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2021 ◽  
Vol 21 (1) ◽  
Author(s):  
Wenyuan Liu ◽  
Yanjia Lv ◽  
Xiaoyue Li ◽  
Zongqin Feng ◽  
Lichen Wang

Abstract Background Tetraploid cotton plants serve as prime natural fiber source for the textile industry. Although various omics studies have revealed molecular basis for fiber development, a better understanding of transcriptional regulation mechanism regulating lint fiber initiation is necessary to meet global natural fiber demand. Results Here, we aimed to perform transcriptome sequencing to identify DEGs (differentially expressed genes) in ovules of the cotton variety Xu142 and its fibreless mutant Xu142fl during early lint fiber initiation period. Totally, 5516 DEGs including 1840 upregulated and 3676 downregulated were identified. GO enrichment analysis revealed that the downregulated DEGs were mainly associated with biological processes such as transcription related biosynthesis and metabolism, organic cyclic compound biosynthesis and metabolism, photosynthesis, and plant cell wall organization, with molecular functions involving transcription related binding, organic cyclic compound binding, and dioxygenase activity, while the upregulated DEGs were associated with DNA replication and phospholipid biosynthetic related processes. Among the 490 DEGs annotated as transcription factor genes, 86.5% were downregulated in the mutant including the Malvaceae-specific MMLs, expression patterns of which were confirmed during the central period of lint fiber initiation. Investigation of the 16 genes enriched in the cell wall organization revealed that 15 were EXPA coding genes. Conclusions Overall, our data indicate that lint fiber initiation is a complicated process involving cooperation of multiple transcription factor families, which might ultimately lead to the reorganization of the cell wall and terminated cell division of the differentiating fiber initials.


Author(s):  
Ravi Kumar Konda ◽  
Anish Kumar K ◽  
Phani Lakshman M ◽  
Mohammed Asif ◽  
Anusha Reddy D

Heterocyclic compounds are cyclic compounds containing carbon and other heteroatoms. The most common heteroatoms are oxygen, nitrogen, and Sulphur. A heterocyclic compound is a cyclic compound that has atoms at least two different elements as members of its ring. A Schiff base (azomethine) is named after its inventor, Hugo Schiff and it is a functional group that contains a carbon-nitrogen double bond with the nitrogen atom connected to an aryl or alkyl group but not hydrogen. Schiff bases of Pyridin-3 yl-carbohydrazide derivatives from ethyl nicotinate and different aromatic aldehydes. Schiff’s bases are aromatic substituted imine compounds. These compounds are very important in the medicinal and pharmaceutical fields because of their wide spectrum of biological activity. Schiff’s bases show antibacterial activity, antifungal activity, and also antitumor activity. Aromatic aldehydes were refluxed with ethyl nicotinate using ethanol as a solvent to form Schiff's bases. All chemicals are taken in equimolar concentrations. The synthesized compounds were characterized by melting point, solubility, percentage yield, TLC, and IR spectral analysis. All derivatives are evaluated for anti-bacterial activity by the cup plate method. The antibacterial activity of test compounds was compared against standard Streptomycin. The 5 synthesized compounds show moderate antimicrobial activity. The experimental work summarizes the synthesis and in-vitro antibacterial activity of Schiff base derivatives.


2021 ◽  
Vol 2021 ◽  
pp. 1-17
Author(s):  
Mingrui Hu ◽  
Yuanyuan Zhong ◽  
Wei Xiao ◽  
Yang Wang ◽  
Tao Tang ◽  
...  

Background. Infertility affects approximately 15% of couples around the world, and male factors are accounted for 40–50%. Oligoasthenozoospermia is the most common reason for male infertility. Unfortunately, effective drug therapy is still lacking except for assisted reproductive technology (ART). Previous researchers found that Wuzi Ershen decoction (WZESD) can increase sperm count, enhance sperm vitality, and improve semen quality. However, the pharmacological mechanisms remain unclear. Methods. In this study, we screened compounds and predicted the targets of WZESD based on the TCMSP and BATMAN-TCM database combined with literature searching in the PubMed database. We obtained proteins related to oligoasthenozoospermia through GeneCards and submitted them to STRING to obtain the protein-protein interaction (PPI) network. Potential targets of WZESD were mapped to the network, and the hub targets were screened by topology. We used online platform Metascape and Enrichr for GO and KEGG enrichment analyses. AutoDock Vina was utilized for further verification of the binding mode between compounds and targets. Results. Totally, 276 bioactive compounds were obtained and targeted 681 proteins. 446 oligoasthenozoospermia disease-specific proteins were acquired, and further bioinformatics analysis found that they were mainly involved in the formation of gametes, meiosis, and sperm differentiation. Protein interaction network analysis revealed that target proteins of WZESD were associated with oligoasthenozoospermia disease-specific proteins. The 79 targets of disease-specific proteins, which were anchored by WZESD, mainly participate in the cellular response to the organic cyclic compound, regulation of the apoptotic process, nitricoxide biosynthetic and metabolic process, oxidative stress, and protein phosphorylation regulation, which are the causes for oligoasthenozoospermia. Molecular docking simulation further validated that bioactive compounds originated from WZESD with targeted proteins showed high binding efficiency. Conclusions. This study uncovers the therapeutic mechanisms of WZESD for oligoasthenozoospermia treatment from the perspective of network pharmacology and may provide a valuable reference for further experimental research studies and clinical applications.


2021 ◽  
pp. 1-5
Author(s):  
Osarumwense Peter Osarodion ◽  
◽  
Omotade Treasure Ejodamen ◽  

Looking at the previous studies on quinazolinones derivatives, only limited information’s are available on their mass spectral along with the preparation of novel quinazolin-4-(3H)-one derivatives The condensation of Methyl-2-amino-4-Chlorobenzoate with acetic anhydride yielded the cyclic compound 2-methyl 7-Chloro-1, 3-benzo-oxazine-4-one (1) which further produce 3-Amino-2-Methyl 7-Chloro quinazolin-4(3H)-ones (2) via the reaction with hydrazine hydrate. The compounds synthesized were unequivocally confirmed by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography-Mass spectrophotometry and Elemental analysis. Discussion: The molecular ion of m/z 235 fragments to give m/z 220 by loss of –NH group. The ion of m/z 220 was broken to give m/z 206 by losing CH2 group and fragment to m/z 177 by loss of HCO. This fragmented to m/z 162 by loss of –CH3 group and then m/z 136 by loss of CN group. The loss of O gave m/z 120 which fragment to give m/z 93 by loss of –HCN and finally gave m/z 65 by loss of CO group. Conclusion: The electron impact ionization mass spectra of compound 2show a weak molecular ion peak and a base peak of m/z 235resulting from a cleavage fragmentation. Compound 2 give a characteristic fragmentation pattern. From the study of the mass spectra of compound 2, it was found that the molecular ion had fragmented to the m/z 220. The final fragmentation led to ion of m/z 93 and ion of mass m/z 65, respectively


2021 ◽  
Author(s):  
Wenyuan Liu ◽  
Yanjia Lv ◽  
Xiaoyue Li ◽  
Zongqin Feng ◽  
Lichen Wang

Abstract Background Tetraploid cotton plants serve as prime natural fiber source for the textile industry. Although various omics studies have revealed molecular basis for fiber development, a better understanding of transcriptional regulation mechanism regulating lint fiber initiation is necessary to meet global natural fiber demand. Conclusions Here, we aimed to perform transcriptome sequencing to identify DEGs (differentially expressed genes) in ovules of the cotton variety Xu142 and its fibreless mutant Xu142fl during early lint fiber initiation period. Totally, 5516 DEGs including 1840 upregulated and 3676 downregulated were identified. GO enrichment analysis revealed that the downregulated DEGs mainly associated with biological processes such as transcription related biosynthesis and metabolism, organic cyclic compound biosynthesis and metabolism, photosynthesis, and plant cell wall organization, with molecular functions involving transcription related binding, organic cyclic compound binding, and dioxygenase activity, while the upregulated DEGs were associated with DNA replication and phospholipid biosynthetic related processes. Among the 490 DEGs annotated as transcription factor genes 86.5% were downregulated in the mutant including the Malvaceae-specific MMLs, expression patterns of which were confirmed during the central period of lint fiber initiation. Investigation of the 20 genes enriched in the cell wall organization revealed that 17 were EXPA coding genes. Overall, we suggest that lint fiber initiation is a complicated process involving cooperation of multiple transcription factor families, which might ultimately lead to the reorganization of the cell wall and terminated cell division of the differentiating fiber initials.


2021 ◽  
Vol 1 (2) ◽  
pp. 077-084
Author(s):  
Peter Osarodion Osarumwense ◽  
Mary Olire Edema ◽  
Cyril Odianosen Usifoh

Background: Quinazoline and quinazolinone scaffolds represent an important class of biologically active nitrogen heterocyclic compounds. Many marketed drugs are based on these moieties. A diverse range of molecules with quinazoline/quinazolinone moieties have been reported to exhibit broad spectrum of biological activities Objective: This study is aimed at the synthesis of these quinazolinone derivatives, quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one and evaluate them for their antibacterial activities. Method: The consolidation of 2-amino-methyl-4-methoxybenzoate with acetic anhydride produced the cyclic compound 2-methyl-4, 5-disubstituted-1, 3-benzo-oxazine-4-one which also produce a novel 2,3-disubstituted quinazolin-4 ones via the reaction with hydrazine hydrate. The quinazolinone derivatives quinazolin-4(3H)-One, 2-Methyl-4(3H)-quinazolinone and 2–Phenyl-4(3H)-quinazolin-4(3H)–one were evaluated pharmacologically for their in vivo analgesic activities by acetic acid induced writhing in mice. The compounds synthesized were assuredly validated by means of Infrared, Nuclear Magnetic Resonance (1H and 13C), Gas Chromatography Mass Spectrophotometer and Elemental analysis. The synthesized compounds were tested for their antibacterial activity.Compounds 1,2 and 3 showed significant antibacterial activities. Discussion: Compound 1 was identified by the absence of methyl group and the presence of methyl group for compound 2. The test analysed compounds exhibited significant antibacterial activities. The compounds synthesized exhibited promising antibacterial activities against the tested organisms. Conclusion: The compounds have high antibacterial activities. Compound 2 has a higher activity compared to Compound 1 and 3. Compound 2 has a higher antibacterial against Escherichia coli, Klebsiella pneumonia and Pseudomonas aeuriginosa


2021 ◽  
Author(s):  
Francisco Ros

Abstract Reaction of 2-chloroisobutyrophenonewith two equivalents of malononitrile anion furnishes 2-amino-1,3-dicyano-5,5-dimethyl-4-phenylcyclopenta-1,3-diene. The cyclic compound represents the novel 2-amino-1,3-dicyanocyclopentadiene structure. The unique 1-cyano-2-amino-3-cyano arrangement in the cyclopentadiene brings about a strong polarization of the electronic configuration of the diene system that is conformed by two opposite dipolar halves. The polarized electronic configuration accounts for the extreme persistence manifested by the cyclopentadiene. The compound owns a vivid lemon-hued yellow color consequent to an unusually intense n ®p*absorption of a cyano group in the extensively conjugated compound. This is built up by consecutive one-pot reaction of two molecules of malononitrile carbanion and the ketonic substrate followed by a new tandem carbon-carbon cyclization with final elimination of cyanate ion.


2021 ◽  
Vol 34 (1) ◽  
pp. 1-8
Author(s):  
Nidhi Dhama ◽  
Sucheta ◽  
Aadesh Kumar ◽  
Vikrant Verma ◽  
Sunil Kumar

Piracetam is generally utilized as a nootropic drug, which is normally used in the treatment of CNS disorders. Piracetam is a cyclic compound and a derivative of γ-aminobutyric acid and improves learning, memory, brain metabolism, and ability. This drug belongs to the racetams group with the chemical name 2-oxo-1-pyrrolidine acetamide. The emphasis of this review article is to highlight different biological activities associated with piracetam and also some of its synthetic methodologies. Promising effects have been achieved in the management and treatment of several diseases for example alcoholism, Raynaud’s phenomenon, deep vein thrombosis and brain injury.


2020 ◽  
Vol 17 (5) ◽  
pp. 631-646
Author(s):  
Ravi D. Sharma ◽  
Jainendra Jain ◽  
Ratan L. Khosa

Background: In spite of current progress in treatment methods, cancer is a major source of morbidity and death rate all over the world. Traditional chemotherapeutic agents aim to divide cancerous cells, are often associated with deleterious side effects to healthy cells and tissues. Host defense peptides Cecropin A and B obtained from insects are capable to lyses various types of human cancer cells at peptide concentrations which are not fatal to normal eukaryotic cells. Methods: In the present work we have designed short chain α-helical linear and cyclic peptide from cecropin A having same cationic charge, hydrophobicity and helicity. Synthesis of designed novel short chain linear (10) and cyclic compound (12) was accomplished by using solution phase method. All the coupling reactions were carried out by using dicyclohexylcarbodiimide (DCC) as the coupling reagent at room temperature in the presence of N-methylmorpholine (NMM) as the base. The Structure of newly synthesized peptidse were elucidated by 1H-NMR, 13C-NMR, FT-IR, FABMS and elemental analysis data.Cytotoxicity of synthesized compound was tested against Dalton’s Lymphoma Ascites (DLA), Ehrlich’s Ascites Carcinoma (EAC) and MCF-7 cell lines by using MTT assay and 5-FU as reference compound. Results: From biological assessment,it was found that short chain cyclicpeptide12 showed high level of cytotoxic activity against DLA and EAC cell lines. Conclusion: By utilizing a structure-based rational approach to anticancer peptide design from cecropin A, we were able to develop short chain linear and cyclic peptides having same charge, hydrophobicity and with improved activity. Systematically removing amino acids, we were able to retaining peptide charge and hydrophobicity/hydrophilicity in linear and cyclic peptide which results to optimize the anticancer activity against DLA and EAC cell lines.


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