

Article Chemistry, Physical

Synthesis of novel naphthalimide tethered 1,2,3-triazoles: In vitro biological evaluation and docking study of anti-inflammatory inhibitors

Rosina Begam et al.

Summary: A novel heterocyclic naphthalimide tethered 1,2,3-triazoles compound was synthesized using click chemistry. The chemical structure was confirmed through spectral data and X-ray diffraction technique. The compound 10a exhibited potent anti-inflammatory and protein denaturation inhibition activities, as well as stronger COX1 and COX2 inhibitory effects.

JOURNAL OF MOLECULAR STRUCTURE (2022)

Add to Collection

Article Chemistry, Inorganic & Nuclear

Design, synthesis and nematocidal activity of novel 1,2,4-oxadiazole derivatives with a 1,3,4-thiadiazole amide moiety

Dan Liu et al.

Summary: A series of novel 1,2,4-oxadiazole derivatives containing 1,3,4-thiadiazole amide group were synthesized and their nematocidal activities were evaluated. Compounds 4i and 4p showed good nematocidal activity against Bursaphelenchus xylophilus and exhibited inhibition of its activity and respiration, leading to fluid leakage. Furthermore, they have good druggability properties similar to those of Tioxazafen.

PHOSPHORUS SULFUR AND SILICON AND THE RELATED ELEMENTS (2022)

Add to Collection

Article Chemistry, Medicinal

Structure-based screening for the discovery of 1,2,4-oxadiazoles as promising hits for the development of new anti-inflammatory agents interfering with eicosanoid biosynthesis pathways

Marianna Potenza et al.

Summary: This study identified three 1,2,4-oxadiazole compounds as potential multi-target inhibitors in the treatment of inflammatory disorders, with compound 5 showing promising results in in vivo experiments. The results suggest the potential for developing novel anti-inflammatory agents with a favorable pharmacological profile by expanding chemical diversity around the 1,2,4-oxadiazole central core.

EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY (2021)

Add to Collection

Article Agriculture, Multidisciplinary

Synthesis and Biological Evaluation of 1,2,4-Triazole Thioethers as Both Potential Virulence Factor Inhibitors against Plant Bacterial Diseases and Agricultural Antiviral Agents against Tobacco Mosaic Virus Infections

Wu-Bin Shao et al.

Summary: Targeting the virulence factors of phytopathogenic bacteria is a novel strategy for disease control. Compound A10 showed significant inhibition of Xoo virulence factors and antiviral activity against tobacco mosaic virus, indicating its potential as a versatile agricultural chemical.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY (2021)

Add to Collection

Article Agriculture, Multidisciplinary

Design, Synthesis, and Pesticidal Activities of Pyrimidin-4-amine Derivatives Bearing a 5-(Trifluoromethyl)-1,2,4-oxadiazole Moiety

Xing-Hai Liu et al.

Summary: The study designed and synthesized a series of novel pyrimidin-4-amine derivatives with good insecticidal and fungicidal activities. Among them, compounds U7 and U8 showed broad-spectrum activity, and further optimization is possible. The structure-activity relationships were discussed, and density functional theory analysis may help design more active compounds.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY (2021)

Add to Collection

Article Agriculture, Multidisciplinary

Synthesis, Crystal Structure, Herbicidal Activity, and SAR Study of Novel N-(Arylmethoxy)-2-chloronicotinamides Derived from Nicotinic Acid

Chen-Sheng Yu et al.

Summary: Nicotinic acid, also known as niacin, is a natural product found in plants and animals. In this study, N-(arylmethoxy)-2-chloronicotinamides were designed and synthesized as potential herbicides. Some of these compounds showed promising herbicidal activity and could be used for the development of new herbicides against monocotyledonous weeds.

JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY (2021)

Add to Collection

Article Chemistry, Multidisciplinary

In-vitro Anticancer and Molecular Docking Studies of 4-Azaindole-1,2,4-Oxadiazole Hybrids

Ravikumar Reddy Sagam et al.

Summary: This study described the synthesis of novel 4-azaindole-1,2,4-oxadiazole hybrids and identified three compounds with superior inhibitory activity against melanoma, breast cancer, and lung cancer cell lines. In particular, compound 5 m exhibited outstanding activity in MCF-7 cancer cell line. Further in silico studies confirmed the interactions of these compounds with EGFR receptor and their promising inhibitory activity against tyrosine kinase EGFR.

CHEMISTRYSELECT (2021)

Add to Collection

Article Chemistry, Medicinal

Design and Synthesis of Novel Thiazolo[5,4-d]pyrimidine Derivatives with High Affinity for Both the Adenosine A1 and A2A Receptors, and Efficacy in Animal Models of Depression

Flavia Varano et al.

Summary: New compounds with high affinity and antidepressant-like activity were synthesized and evaluated in vitro for their potential as A(1) and A(2A) adenosine receptor ligands.

PHARMACEUTICALS (2021)

Add to Collection

Article Chemistry, Organic

Synthesis, Cyrstal Structure and Fungicidal Activity of New Triazole Compounds Containing Trifluoromethylphenyl Moiety

Chensheng Yu et al.

Summary: A series of 1,2,4-triazole compounds were designed and synthesized with Uniconazole as the template compound, and their structures were confirmed using various spectra methods. The X-ray single crystal diffraction determined the crystal structure of one of the compounds. Bioassay data showed that some target compounds exhibited good activity against Sclerotinia sclerotiorum and Rhizoctonia solani at a concentration of 50 μg/mL.

CHINESE JOURNAL OF ORGANIC CHEMISTRY (2021)

Add to Collection

Article Chemistry, Organic

Synthesis and Fungicidal Activity of Novel Allyl Benzoate Compounds Containing Triazole

Wei Yu et al.

Summary: A series of unreported allyl benzoate compounds containing triazole were synthesized and tested for fungicidal activity, showing that three compounds exhibited good control efficacy against Sclerotinia sclerotiorum. This study demonstrates the potential of these new compounds as pesticide lead compounds.

CHINESE JOURNAL OF ORGANIC CHEMISTRY (2021)

Add to Collection

Article Chemistry, Organic

Synthesis and antimicrobial evaluation of novel polyheterocyclic systems derived from cyclopenta[4′,5′]pyrido[3′,2′:4,5]furo[3,2-d]pyrimidine

Samvel N. Sirakanyan et al.

Summary: The synthesis of new cyclopenta[4',5']pyrido[3',2':4,5]furo[3,2-d]pyrimidin-7-amines has shown potent antimicrobial properties, with the 3,5-dimethyl-1H-pyrazol-1-yl moiety playing a crucial role in their activity. The impact of the 3,5-dimethyl-1H-pyrazol-1-yl group on Dimroth rearrangement and azide-tetrazole equilibrium has also been explored.

CHEMISTRY OF HETEROCYCLIC COMPOUNDS (2021)

Add to Collection

Article Agronomy