Hameed P, Shahul’s team published research in Journal of Medicinal Chemistry in 2014-07-10 | CAS: 502546-41-0

Journal of Medicinal Chemistry published new progress about Antimalarials. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Category: triazoles.

Hameed P, Shahul published the artcileAminoazabenzimidazoles, a Novel Class of Orally Active Antimalarial Agents, Category: triazoles, the main research area is aminoazabenzimidazole preparation SAR antimalarial Plasmodium.

Whole-cell high-throughput screening of the AstraZeneca compound library against the asexual blood stage of Plasmodium falciparum (Pf) led to the identification of amino imidazoles, a robust starting point for initiating a hit-to-lead medicinal chem. effort. Structure-activity relation studies followed by pharmacokinetics optimization resulted in the identification of (I) as an attractive lead with good oral bioavailability. Compound I was efficacious (ED90 of 28.6 mg·kg-1) in the humanized P. falciparum mouse model of malaria (Pf/SCID model). Representative compounds displayed a moderate to fast killing profile that is comparable to that of chloroquine. This series demonstrates no cross-resistance against a panel of Pf strains with mutations to known antimalarial drugs, thereby suggesting a novel mechanism of action for this chem. class.

Journal of Medicinal Chemistry published new progress about Antimalarials. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Category: triazoles.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Sanchez, Robert M.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2012-05-01 | CAS: 502546-41-0

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Application In Synthesis of 502546-41-0.

Sanchez, Robert M. published the artcileSynthesis and structure-activity relationships of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones as novel series of potent β isoform selective phosphatidylinositol 3-kinase inhibitors, Application In Synthesis of 502546-41-0, the main research area is triazolo pyrimidinone preparation phosphatidylinositol 3 kinase inhibitor anticancer SAR.

A series of 1,2,4-triazolo[1,5-a]pyrimidin-7(3H)-ones with excellent enzyme inhibition, improved isoform selectivity, and excellent inhibition of downstream phosphorylation of AKT has been identified. Several compounds in the series demonstrated potent (∼ 0.100 μM IC50) growth inhibition in a PTEN deficient cancer cell line.

Bioorganic & Medicinal Chemistry Letters published new progress about Antitumor agents. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Application In Synthesis of 502546-41-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Clough, John M.’s team published research in Pest Management Science in 2016 | CAS: 502546-41-0

Pest Management Science published new progress about Amaranthus retroflexus. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, HPLC of Formula: 502546-41-0.

Clough, John M. published the artcileSynthesis and evaluation of hydroxyazolopyrimidines as herbicides; the generation of amitrole in planta, HPLC of Formula: 502546-41-0, the main research area is hydroxyazolopyrimidine amitrole herbicide azolopyrimidine; amitrole; herbicides; metabolism; mode of action.

BACKGROUND : Exploiting novel herbicidal modes of action is an important method to overcome the challenges faced by increasing resistance and regulatory pressure on existing com. herbicides. Recent reports of inhibitors of enzymes in the non-mevalonate pathway of isoprenoid biosynthesis led to the design of a novel class of azolopyrimidines which were assessed for their herbicidal activity. Studies were also undertaken to determine the mode of action responsible for the observed herbicidal activity. RESULTS : In total, 30 novel azolopyrimidines were synthesized and their structures were unambiguously determined by 1H NMR, mass spectroscopy and X-ray crystallog. anal. The herbicidal activity of this new chem. class was assessed against six common weed species, with compounds from this series displaying bleaching symptomol. in post-emergence tests. A structure-activity relationship for the novel compounds was determined, which showed that only those belonging to the hydroxytriazolopyrimidine subclass displayed significant herbicidal activity. Observed similarities between the bleaching symptomol. displayed by these herbicides and amitrole suggested that hydroxytriazolopyrimidines could be acting as elaborate propesticides of amitrole, and this was subsequently demonstrated in plant metabolism studies using Amaranthus retroflexus. It was shown that selected hydroxytriazolopyrimidines that displayed promising herbicidal activity generated amitrole, with peak concentrations of amitrole generally being observed 1 day after application. Addnl., the herbicidal activity of selected compounds was profiled against tobacco plants engineered to overexpress 4-diphosphocytidyl-2C-methyl-D-erythritol synthase (IspD) or lycopene β-cyclase, and the results suggested that, where significant herbicidal activity was observed, inhibition of IspD was not responsible for the activity. Tobacco plants overexpressing lycopene β-cyclase showed tolerance to amitrole and the two most herbicidally active triazolopyrimidines. CONCLUSIONS : Inhibition of IspD leading to herbicidal activity has been ruled out as the mode of action for the hydroxytriazolopyrimidine class of herbicides. Addnl., tobacco plants overexpressing lycopene β-cyclase showed tolerance to amitrole, which indicates that this is the main herbicidal mode of action for amitrole. Results from the metabolic fate study of selected hydroxytriazolopyrimidines suggested that the herbicidal activity displayed by these compounds is due to amitrole production, which was confirmed when tobacco plants overexpressing lycopene β-cyclase also showed tolerance towards two triazolopyrimidines from this study. © 2016 Society of Chem. Industry.

Pest Management Science published new progress about Amaranthus retroflexus. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, HPLC of Formula: 502546-41-0.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Cox, Jason M.’s team published research in Bioorganic & Medicinal Chemistry Letters in 2016-06-01 | CAS: 502546-41-0

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Application of 5-Cyclopropyl-4H-1,2,4-triazol-3-amine.

Cox, Jason M. published the artcileThe discovery of novel 5,6,5- and 5,5,6-tricyclic pyrrolidines as potent and selective DPP-4 inhibitors, Application of 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, the main research area is tricyclic pyrrolidine preparation DPP4 inhibitor structure diabetes; Dipeptidyl peptidase IV (DPP-4); Omarigliptin; Sitagliptin; Type 2 diabetes mellitus.

Novel potent and selective 5,6,5- and 5,5,6-tricyclic pyrrolidine dipeptidyl peptidase IV (DPP-4) inhibitors were identified. Structure-activity relationship (SAR) efforts focused on improving the intrinsic DPP-4 inhibition potency, increasing protease selectivity, and demonstrating clean ion channel and cytochrome P 450 profiles while trying to achieve a pharmacokinetic profile suitable for once weekly dosing in humans.

Bioorganic & Medicinal Chemistry Letters published new progress about Antidiabetic agents. 502546-41-0 belongs to class triazoles, name is 5-Cyclopropyl-4H-1,2,4-triazol-3-amine, and the molecular formula is C5H8N4, Application of 5-Cyclopropyl-4H-1,2,4-triazol-3-amine.

Referemce:
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics