Poly(adenosine diphosphate-ribose) polymerase (PARP) is a group of enzymes with several subtypes and it manages various ailment such as cancer, inflammatory disorders, diabetes mellitus, neuronal injury, HIV infection, Parkinsonism, aging, and ischemia-reperfusion injury. Various PARP inhibitors share a common property of bicyclic lactam in its main structural frame. The core moiety containing bicyclic lactam rings are isoquinolinones, dihydroisoquinolinones, quinazolinediones, phthalazinones, quinazolinones, and phenanthridones. The quinazolinone with diverse substituents displayed low nanomolar inhibition. Quinazolinone is an important and vital molecule in the field of medicinal chemistry possessing multitude pharmacological actions. Though the chemistry of quinazolinones has been discussed through centuries, its concise role on PARP inhibition needed a special consideration. The aim of this review is to discover the effect of quinazolinone substitutents and its role in PARP inhibition. This precise review will discuss the effect of quinazolinones on PARP subtypes such as PARP-1, PARP-2, PARP-5a, and PARP-5b. In addition to its pharmacological actions, PARP inhibitors can also act as a chemosensitizing agent, and it is used in combination with the other anticancer agents. This summarization will definitely be a supportive report for the scientist working toward the novelty in the quinazolinone nucleus and its role in PARP inhibition.

Hemalatha S

Department of Software and Systems Engineering

School of Information Technology and Engineering

Vellore Campus

Madhumitha G

Department of Chemistry

School of Advanced Sciences

Vellore Institute of Technology (VIT) is a private university located in&nbsp;Tamil Nadu, India. Founded in 1984, as Vellore Engineering College, the institution offers 20 undergraduate, 34 postgraduate, four integrated and four research programs. It has campuses in Vellore, Amravati, Bhopal and Chennai.

VIT is one of the top ranked private universities in India according to NIRF, THE and QS Rankings.&nbsp;Govt. of India has recognized&nbsp;VIT, Vellore as an&nbsp;Institution of Eminence. This has allowed VIT to take independent quality initiatives and move up in world ranking.

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VIT University

Applied Microbiology and Biotechnology

Dihydroquinazolinones is an important core structure reported with a wide variety of pharmacological activities. They are capable of undergoing various transformations because of its reactivity towards various reagents. The synthetic strategies for the functionalization and derivatization of the nucleus were explained. The diversified pharmacological actions of this moiety were illustrated through various biochemical pathways. The structural-activity relationship study of dihydroquinazolinones anticipated the relationship between the various substituents and its role in the pharmacological action. The main objective of this review is to summarize the importance of dihydroquinazolinones in the field of chemical biology.

European Journal of Medicinal Chemistry

Synthetic strategy with representation on mechanistic pathway for the therapeutic applications of dihydroquinazolinones

A new series of brominated derivatives of 2, 3-dihydroquinazolin-4(1H)-one were synthesized and their structures were confirmed using IR, NMR and mass spectra. The synthesized derivatives were screened for their in vitro anthelmintic activity. The investigations on interaction of the bioactive compound, 2i with bovine serum albumin (BSA) were evaluated. The quenching mechanism of the compound, 2i was deduced based on the results of Stern–Volmer equation. The number of binding site, prediction of binding site region and the changes in the secondary structure of protein were predicted using various spectroscopic studies.

Journal of Luminescence

Study of binding interaction between anthelmintic 2, 3-dihydroquinazolin-4-ones with bovine serum albumin by spectroscopic methods

The main aim of this study is to investigate the interaction of 7-fluoro-2,2-dimethyl-2,3-dihydroquinazolin-4(1H)-one with lysozyme through various spectrophotometric studies. The graph such as Stern-Volmer plot, modified Stern Volmer plot, double logarithmic plot and Van't Hoff plot were plotted to determine the various parameters essential for predicting the interaction. The interaction of the ligand with the protein was further confirmed by circular dichroism and NMR study. The molecular docking was performed and the results obtained were correlated with the other studies. The importance of fluorine was justified through the prediction of pKa values and the possible metabolic pathway using the in silico tools. In addition, the cytotoxicity of the compound was carried out using HeLa cancer cell.

Journal of Photochemistry and Photobiology B: Biology

Importance of fluorine in 2,3-dihydroquinazolinone and its interaction study with lysozyme

Aspergillosis is one of the infectious fungal diseases affecting mainly the immunocompromised patients. The scarcity of the antifungal targets has identified the importance of N-myristoyl transferase (NMT) in the regulation of fungal pathway. The dihydroquinazolinone molecules were designed on the basis of fragments responsible for binding with the target enzyme. The aryl halide, 1(a-g), aryl boronic acid and potassium carbonate were heated together in water and dioxane mixture to yield new C-C bond formation in dihydroquinazolinone. The bis(triphenylphosphine)palladium(II) dichloride was used as catalyst for the C-C bond formation. The synthesized series were screened for their in vitro antifungal activity against Aspergillus Niger and Aspergillus fumigatus. The binding interactions of the active compound with lysozyme were explored using multiple spectroscopic studies. Molecular docking study of dihydroquinazolinones with the enzyme revealed the information regarding various binding forces involved in the interaction.

Binding mode of dihydroquinazolinones with lysozyme and its antifungal activity against Aspergillus species

Bottle gourd (Lagenaria siceraria) belongs to the family Cucurbitaceae, which comprises about 118 genera and 825 species. It is an important vegetable crop of India, and its production is influenced by a number of factors viz., environmental, nutritional, cultural operation and use of plant growth regulators. Since, bottle gourd belongs to a medicinal family, it plays a major role in the treatment of several diseases related to the skin and heart. There are several organic chemical compounds including vitamin B complex, pectin, dietary soluble fibres, ascorbic acid, beta-carotene, amino acids and minerals which have been isolated from this species. Therefore, the bottle gourd is considered to have a great impact on therapeutic health benefits. Due to drastic industrialization and urbanization, most of the human beings are facing several ill effects which may lead to death at extreme cases. Hence, the major research area was said to be nanotechnology. Taking into consideration, we have combined nanotechnology field with waste source in the name of green synthesis and planned to cure several diseases, as most of the researchers focused their work on this and succeeded too. The present study is a complete review of L. siceraria that covers the ethnomedical uses, chemical constituents, and pharmacological profile. This study is mainly focused on the antibacterial, hepatoprotective, diuretic and anthelminthic activities. © 2015, Springer-Verlag Berlin Heidelberg.

Biotechnology and pharmacological evaluation of Indian vegetable crop Lagenaria siceraria: an overview

The physicochemical methods of the synthesis of zinc nanoparticles (ZnO NPs) and some detailed studies on ZnO toxicity mechanism and biokinetics have been reported. However, some of these physical and chemical methods of synthesis are expensive and can also have toxic substances absorbed onto them. Hence, eco-friendly synthesis of nanoparticles due to their easier process, cheaper availability, and high stability is dominating new research. In particular, ZnO NPs which are now being synthesized through major biological systems involved in this are bacteria, fungi, and plant extracts; this has increased studies in various applications in the biological field. In this review, we have elaborated on various natural source-mediated syntheses of ZnO NPs and their role in various biological activities like antimicrobial, anticandidal, larvicidal, cytotoxic, and photocatalytic activities. Apart from these applications, ZnO NPs are also reported to help to prevent dust formation, for several years, on oil paintings. © 2015, Springer-Verlag Berlin Heidelberg.

Journal	Data powered by TypesetApplied Microbiology and Biotechnology
Publisher	Data powered by TypesetSpringer Science and Business Media LLC
ISSN	0175-7598
Open Access	0