Synthesis, Molecular Modeling of Novel Substituted Pyridazinones and Their Vasorelaxant activities.

Synthesis, Molecular Modeling of Novel Substituted Pyridazinones and Their Vasorelaxant activities. Med Chem. 2020 Mar 27;: Authors: Ismail M, Soliman D, Elmoniem MHA, Jaleel GARA Abstract BACKGROUND: Hypertension, one of the most common cardiovascular diseases that can cause coronary disease, stroke, myocardial infarction and sudden death, it is the major contributor to cardiac failure as well as renal insufficiency. OBJECTIVES: As there are many cardio-active pyridazinone-base derivatives in clinical use, therefore, it we aimed to synthesize a new series of pyridazin-3-ones and evaluate their vasorelaxant activity. METHODS: The new series of synthesized compounds were carried out first by synthesis of 6-flouroarylpyridazinones by cyclization of 3-(4-flourobenzoyl) propionic acid with hydrazine hydrate or arylhydrazines to provide the corresponding pyridazinone derivatives 2a-d. Mannich reaction was performed using morpholine or piperidine formaldehyde to obtain compounds 3a,b. On the other hand reaction of 2a with various chloroacetamide intermediates, in dimethylformamide and potassium carbonate as a catalyst, afforded the target compounds 5a-c. The aromatic acid hydrazides intermediates 6a-g were prepared in 50-90% yield, by reacting the prepared esters with hydrazine hydrate under reflux in ethanol. The two compounds 8a,b were prepared via condensation of 7a,b with ethyl chloroacetate in dry acetone. Finally, the target 2,4,6-trisubstitute...
Source: Medicinal Chemistry - Category: Chemistry Authors: Tags: Med Chem Source Type: research

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In conclusion, the findings of the present study suggested that miR‑340‑5p may protect PC12 cells against OGD/R through targeting Neurod4, which could provide important implications for the treatment of ischemia‑reperfusion injury based on miR‑340‑5p expression levels in vivo. PMID: 32468054 [PubMed - as supplied by publisher]
Source: Molecular Medicine Reports - Category: Molecular Biology Tags: Mol Med Rep Source Type: research
Authors: Susmitha K, Chandrasekhar V, Kiran G, Divya A, Rani GS, Sarangapani M Abstract Stroke is becoming a main cause of early death and disability in developing countries like India, and it is mostly enhanced by increased predominance of major risk factors. A detailed knowledge about the nature and magnitude of the stroke cases in this particular area is not only important for acute treatment but also it helps to prevent hospital admissions due to reoccurring stroke. The present study was conducted in the Department of Stroke at MGM Hospital, Warangal, India, to study the patterns of stroke admissions. All the c...
Source: Advances in Experimental Medicine and Biology - Category: Research Tags: Adv Exp Med Biol Source Type: research
Contributors : Yejie Shi ; Jun ChenSeries Type : Expression profiling by high throughput sequencingOrganism : Mus musculusSenescence-associated alterations in microglia may have profound impact on cerebral homeostasis and stroke outcomes. However, the lack of a transcriptome-wide comparison between young and aged microglia in the context of ischemia limits our understanding of aging-related mechanisms. Herein, we performed bulk RNA sequencing analysis of microglia purified from cerebral hemispheres of young adult (10-week-old) and aged (18-month-old) mice 5 days after distal middle cerebral artery occlusion or sham operati...
Source: GEO: Gene Expression Omnibus - Category: Genetics & Stem Cells Tags: Expression profiling by high throughput sequencing Mus musculus Source Type: research
Abstract Stroke is a leading cause of death and disability in developed countries. N-methyl-D-aspartate glutamate receptors (NMDARs) have important roles in stroke pathology and recovery. Depending on their subtypes and locations, these NMDARs may promote either neuronal survival or death. Recently, the functions of previously overlooked NMDAR subtypes during stroke were characterized, and NMDARs expressed at different subcellular locations were found to have synergistic rather than opposing functions. Moreover, the complexity of the neuronal survival and death signaling pathways following NMDAR activation was fur...
Source: Trends in Molecular Medicine - Category: Molecular Biology Authors: Tags: Trends Mol Med Source Type: research
Publication date: Available online 29 May 2020Source: Journal of Electroanalytical ChemistryAuthor(s): Masaki Motoike, Keisuke Kimura, Yuki Kitazumi, Kenji Kano, Osamu Shirai
Source: Journal of Electroanalytical Chemistry - Category: Chemistry Source Type: research
Familial hypercholesterolaemia is often symptomless, but if untreated, patients can die before reaching middle age or even as children, like Rianna Wingett from Essex, pictured.
Source: the Mail online | Health - Category: Consumer Health News Source Type: news
HEART attack symptoms include difficulty breathing, severe chest pain, and feeling sick. But, you could also be at risk of a deadly myocardial infarction and heart disease if your toes turn a strange colour. This is the skin condition you should avoid.
Source: Daily Express - Health - Category: Consumer Health News Source Type: news
Publication date: Available online 29 May 2020Source: Pregnancy HypertensionAuthor(s): Mamoru Morikawa, Michinori Mayama, Yoshihiro Saito, Kinuko Nakagawa, Takeshi Umazume, Kentaro Chiba, Satoshi Kawaguchi, Kazutoshi Cho, Hidemichi Watari
Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health - Category: OBGYN Source Type: research
Publication date: Available online 29 May 2020Source: Pregnancy HypertensionAuthor(s): Adebamike A. Oshunbade, Arsalan Hamid, Seth T. Lirette, Semiu O. Gbadamosi, Wondwosen K. Yimer, Olusola A. Orimoloye, Donald Clark, Daisuke Kamimura, Stephen D. Grado, Elizabeth A. Lutz, Robert J. Mentz, Ervin R. Fox, Javed Butler, B. Gwen Windham, Kenneth R. Butler, Thomas H. Mosley, Michael E. Hall
Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health - Category: OBGYN Source Type: research
Publication date: Available online 29 May 2020Source: Pregnancy HypertensionAuthor(s): Sunitha Suresh, Ariel Mueller, Saira Salahuddin, Heba Naseem, Rohin Dhir, Sarosh Rana
Source: Pregnancy Hypertension: An International Journal of Womens Cardiovascular Health - Category: OBGYN Source Type: research
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