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Bioorganic Chemistry

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https://www.readbyqxmd.com/read/28346874/protective-effects-of-hepatocyte-specific-glycyrrhetic-derivatives-against-carbon-tetrachloride-induced-liver-damage-in-mice
#1
Yifei Yang, Lingyun Yang, Yaodan Han, Zhenwei Wu, Pan Chen, Huibin Zhang, Jinpei Zhou
Glycyrrhetic acid (GA), the main hydrolysate of glycyrrhizic acid extracted from the roots of the Chinese herb Glycyrrhiza glabra, was reported to be accumulated in hepatocytes due to the extensive distribution of GA receptors in liver. A series of hepatocyte-specific derivatives on the basis of anetholtrithione and glycyrrhizic were designed and synthesized. The potential beneficial effect was evaluated in carbon tetrachloride (CCl4)-induced liver injury model. In addition, the hepatoprotective activity of these derivatives was assessed by measuring levels of serum marker enzymes, including serum glutamate oxaloacetate transaminase (GOT), serum glutamate pyruvate transaminase (GPT), alkaline phosphatase (AKP), lactate dehydrogenase (LDH) and the ratio of GSH to GSSG...
March 20, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28346872/5-bromo-2-aryl-benzimidazole-derivatives-as-non-cytotoxic-potential-dual-inhibitors-of-%C3%AE-glucosidase-and-urease-enzymes
#2
Tanzila Arshad, Khalid Mohammed Khan, Najma Rasool, Uzma Salar, Shafqat Hussain, Humna Asghar, Mohammed Ashraf, Abdul Wadood, Muhammad Riaz, Shahnaz Perveen, Muhammad Taha, Nor Hadiani Ismail
On the basis of previous report on promising α-glucosidase inhibitory activity of 5-bromo-2-aryl benzimidazole derivatives, these derivatives were further screened for urease inhibitory and cytotoxicity activity in order to get more potent and non-cytotoxic potential dual inhibitor for the patients suffering from diabetes as well as peptic ulcer. In this study, all compounds showed varying degree of potency in the range of (IC50=8.15±0.03-354.67±0.19μM) as compared to standard thiourea (IC50=21.25±0.15μM)...
March 20, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28346873/design-synthesis-docking-studies-and-biological-evaluation-of-novel-chalcone-derivatives-as-potential-histone-deacetylase-inhibitors
#3
Mamdouh F A Mohamed, Montaser Sh A Shaykoon, Mostafa H Abdelrahman, Bakheet E M Elsadek, Ahmed S Aboraia, Gamal El-Din A A Abuo-Rahma
A group of novel chalcone derivatives comprising hydroxamic acid or 2-aminobenzamide group as zinc binding groups (ZBG) were synthesized. The structure of the prepared compounds was fully characterized by IR, NMR and elemental microanalyses. Most of the tested compounds displayed strong to moderate HDAC inhibitory activity. Some of these compounds showed potent anti-proliferative activity against human HepG2, MCF-7 and HCT-116 cell lines. In particular, compounds 4a and 4b exhibited significant anti-proliferative activity against the three cell lines compared to SAHA as reference drug and displayed promising profile as anti-tumor candidates...
March 19, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28346871/synthesis-in-vitro-evaluation-and-molecular-docking-studies-of-novel-amide-linked-triazolyl-glycoconjugates-as-new-inhibitors-of-%C3%AE-glucosidase
#4
Shyam Ji Gupta, Samrat Dutta, Rahul L Gajbhiye, Parasuraman Jaisankar, Asish Kumar Sen
A series of N-substituted amide linked triazolyl β-d-glucopyranoside derivatives (4a-l) were synthesized and their in vitro inhibitory activity against yeast α-glucosidase enzyme [EC.3.2.1.20] was assessed. Compounds 4e (IC50=156.06μM), 4f (IC50=147.94μM), 4k (IC50=127.71μM) and 4l (IC50=121.33μM) were identified as the most potent inhibitors for α-glucosidase as compared to acarbose (IC50=130.98μM) under the same in vitro experimental conditions. Kinetic study showed that both 4e and 4f inhibit the enzyme in a competitive manner with p-nitrophenyl α-d-glucopyranoside as substrate...
March 18, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28340404/synthesis-in-vitro-antiproliferative-activity-and-kinase-profile-of-new-benzimidazole-and-benzotriazole-derivatives
#5
Konrad Chojnacki, Patrycja Wińska, Katarzyna Skierka, Monika Wielechowska, Maria Bretner
Protein kinase 2 (CK2), a member of the serine/threonine kinase family, has been established as a promising target in anticancer therapy. New derivatives of known CK2 inhibitors 4,5,6,7-tetrabromo-1H-benzimidazole (TBBi) and 4,5,6,7-tetrabromo-1H-benzotriazole (TBBt) bearing azide or substituted triazole groups were synthesized. Their influence on the activity of human recombinant CK2α and cytotoxicity against normal and cancer cell lines were evaluated. TBBi derivatives with triazole substituted with carboxyl substituent (7 and 10) exhibited the most potent inhibitory activity against CK2 with Ki value in the range of 1...
March 16, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28302310/design-synthesis-and-anti-diabetic-activity-of-triazolotriazine-derivatives-as-dipeptidyl-peptidase-4-dpp-4-inhibitors
#6
Bhumika D Patel, Shraddha V Bhadada, Manjunath D Ghate
Type 2 diabetes mellitus (T2DM) is one of the major global metabolic disorders characterized by insulin resistance and chronic hyperglycemia. Inhibition of the enzyme, dipeptidyl peptidase-4 (DPP-4) has been proved as successful and safe therapy for the treatment of T2DM since last decade. In order to design novel DPP-4 inhibitors, various in silico studies such as 3D-QSAR, pharmacophore modeling and virtual screening were performed and on the basis of the combined results of them, total 50 triazolo[5,1-c][1,2,4]triazine derivatives were designed and mapped on the best pharmacophore model...
March 6, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28285876/one-pot-synthesis-of-a-new-2-substituted-1-2-3-triazole-1-oxide-derivative-from-dipyridyl-ketone-and-isonitrosoacetophenone-hydrazone-nickel-ii-complex-dna-binding-and-cleavage-properties
#7
Ramazan Gup, Oktay Erer, Nefise Dilek
An efficient and simple one-pot synthesis of a new 1,2,3-triazole-1-oxide via reaction between isonitrosoacetophenone hydrazone and dipyridyl ketone in the EtOH/AcOH at room temperature has been developed smoothly in high yield. The reaction proceeds via metal salt free, in-situ formation of asymmetric azine followed by cyclization to provide 1,2,3-triazole 1-oxide compound. It has been structurally characterized. The 1:1 ratio reaction of the 1,2,3-triazole 1-oxide ligand with nickel(II) chloride gives the mononuclear complex [Ni(L)(DMF)Cl2], hexa-coordinated within an octahedral geometry...
March 3, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28285874/selective-fluorescence-sensing-and-quantification-of-uric-acid-by-naphthyridine-based-receptor-in-biological-sample
#8
Prithidipa Sahoo, Sujoy Das, Himadri Sekhar Sarkar, Kalipada Maiti, Md Raihan Uddin, Sukhendu Mandal
Naphthyridine-based fluorescent probe H1 was synthesized and characterized for the quantification and selective detection of Uric Acid (UA) in live cell. In presence of UA, H1 forms the specific host-guest complex mainly through intermolecular hydrogen bonding and aromatic stacking which produces "turn-off" fluorescence. The probe and UA is found to be 1:1 stoichiometry on the basis of absorption and fluorescence titrations. The probe H1 has been shown to detect UA up to 0.6µM at pH 7.4. DFT-TDDFT calculations were performed in order to demonstrate the sensing mechanism and the electronic properties of the receptor-donor complex...
March 3, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28302311/the-first-synthesis-of-4-phenylbutenone-derivative-bromophenols-including-natural-products-and-their-inhibition-profiles-for-carbonic-anhydrase-acetylcholinesterase-and-butyrylcholinesterase-enzymes
#9
Çetin Bayrak, Parham Taslimi, İlhami Gülçin, Abdullah Menzek
The first synthesis of (E)-4-(3-bromo-4,5-dihydroxyphenyl)but-3-en-2-one (1), (E)-4-(2-bromo-4,5-dihydroxyphenyl)but-3-en-2-one (2), and (E)-4-(2,3-dibromo-4,5-dihydroxyphenyl)but-3-en-2-one (3) was realized as natural bromophenols. Derivatives with mono OMe of 2 and 3 were obtained from the reactions of their derivatives with di OMe with AlCl3. These novel 4-phenylbutenone derivatives were effective inhibitors of the cytosolic carbonic anhydrase I and II isoenzymes (hCA I and II), acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) with Ki values in the range of 158...
March 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28285875/thermodynamic-structural-and-fluorescent-characteristics-of-dna-hairpins-containing-functionalized-pyrrolo-2-deoxycytidines
#10
Zofia Jahnz-Wechmann, Jolanta Lisowiec-Wachnicka, Grzegorz Framski, Joanna Kosman, Jerzy Boryski, Anna Pasternak
Herein, we present comprehensive physicochemical and structural analysis of various DNA hairpins modified with pyrrolo-2'-deoxycytidine (Py-dC) derivatives. The introduction of modified Py-dC in most cases causes minor decrease of hairpin thermodynamic stability. The energetically unfavorable effect is more pronounced when modified residue is present within hairpin loop. Our studies indicate that thermodynamic effects induced by all Py-dC derivatives are net results of increased stacking interactions caused by larger surface of pyrrolo-2'-deoxycytidine aromatic ring and unfavorable effect implied by the presence of additional side chains...
March 2, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28267984/pyridoxine-resveratrol-hybrids-mannich-base-derivatives-as-novel-dual-inhibitors-of-ache-and-mao-b-with-antioxidant-and-metal-chelating-properties-for-the-treatment-of-alzheimer-s-disease
#11
Xia Yang, Xiaoming Qiang, Yan Li, Li Luo, Rui Xu, Yunxiaozhu Zheng, Zhongcheng Cao, Zhenghuai Tan, Yong Deng
A series of pyridoxine-resveratrol hybrids Mannich base derivatives as multifunctional agents have been designed, synthesized and evaluated for cholinesterase (ChE) and monoamine oxidase (MAO) inhibitory activity. To further explore the multifunctional properties of the new derivatives, their antioxidant activities and metal-chelating properties were also tested. The results showed that most of these compounds could selectively inhibit acetylcholinesterase (AChE) and MAO-B. Among them, compounds 7d and 8b exhibited the highest potency for AChE inhibition with IC50 values of 2...
February 28, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28267983/synthesis-molecular-modeling-studies-and-anticonvulsant-activity-of-certain-1-benzyl-aryl-amino-cyclohexyl-methyl-esters
#12
Walaa Hamada Abd-Allah, Mona Elsayed Aboutabl, Mohamed Nabil Aboul-Enein, Aida Abdel Sattar El-Azzouny
A series of (1-(benzyl (aryl) amino) cyclohexyl) methyl esters 7a-n were prepared and screened for their anticonvulsant profile. Screening of these esters 7a-n and their starting alcohols 6a and 6b revealed that compound 7k was the most potent one in the scPTZ screening test with an ED50 value of 0.0056mmol/kg being about 10- and 164-fold more potent than phenobarbital (ED50=0.056mmol/kg) and ethosuximide (ED50=0.92mmol/kg) as reference drugs, respectively. Meanwhile, in the MES test, compounds 7b and 7k at doses 0...
February 27, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28267982/synthesis-of-2-morpholinetetraphenylporphyrins-and-their-photodynamic-activities
#13
Ping-Yong Liao, Xin-Rong Wang, Xiang-Hua Zhang, Tai-Shan Hu, Mei-Zhen Zheng, Ying-Hua Gao, Yi-Jia Yan, Zhi-Long Chen
A series of 2-morpholinetetraphenylporphyrins functionalized with various substituents (Cl, Me, MeO group) at 4-phenyl position were prepared via nucleophilic substitution of 2-nitroporphyrin copper derivatives with morpholine by refluxing under a nitrogen atmosphere and then demetalization. Their basic photophysical properties, intracellular localization, cytotoxicities in vitro and in vivo were also investigated. All synthesized photosensitizers exhibited longer maxima absorption wavelengths than Hematoporphyrin monomethyl ether (HMME)...
February 27, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28274582/estrogen-receptor-agonists-antagonists-in-breast-cancer-therapy-a-critical-review
#14
REVIEW
A Jameera Begam, S Jubie, M J Nanjan
Estrogens display intriguing tissue selective action that is of great biomedical importance in the development of optimal therapeutics for the prevention and treatment of breast cancer. There are also strong evidences to show that both endogenous and exogenous estrogens are involved in the pathogenesis of breast cancer. Tamoxifen has been the only drug of choice for more than 30years to treat patients with estrogen related (ER) positive breast tumors. There is a need therefore, for identifying newer, potential and novel candidates for breast cancer...
February 23, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28267985/in-vitro-modulatory-effects-of-functionalized-pyrimidines-and-piperidine-derivatives-on-aryl-hydrocarbon-receptor-ahr-and-glucocorticoid-receptor-gr-activities
#15
Muhammad Yar, Lubna Shahzadi, Ariba Farooq, Saima Jalil Imran, José P Cerón-Carrasco, Helena den-Haan, Sanjay Kumar, Jorge Peña-García, Horacio Pérez-Sánchez, Aneta Grycova, Zdenek Dvorak, Radim Vrzal
The development of biologically active molecules based on molecular recognition is an attractive and challenging task in medicinal chemistry and the molecules that can activate/deactivate certain receptors are of great medical interest. In this contribution, selected pyrimidine/piperidine derivatives were synthesized and tested for the ability to activate/deactivate Aryl hydrocarbon receptor (AhR) and Glucocorticoid receptor (GR). Tested compounds are shown to activate the receptors but to much lesser extent than positive controls, dioxin and dexamethasone for Ahr and GR, respectively...
February 21, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28245905/synthesis-of-readily-available-fluorophenylalanine-derivatives-and-investigation-of-their-biological-activity
#16
Martin Krátký, Šárka Štěpánková, Katarína Vorčáková, Lucie Navrátilová, František Trejtnar, Jiřina Stolaříková, Jarmila Vinšová
A series of thirty novel N-acetylated fluorophenylalanine-based aromatic amides and esters was synthesized using N-(3-dimethylaminopropyl)-N'-ethylcarbodiimide or phosphorus trichloride in pyridine. They were characterized by spectral methods and screened against various microbes (Mycobacterium tuberculosis, non-tuberculous mycobacteria, other bacteria, fungi), for their inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) and cytotoxicity. All amino acids derivatives revealed a moderate inhibition of both cholinesterases with IC50 values for AChE and BChE of 57...
February 21, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28242062/synthesis-and-topoisomerase-i-inhibitory-properties-of-klavuzon-derivatives
#17
İsmail Akçok, Derya Mete, Ayhan Şen, Pınar Kasaplar, Kemal S Korkmaz, Ali Çağır
Klavuzon is a naphthalen-1-yl substituted α,β-unsaturated δ-lactone derivative, and is one of the anti-proliferative members of this class of compounds. Asymmetric and racemic syntheses of novel α,β-unsaturated δ-lactone derivatives are important to investigate their potential for the treatment of cancer. In this study, asymmetric and racemic syntheses of heteroatom-substituted klavuzon derivatives are reported. The syntheses were completed by a well-known three-step procedure. Anti-proliferative activity of seven novel racemic klavuzon derivatives were reported against MCF-7, PC3, HCT116 p53+/+ and HCT116 p53-/- cancer cell lines...
February 21, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28228228/molecular-hybridization-conceded-exceptionally-potent-quinolinyl-oxadiazole-hybrids-through-phenyl-linked-thiosemicarbazide-antileishmanial-scaffolds-in-silico-validation-and-sar-studies
#18
Muhammad Taha, Nor Hadiani Ismail, Muhammad Ali, Umer Rashid, Syahrul Imran, Nizam Uddin, Khalid Mohammed Khan
The high potential of quinoline containing natural products and their derivatives in medicinal chemistry led us to discover a novel series of compounds 6-23 based on the concept of molecular hybridization. Most of the synthesized analogues exhibited potent leishmanicidal potential. The most potent compound (23, IC50=0.10±0.001μM) among the series was found ∼70 times more lethal than the standard drug. The current series 6-23 conceded in the development of fourteen (14) extraordinarily active compounds against leishmaniasis...
February 20, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28238402/design-synthesis-anticonvulsant-evaluation-and-docking-study-of-2-6-substituted-benzo-d-thiazol-2-ylcarbamoyl-methyl-1-4-substituted-phenyl-isothioureas
#19
Nadeem Siddiqui, Md Shamsher Alam, Meeta Sahu, Mohd Javed Naim, M Shahar Yar, Ozair Alam
In this paper, we report the synthesis of 2-[(6-substituted benzo[d]thiazol-2-ylcarbamoyl)methyl]-1-(4-substituted phenyl)isothiourea derivatives (4a-y) carrying active pharmacophores essential for anticonvulsant activity. The anticonvulsant activity was evaluated in vivo by maximal electroshock (MES) test and subcutaneous pentylenetetrazole (scPTZ) test in mice. Most of the compounds showed promising anticonvulsant activity. The most active compounds 4b and 4q were found active in both MES and scPTZ models, without signs of neurotoxicity...
February 17, 2017: Bioorganic Chemistry
https://www.readbyqxmd.com/read/28228229/oxidative-transformation-of-a-tunichrome-model-compound-provides-new-insight-into-the-crosslinking-and-defense-reaction-of-tunichromes
#20
Adal Abebe, Qun F Kuang, Jason Evans, William E Robinson, Manickam Sugumaran
Tunichromes, small oligopeptides with dehydrodopa units isolated from the blood cells of ascidians, have been implicated in the defense reactions, metal binding, wound repair, or tunic formation. Their instability and high reactivity has severely hampered the assessment of their biological role. Experiments conducted with the model compound, 1,2-dehydro-N-acetyldopamine, indicated that the instability of tunichromes is due to this basic structure. Exposure of this catecholamine derivative to even mild alkaline condition such as pH 7...
February 16, 2017: Bioorganic Chemistry
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