Bioorganic Chemistry
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#1Salman A. KhanH-Index: 17
#2Qasim UllahH-Index: 2
Last. Humaira ParveenH-Index: 7
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A donor-π-acceptor (D-π-A) chromophore, 2-amino-4-(9-ethyl-9H-carbazol-3-yl)-8-methoxy-5,6-dihydrobenzo[h]quinoline-3-carbonitrile (AEDQ) was synthesized from the condensation of 6-methoxy-3,4-dihydronaphthalen-1(2H)-one, 9-ethyl-9H-carbazole-3-carbaldehyde, malononitrile and NH4OAc in ethanol. Spectroscopic techniques and elemental analysis were employed to establish the structure of AEDQ. Photophysical parameters and fluorescence quantum yield were calculated in the different polarity solvents...
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Abstract A novel series of enantiopure naphthalimide-cycloalkanediamine conjugates were designed, synthetized and evaluated for in vitro cytotoxicity against human colon adenocarcinoma (LoVo), human lung adenocarcinoma (A549), human cervical carcinoma (Hela) and human promyelocytic leukemia cell lines (HL-60). The cytotoxicity of the compounds was highly dependent on size and relative stereochemistry of the cycloalkyl ring as well as length of the spacer. By contrast, any kind of enantioselectio...
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#1Shuai Wang (Haida: Hainan University)H-Index: 2
#2Jie Ren (Xida: Guangxi University)
Last. Sulan Luo (Haida: Hainan University)H-Index: 15
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Abstract Head-to-tail cyclization is an effective strategy to improve the biological stability of peptides. The α-conotoxin [S9A]TxID is a peptide that inhibits α3β4 nAChR with high activity and selectivity. Herein, we established a method for cyclizing and oxidative folding of [S9A]TxID, and six cyclic analogues of [S9A]TxID were chemically synthesized with various linker lengths. We used the electrophysiology assay to measure activity values of these cyclic analogues, and obtained the most pot...
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#1Tuğba Gürses (Gazi University)
#2Abdurrahman Olgaç (Gazi University)H-Index: 7
Last. Erden Banoglu (Gazi University)H-Index: 20
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Abstract Microsomal prostaglandin E2 synthase-1 (mPGES-1), 5-lipoxygenase (5-LO) and 5- lipoxygenase-activating protein (FLAP) are key for biosynthesis of proinflammatory lipid mediators and pharmacologically relevant drug targets. In the present study, we made an attempt to explore the role of small heteroaromatic fragments on the 4,5-diarylisoxazol-3-carboxylic acid scaffold, which are selected to interact with focused regions in the active sites of mPGES-1, 5-LO and FLAP. We report that the s...
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#1Alessandro PalmioliH-Index: 14
#2Paola SperandeoH-Index: 18
Last. Cristina AiroldiH-Index: 26
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Abstract We describe the development of an on-cell NMR method for the rapid screening of FimH ligands and the structural identification of ligand binding epitopes. FimH is a mannose-binding bacterial adhesin expressed at the apical end of type 1 pili of uropathogenic bacterial strains and responsible for their d -mannose sensitive adhesion to host mammalian epithelial cells. Because of these properties, FimH is a key virulence factor and an attractive therapeutic target for urinary tract infecti...
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#1Heba A. Hofny (Sohag University)
#2Mamdouh F.A. Mohamed (Sohag University)H-Index: 9
Last. Ahmed S. Aboraia (Assiut University)H-Index: 9
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Abstract DNA gyrase and topoisomerase IV (topo IV) inhibitors are among the most interesting antibacterial drug classes without antibacterial pipeline representative. Twenty-four new quinoline-1,3,4-oxadiazole and quinoline-1,2,4-triazole hybrids were developed and tested against DNA gyrase and topoisomerase IV from Escherichia coli and Staphylococcus aureus. The most potent compounds 4c, 4e, 4f, and 5e displayed an IC50 of 34, 26, 32, and 90 nM against E. coli DNA gyrase, respectively (novobioc...
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#1Manar G. Salem (Suez Canal University)H-Index: 2
#2Yasmine M. Abdel Aziz (Suez Canal University)H-Index: 6
Last. Mohamed Said (Suez Canal University)H-Index: 16
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Abstract In the present study, a novel generation of selective aldose reductase ALR2 inhibitors with significant hypoglycemic activities was designed and modulated based on rhodanine scaffold joined to an acetamide linker in between two lipophilic moieties. The synthesis of the novel compounds was accomplished throughout simple chemical pathways. Molecular docking was performed on B-cell membrane protein SUR1, aldehyde reductase ALR1 and aldose reductase ALR2 active sites. Compounds 10B, 11B, 12...
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#1Neelam Kumari (BBAU: Babasaheb Bhimrao Ambedkar University)
#2Ankur KaulH-Index: 12
Last. Anjani K. Tiwari (BBAU: Babasaheb Bhimrao Ambedkar University)H-Index: 14
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Abstract Quantitative changes in expression level of 5HT1A are somewhere related to common neurological disorders such as anxiety, major depression and schizophrenia. We have designed EDTA conjugated SPECT imaging probe for localization of 5HT1A receptor in brain. For designing SPECT probe we have employed the concept of bivalent approach and a homodimeric system with desirable pharmacokinetics of 5HT1A imaging. 99mTc-EDHT was also evaluated for its stability through serum stability assay and gl...
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#1Shantanu Sen (IITK: Indian Institute of Technology Kanpur)
#2Prerana Singh (IITK: Indian Institute of Technology Kanpur)H-Index: 3
Last. Sandeep Verma (IITK: Indian Institute of Technology Kanpur)H-Index: 51
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Abstract Insulin, a peptide hormone and a key regulator of blood glucose level, is routinely administered to type-I diabetic patients to achieve the required glycemic control. Insulin aggregation and ensuing amyloidosis has been observed at repeated insulin injection sites and in injectable formulations. The latter occurs due to insulin agglomeration during shipping and storage. Such insulin amyloid leads to enhanced immunogenicity and allow potential attachment to cell membranes leading to cell...
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#1Saman SargaziH-Index: 4
#2Sheida ShahrakiH-Index: 1
Last. Ramin SaravaniH-Index: 11
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Abstract Due to their unique pharmacological characteristics, methylxanthines are known as therapeutic agents in a fascinating range of medicinal scopes. In this report, we aimed to examine some biological effects of previously synthesized 8-alkylmercaptocaffeine derivatives. Cytotoxic and antioxidative activity of 8-alkylmercaptocaffeine derivatives were measured in malignant A549, MCF7, and C152 cell lines. Assessment of cGMP levels and caspase-3 activity were carried out using a colorimetric ...
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