Article
Chemistry, Multidisciplinary
Sajedeh Safapoor, Mohammad Halimi, Minoo Khalili Ghomi, Milad Noori, Navid Dastyafteh, Shahrzad Javanshir, Samanesadat Hosseini, Somayeh Mojtabavi, Mohammad Ali Faramarzi, Ensieh Nasli-Esfahani, Bagher Larijani, Azadeh Fakhrioliaei, Mohammad G. Dekamin, Maryam Mohammadi-Khanaposhtani, Mohammad Mahdavi
Summary: A new series of quinoline-quinazolinone-thioacetamide derivatives 9a-p were designed and synthesized. These compounds showed significant anti-a-glucosidase activity, with compound 9g being the most potent inhibitor. Molecular simulation studies revealed that compound 9g occupied the active site of a-glucosidase with favorable binding energy. In silico ADMET studies of the most potent compounds predicted their drug-likeness, pharmacokinetic, and toxicity properties.
Article
Biochemistry & Molecular Biology
Faryal Chaudhry, Wardah Shahid, Mariya Al-Rashida, Muhammad Ashraf, Munawar Ali Munawar, Misbahul Ain Khan
Summary: Developing improved enzyme inhibitors is an effective therapy for various diseases. A new series of bis-diazoles conjugated with an aryl linker were found to be effective against alpha-glucosidase and moderately active against LOX enzyme. The inhibitory potentials of these compounds were influenced by factors such as lipophilicity, bulkiness, and specific interactions with enzyme active pockets.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Nabeela Kausar, Saeed Ullah, Maria Aqeel Khan, Humaira Zafar, Atia-tul-Wahab, M. Iqbal Choudhary, Sammer Yousuf
Summary: Celebrex, commonly used as an anti-inflammatory drug, was functionalized to identify new alpha-glucosidase inhibitors. Many synthesized derivatives showed potent alpha-glucosidase inhibitory activity in vitro, with compound 9 being the most effective inhibitor. Molecular docking studies revealed interactions of compounds 6 and 9 with key amino acid residues of alpha-glucosidase.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Xin Zhao, Jia-Yi Shou, Josiah J. Newton, Feng-Ling Qing
Summary: A silver-promoted selective synthesis of trans-CF3SF4Cl under safe gas-reagent-free conditions is described, and its synthetic application in α-diazo carbonyl compounds is demonstrated.
Article
Chemistry, Organic
Mingshuai Zhang, Longkun Chen, Haifeng Sun, Zhuoyuan Liu, Sheng-Jiao Yan, Fuchao Yu
Summary: A novel Rh(III)-catalyzed cascade reaction involving alkenyl C-H activation, [3 + 2] annulation, and pinacol rearrangement has been developed. This method provides a new and straightforward synthetic strategy for the synthesis of highly functionalized 2-spirocyclo-pyrrol-3-ones.
Article
Chemistry, Applied
Jichen Yang, Xiaoli Wang, Chuanying Zhang, Lun Ma, Tao Wei, Yajing Zhao, Xin Peng
Summary: Flavonoid compounds have anti-diabetic activity by controlling blood glucose levels through inhibiting the activity of alpha-glucosidase. The study showed that these compounds had higher inhibitory activities compared to acarbose, with scutellarein potentially serving as the most effective inhibitor. Additionally, the synergistic effects of flavonoid compounds combined with acarbose on alpha-glucosidase activity were observed.
Review
Chemistry, Multidisciplinary
Cai Zhang, Jie-Ping Wan
Summary: Diazomethyl-substituted iodine(III) compounds with electron-withdrawing groups have potential reaction abilities and can be used as key intermediates in organic synthesis.
CHEMISTRY-A EUROPEAN JOURNAL
(2023)
Article
Chemistry, Multidisciplinary
Bao-Gui Cai, Ye-Peng Bao, Chao Pei, Qian Li, Lei Li, Rene M. Koenigs, Jun Xuan
Summary: This paper reports on the photochemical reaction of diazoalkanes with azodicarboxylates, wherein a triplet species formed upon photoexcitation reacts with diazoalkanes to generate an azomethine ylide, followed by dipolar cycloaddition reaction with organic nitriles to form 1,2,4-triazoles. The reaction exhibits broad substrate scope and can be scaled up via flow chemistry and downstream transformations.
Article
Chemistry, Multidisciplinary
Nicholas J. Porter, Emma Danelius, Tamir Gonen, Frances H. Arnold
Summary: This study developed a catalyst that uses diazirines as carbene precursors, providing a new strategy for selective carbene transfer. By engineering variants of ApePgb protoglobin, selective carbene transfer from diazirines can be achieved at room temperature. The structure of an ApePgb variant, determined by microcrystal electron diffraction, revealed how evolution has enhanced access to the heme active site for this new-to-nature catalysis.
JOURNAL OF THE AMERICAN CHEMICAL SOCIETY
(2022)
Article
Chemistry, Applied
Mandeep Kaur, Raj Kaushal
Summary: The synthesized vanadyl chalcone complexes showed moderate to significant inhibition activity against antidiabetic enzymes and demonstrated remarkable antioxidant activity. This suggests promising potential for both antidiabetic and antioxidant applications.
APPLIED ORGANOMETALLIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Loghman Alaei, Zhila Izadi, Samira Jafari, Fatemeh Jahanshahi, Mehdi Jaymand, Pantea Mohammadi, Bilal Ahamad Paray, Anwarul Hasan, Mojtaba Falahati, Behrang Shiri Varnamkhasti, Ali Akbar Saboury, Zahra Moosavi-Nejad, Mehrnaz Sheikh-Hosseini, Hossein Derakhshankhah
Summary: In this study, the structure-activity relationship and kinetics of thermal inactivation of alpha-glucosidase A (AglA) were investigated using p-nitrophenyl alpha-D-glucopyranoside as the synthetic substrate in a potassium phosphate buffer at pH 6.8. The Arrhenius plot showed a biphasic appearance in the thermal inactivation rate constant before and after 45 degrees C, indicating the involvement of contact areas and active centers in the enzyme inactivation process.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2021)
Article
Chemistry, Organic
Mitsuru Kitamura, Takashi Eto, Kazushige Konai, Shuhei Takahashi, Hirokazu Shimooka, Tatsuo Okauchi
Summary: This study describes the first efficient diazo-transfer reaction of phenols. By using a safe and stable crystalline catalyst, high yields of diazoquinones can be obtained from phenols. The reaction proceeds efficiently in methanol solution, demonstrating excellent reactivity.
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2022)
Review
Chemistry, Applied
Daksh Singh Davas, Srashti Bhardwaj, Raju Sen, Dinesh Kumar Gopalakrishnan, Janakiram Vaitla
Summary: This review surveys the coupling of two carbene precursors for the synthesis of alkenes. The key factor for selective carbene coupling is the difference in carbene generation rate between the two precursors. This strategy requires careful selection of precursors and fine-tuning of reaction conditions to achieve the desired chemo- and stereoselectivity. The review covers inter- and intramolecular coupling of diazo compounds as well as cross-coupling between diazo and non-diazo compounds.
ADVANCED SYNTHESIS & CATALYSIS
(2022)
Article
Nutrition & Dietetics
Hua Zhou, Jin Liao, Juanying Ou, Jiayu Lin, Jie Zheng, Yifei Li, Shiyi Ou, Fu Liu
Summary: The ethanolic extract of Fenghuang Dancong tea showed potential alpha-glucosidase inhibitory activity. The most bioactive fraction was further purified to yield three novel compounds, with compound 1 exhibiting the strongest inhibitory activity.
FRONTIERS IN NUTRITION
(2022)
Article
Chemistry, Applied
Wei Zhang, He-Ying Wang, Huai-Xu Wang, Zhen-Yuan Zhu
Summary: The synthesis of methyl glycyrrhetinate glycosides and their inhibition of alpha-glucosidase were examined in this study. It was found that the compounds showed significant inhibitory activity against alpha-glucosidase, with Compound 1 exhibiting the most potent inhibition.
NATURAL PRODUCT RESEARCH
(2021)
Article
Chemistry, Multidisciplinary
Yogesh Jaiswal, Yogesh Kumar, Jagannath Pal, Ranga Subramanian, Amit Kumar
CHEMICAL COMMUNICATIONS
(2018)
Article
Chemistry, Organic
Yogesh Kumar, Yogesh Jaiswal, Amit Kumar
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
(2018)
Article
Chemistry, Organic
Yogesh Kumar, Yogesh Jaiswal, Amit Kumar
Article
Chemistry, Organic
Mukta Shaw, Rima Thakur, Amit Kumar
JOURNAL OF ORGANIC CHEMISTRY
(2019)
Article
Chemistry, Organic
Mukta Shaw, Amit Kumar
Article
Chemistry, Multidisciplinary
Mukta Shaw, Amit Kumar
CHEMISTRY-AN ASIAN JOURNAL
(2019)
Article
Chemistry, Physical
Yogesh Jaiswal, Amit Kumar
CATALYSIS COMMUNICATIONS
(2019)
Article
Chemistry, Physical
Muhammad Nadeem Arshad, Hassan M. Faidallah, Abdullah M. Asiri, Naveen Kosar, Tariq Mahmood
JOURNAL OF MOLECULAR STRUCTURE
(2020)
Article
Chemistry, Organic
Yogesh Jaiswal, Saptarshi Mandal, Prolay Das, Amit Kumar
Article
Chemistry, Organic
Akanksha Singh Baghel, Yogesh Jaiswal, Amit Kumar
Article
Chemistry, Organic
Hassan M. Faidallah, Tariq R. Sobahi, Abdulrahman S. Alharbi, Khaled M. El-Avia
Summary: This study reports the synthesis and characterization of new bicyclic and tricyclic heterocyclic macromolecules starting from new dienones. The cytotoxicity of some of the synthesized derivatives was also investigated.
POLYCYCLIC AROMATIC COMPOUNDS
(2022)
Article
Multidisciplinary Sciences
Abdulrashid Umar, Hassan M. Faidallah, Qamar Uddin Ahmed, Khalid A. Alamry, Sayeed Mukhtar, Meshari A. Alsharif, Syed Najmul Hejaz Azmi, Humaira Parveen, Zainul Amiruddin Zakaria, Mostafa A. Hussien
Summary: This study describes the design and synthesis of a series of novel benzoquinoline analogues and evaluates their antiproliferative activity against colon, breast, and hepatocellular cancers. One compound (CNMP, 2) exhibited the most potent anticancer effect and molecular docking studies confirmed its binding affinity. The results suggest that CNMP may serve as a potential lead structure for the development of more effective anticancer candidates.
JOURNAL OF KING SAUD UNIVERSITY SCIENCE
(2022)
Review
Chemistry, Organic
Rima Thakur, Yogesh Jaiswal, Amit Kumar
ORGANIC & BIOMOLECULAR CHEMISTRY
(2019)
Article
Chemistry, Organic
Yogesh Jaiswal, Yogesh Kumar, Amit Kumar
ORGANIC & BIOMOLECULAR CHEMISTRY
(2019)
Article
Crystallography
Abdullah M. Asiri, Khalid A. H. Alzahrani, Hassan M. Faidallah, Khalid A. Alamry, Mukesh M. Jotani, Edward R. T. Tiekink
ACTA CRYSTALLOGRAPHICA SECTION E-CRYSTALLOGRAPHIC COMMUNICATIONS
(2019)