Synthesis of 2-[{2-(1-Acyl-3-aryl-4,5-dihydro-1H­-pyrazol-5-yl)phenoxy}methyl]-5-aryl-1,3,4-oxadiazoles and related compounds as potential pesticides

Cyclization of substituted chalkones 3a,b with hydrazine hydrate followed by acylation of the resulting 3-aryl-4,5-dihydro-5-(2-hydroxyphenyl)-1H-pyrazoles (4a,b) with alkanoic acids furnished 1-acyl-3-aryl-4,5-dihydro-5-(2-hydroxyphenyl)-1H-pyrazoles (5a-d).  The compounds 5a-d are also directly prepared by refluxing 3a,b with hydrazine hydrate in alkanoic acids. Alkylation of 5a-d with ethyl chloroacetate have been yielded the corresponding aryloxyacetates 6a-d.  Aminolysis of the ester 6a-d have resulted in the formation of corresponding substituted aryloxyacetamides 7a-l.  Hydrazinolysis of esters 6a-d with hydrazine hydrate followed by cyclization of the resulting aryloxyacetic acid hydrazides 8a-d with aromatic acids in refluxing POCl3 have afforded the title compounds 9a-t. The compounds 3-9 have been evaluated for their in vitro growth-inhibitory activity against four fungal pests, Alternaria helianthus, Colletotrichum falcatum, fusarium oxysporum and Rhizoctonia solani.  Many of the compounds have displayed promising activity at different concentrations ranging from 313 – 100 mg L-1

Synthesis of 2-[{2-(1-Acyl-3-aryl-4,5-dihydro-1H-pyrazol-5-yl)phenoxy}methyl]- 5-aryl-1,3,4-oxadiazoles and related compounds as potential pesticides

1257-1263Cyclization of substituted chalkones 3a,b with hydrazine hydrate followed by acylation of the resulting 3-aryl-4,5- dihydro-5-(2-hydroxyphenyl)-1H-pyrazoles (4a,b) with alkanoic acids furnished 1-acyl-3-aryl-4,5-dihydro-5-(2- hydroxyphenyl)-1H-pyrazoles (5a-d). The compounds 5a-d are also directly prepared by refluxing 3a,b with hydrazine hydrate in alkanoic acids. Alkylation of 5a-d with ethyl chloroacetate yields the corresponding aryloxyacetates 6a-d. Aminolysis of the ester 6a-d results in the formation of corresponding substituted aryloxyacetamides 7a-ℓ. Hydrazinolysis of esters 6a-d with hydrazine hydrate followed by cyclization of the resulting aryloxyacetic acid hydrazides 8a-d with aromatic acids in refluxing POCl3 affords the title compounds 9a-t. The compounds 3-9 have been evaluated for their in vitro growthinhibitory activity against four fungal pests, Alternaria helianthus, Colletotrichum falcatum, fusarium oxysporum and Rhizoctonia solani. Many of the compounds have displayed promising activity at different concentrations ranging from 3.13 – 100 mg L-1

Association between HSP-Specific T-Cell Counts and Retinal Nerve Fiber Layer Thickness in Patients with Primary Open-Angle Glaucoma

Objective: Previous laboratory reports implicate heat shock protein (HSP)–specific T-cell responses in glaucoma pathogenesis; here, we aimed to provide direct clinical evidence by correlating systemic HSP-specific T-cell levels with glaucoma severity in patients with primary open-angle glaucoma (POAG). Design: Cross-sectional case-control study. Subjects: Thirty-two adult patients with POAG and 38 controls underwent blood draw and optic nerve imaging. Methods: Peripheral blood monocytes (PBMC) were stimulated in culture with HSP27, α-crystallin, a member of the small HSP family, or HSP60. Both interferon-γ (IFN-γ)+ CD4+ T helper type 1 cells (Th1) and transforming growth factor-β1 (TGF-β1)+ CD4+ regulatory T cells (Treg) were quantified by flow cytometry and presented as a percentage of total PBMC counts. Relevant cytokines were measured using enzyme-linked immunosorbent assays. Retinal nerve fiber layer thickness (RNFLT) was measured with OCT. Pearson’s correlation (r) was used to assess correlations. Main Outcome Measures: Correlations of HSP-specific T-cell counts, and serum levels of corresponding cytokine levels with RNFLT. Results: Patients with POAG (visual field mean deviation, -4.7 ± 4.0 dB) and controls were similar in age, gender, and body mass index. Moreover, 46.9% of POAG and 60.0% of control subjects had prior cataract surgery (P = 0.48). Although no significant difference in total nonstimulated CD4+ Th1 or Treg cells was detected, patients with POAG exhibited significantly higher frequencies of Th1 cells specific for HSP27, α-crystallin, or HSP60 than controls (7.3 ± 7.9% vs. 2.6 ± 2.0%, P = 0.004; 5.8 ± 2.7% vs. 1.8 ± 1.3%, P < 0.001; 13.2 ± 13.3 vs. 4.3 ± 5.2, P = 0.01; respectively), but similar Treg specific for the same HSPs compared with controls (P ≥ 0.10 for all). Concordantly, the serum levels of IFN-γ were higher in POAG than in controls (36.2 ± 12.1 pg/ml vs. 10.0 ± 4.3 pg/ml; P < 0.001), but TGF-β1 levels did not differ. Average RNFLT of both eyes negatively correlated with HSP27- and α-crystallin-specific Th1 cell counts, and IFN-γ levels in all subjects after adjusting for age (partial correlation coefficient r = -0.31, P = 0.03; r = -0.52, p = 0.002; r = -0.72, P < 0.001, respectively). Conclusions: Higher levels of HSP-specific Th1 cells are associated with thinner RNFLT in patients with POAG and control subjects. The significant inverse relationship between systemic HSP-specific Th1 cell count and RNFLT supports the role of these T cells in glaucomatous neurodegeneration. Financial Disclosure(s): Proprietary or commercial disclosure may be found after the references

Metadata record for: HIT-COVID, a global database tracking public health interventions to COVID-19

This dataset contains key characteristics about the data described in the Data Descriptor HIT-COVID, a global database tracking public health interventions to COVID-19. Contents: 1. human readable metadata summary table in CSV format 2. machine readable metadata file in JSON forma