Article
Chemistry, Physical
Houssem Boulebd, Yasmine Zine, Imene Amine Khodja, Arif Mermer, Adem Demir, Abdelmadjid Debache
Summary: Hydrazone and hydrazone-hydrazide-based compounds are important classes of compounds with diverse pharmacological actions. In this study, a series of new phenolic hydrazone/hydrazide derivatives were synthesized and evaluated for their antiradical activity, with hydrazones found to be more reactive than hydrazone-hydrazides. Compound 4 was identified as the best radical scavenger among the studied compounds.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Physical
Ozlem Aslanhan, Erbay Kalay, Feyzi Sinan Tokali, Zehra Can, Engin Sahin
Summary: Due to their significant biological activities, there is increasing popularity in the design and synthesis of hydrazone derivatives. In this study, twelve novel isonicotinic hydrazide-hydrazone analogues were synthesized and characterized. These compounds exhibited inhibitory effects against AChE enzyme and showed moderate antioxidant potential.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Physical
Seyedeh Mahdieh Hashemi, Saeed Emami, Patrick Honarchian Masihi, Aidin Shakiba, Leila Dehestani, Nematollah Ahangar
Summary: A series of novel 1-(2-(halophenyl)-2-(2-arylhydrazono)ethyl)-1H-1,2,4-triazoles 7a-l and their Fischer indolic products 2-(halophenyl)-3-(1H-1,2,4-triazol-1-yl)-1H-indoles 8a-l were synthesized conveniently. The (Z or E) geometry of arylhydrazones was identified by 1H NMR spectroscopy. The antiepileptic potential of both series of compounds was evaluated using PTZ and MES seizure models. The majority of hydrazones exhibited significant protective effects against MES-induced seizures, with compounds 7a and 7h being the most potent and rapid-acting. Indolic compounds generally displayed lower activity compared to their original arylhydrazones.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Chemistry, Medicinal
Jiale Wu, Jiafeng Wang, Yinglong Han, Yu Lin, Jing Wang, Ming Bu
Summary: A series of novel betulin derivatives containing hydrazide-hydrazone moieties were synthesized and evaluated for cytotoxicity against human carcinoma cell lines. Compound 6i showed the most potent activity against HepG2 and MCF-7 cell lines, indicating its potential as a promising skeleton for future development of antitumor agents.
NATURAL PRODUCT COMMUNICATIONS
(2021)
Article
Chemistry, Organic
M. Ihsan Han, Ozge Deniz Yesil Baysal, Guzide Satir Basaran, Gulay Sezer, Dilek Telci, S. Guniz Kucukguzel
Summary: In this study, novel Tetracaine derivatives bearing hydrazide-hydrazone moiety were designed, synthesized, and evaluated for anticancer activity. Among the synthesized compounds, 4-(Butylamino)-N'-[(2,4-dichlorophenyl)methylidene]benzohydrazide (2i) showed the most potent anticancer activity against human hepatocellular carcinoma (HepG2) and lung carcinoma (A549) cell lines. Compound 2i induced apoptosis and suppressed the expression of anti-apoptotic proteins Bax and Bcl-2.
Review
Biochemistry & Molecular Biology
Lukasz Popiolek
Summary: This review focuses on the latest scientific reports regarding the antibacterial, antimycobacterial, and antifungal activities of hydrazide-hydrazones published between 2017 and 2021, providing a concise summary that may serve as a practical guide for the design of new molecules with antimicrobial activity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Medicine, Research & Experimental
Lukasz Popiolek
Summary: This review focuses on the synthesis and biological properties of azetidin-2-one derivatives, which serve as important intermediates for the synthesis of heterocyclic systems such as 1,3-benzothiazin-4-one, 1,3-thiazolidin-4-one, azetidin-2-one, and 1,3,4-oxadiazole derivatives. Azetidin-2-one derivatives exhibit antibacterial, antitubercular, antifungal, anti-inflammatory, antioxidant, anticonvulsant, and antidepressant activities, as well as activity against Parkinson's disease.
BIOMEDICINE & PHARMACOTHERAPY
(2023)
Article
Chemistry, Multidisciplinary
Tanisha Arora, Jai Devi, Ankit Boora, Bharti Taxak, Swati Rani
Summary: In this study, new metal complexes were synthesized and characterized. The results showed that some of these complexes exhibited potent antimicrobial and antitubercular activities, as well as good antioxidant properties. Furthermore, in silico ADME studies indicated that these compounds have the potential to be administered orally as active drugs.
RESEARCH ON CHEMICAL INTERMEDIATES
(2023)
Article
Chemistry, Multidisciplinary
Kanwal, Khalid Mohammed Khan, Sridevi Chigurupati, Farman Ali, Munissa Younus, Maha Aldubayan, Abdul Wadood, Huma Khan, Muhammad Taha, Shahnaz Perveen
Summary: Indole-3-acetamides were synthesized and evaluated for their antihyperglycemic and antioxidant potentials, with compound 15 showing the most promising activity. These compounds demonstrate potential value in inhibiting alpha-amylase and acting as antioxidants.
Article
Chemistry, Physical
Naghmana Kausar, Shahzad Murtaza, Muhammad Nadeem Arshad, Rubina Munir, Rahman Shah Zaib Saleem, Hummera Rafique, Abdul Tawab
Summary: A series of novel hydrazone derivatives of thiophene-2-carboxamide based benzohydrazide were synthesized and evaluated for their dual inhibitory activities against cholinesterases and antioxidant potential. Compound 13 was identified as the most active inhibitor, showing promising inhibitory effects against both cholinesterases.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Biochemistry & Molecular Biology
Seyit Ali Gungor
Summary: A series of hydrazide-hydrazone imine derivative compounds were synthesized and characterized using spectroscopic methods. The inhibitory activities of these compounds against AChE and BChE were investigated, and compound 3i exhibited the best inhibitory activity against AChE, while compound 3h showed the best inhibitory property against BChE. The most stable conformations of AChE and BChE with the compounds were determined, and the compounds were found to have good oral bioavailability properties according to the in silico results and pharmacokinetic parameters of ADME.
CHEMICAL BIOLOGY & DRUG DESIGN
(2023)
Article
Biochemistry & Molecular Biology
M. Ihsan Han, Pinar Atalay, Cansu Umran Tunc, Gokhan Unal, Serkan Dayan, Omer Aydin, S. Guniz Kucukguzel
Summary: Novel (S)-Naproxen derivatives were synthesized and compound 3a exhibited potent anticancer activity against two human breast cancer cell lines. The compound also showed anticancer effects in a mouse breast cancer model, reducing tumor volume in both low and high doses.
BIOORGANIC & MEDICINAL CHEMISTRY
(2021)
Article
Chemistry, Physical
Metin Konus, Dogan Cetin, Nurhan Didem Kizilkan, Can Yilmaz, Ceylan Fidan, Muheb Algso, Emrah Kavak, Arif Kivrak, Aslihan Kurt-Kizildogan, Cigdem Otur, Dogukan Mutlu, Amine Hafis Abdelsalam, Sevki Arslan
Summary: Indoles play critical roles in medicinal chemistry to design new biologically active molecules with higher biological activities and new biological properties. In this study, several novel indole compounds were synthesized and compound 3 and 7 showed promising drug candidate characteristics in in silico evaluation.
JOURNAL OF MOLECULAR STRUCTURE
(2022)
Article
Chemistry, Physical
Rima D. Alharthy, Syeda Bakhtawar Zahra, Noor Fatima, Arooma Tabassum, Saeed Ullah, Sobia Ahsan Halim, Ajmal Khan, Javid Hussain, Ahmed Al-Harrasi, Zahid Shafiq
Summary: The objective of this study was to find substances with potential anti-hyperglycemic effects by blocking alpha-glucosidase. Several novel indole-hydrazide conjugates (3a-3r) were synthesized and examined using spectroscopic methods. These compounds showed potent inhibition of alpha-glucosidase, with IC50 values ranging from 0.51-42.91 μM, and the compounds 3p and 3o demonstrated the highest inhibition with IC50 values of 0.51 +/- 0.06 and 1.57 +/- 0.08 μM, respectively. The structure-activity relationships indicated that the alpha-glucosidase potential of these compounds varied with different substituents on the novel indole-hydrazide. Kinetics and docking examination revealed that the active compounds accommodated well in the active site of alpha-glucosidase and displayed mixed-type inhibition.
JOURNAL OF MOLECULAR STRUCTURE
(2023)
Article
Biochemistry & Molecular Biology
Derya Osmaniye, Iqrar Ahmad, Begum Nurpelin Saglik, Serkan Levent, Harun M. Patel, Yusuf Ozkay, Zafer Asim Kaplancikli
Summary: Alzheimer's disease is a progressive and fatal neurodegenerative disease that affects the elderly and is characterized by memory and cognitive impairments. In this study, new compounds were synthesized and their inhibitory potentials against AChE and BChE were evaluated. Two compounds showed significant activity against AChE. Further analysis revealed their interactions with the enzyme active site similar to a reference drug.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Article
Chemistry, Physical
Hakan Goker, Seckin Ozden
JOURNAL OF MOLECULAR STRUCTURE
(2019)
Editorial Material
Biochemistry & Molecular Biology
Luciano Saso, Hande Gurer-Orhan, Visnja Stepanic
Article
Toxicology
A. T. Aliyev, S. Ozcan-Sezer, A. Akdemir, H. Gurer-Orhan
Summary: Apigenin, a flavonoid, is known to act as an estrogen receptor agonist and inhibit aromatase enzyme. Amentoflavone, a biflavonoid, has been evaluated for its endocrine modulatory effects and antitumor activity in breast cancer cells, showing potential selective cytotoxicity but not a viable alternative to current drugs. Further studies are required to investigate its in vivo effects.
HUMAN & EXPERIMENTAL TOXICOLOGY
(2021)
Review
Biochemistry & Molecular Biology
Alev Tascioglu Aliyev, Emiliano Panieri, Visnja Stepanic, Hande Gurer-Orhan, Luciano Saso
Summary: Oxidative stress disrupts the balance between prooxidants and antioxidants, leading to potential biomolecular damage and involvement in various diseases. NRF2, a key regulator of oxidative stress, has potential benefits in the prevention of breast cancer but overactivation may negatively impact cancer therapy. Known oxidative stress modulators like melatonin and polyphenols are suggested to play a role in cancer prevention and treatment through NRF2 activation.
Review
Biochemistry & Molecular Biology
Elif I. Erguc, Alev Tascioglu-Aliyev, Bita Entezari, Hande Gurer-Orhan
Summary: Endocrine disruptors are exogenous chemicals that interfere with the normal function of endogenous hormones. These chemicals, including pharmaceuticals, phytoestrogens, natural hormones, pesticides, plasticizers, can have potential toxic effects depending on their biotransformation.
CURRENT DRUG METABOLISM
(2021)
Article
Chemistry, Physical
Mustafa Orhan Puskullu, Fatima Doganc, Seckin Ozden, Ertan Sahin, Ismail Celik, Hakan Goker
Summary: Imidazole-containing heterocycles, such as imidazopyridines and imidazopyrimidines, were studied for their regioselectivities in N-alkylation reactions with 4-chlorobenzyl bromide under basic conditions. The main findings include the preference for N-benzylation on six-membered heterocycles and structural confirmation through NMR spectroscopy, X-ray crystallography, and Density Functional Theory (DFT) studies.
JOURNAL OF MOLECULAR STRUCTURE
(2021)
Article
Chemistry, Multidisciplinary
Hanif Shirinzadeh, Esra Dilek, Zuhal Alim
Summary: This study investigated the inhibition effects of naphthalenylmethylen hydrazine derivatives on acetylcholinesterase (AChE) and paraoxonase 1 (PON1). The results showed that these derivatives had strong inhibitory effects on both enzymes. This contributes to the determination of side effects of naphthalene-based pharmacological compounds and the synthesis studies of new AChE inhibitors.
Meeting Abstract
Toxicology
D. Bozdag, H. Gurer-Orhan, J. Kamstra
TOXICOLOGY LETTERS
(2022)
Article
Biochemistry & Molecular Biology
Ebru Akman, Hanif Sirinzade, Serap Yilmaz Ozguven, Esra Dilek, Sibel Suzen
Summary: In this study, the in vitro effects of indole Schiff bases on acetylcholinesterase and human carbonic anhydrase isoforms I and II were investigated. The synthesized indole derivatives were found to inhibit the enzymes significantly, with Ki values in the nanomolar range. Docking studies and interactions with enzymes verified the in vitro results.
JOURNAL OF BIOMOLECULAR STRUCTURE & DYNAMICS
(2023)
Meeting Abstract
Toxicology
A. Tascioglu Aliyev, K. Krager, F. LoBianco, K. Ozbilgin, M. Ucoz, N. Aykin-Burns, H. Gurer-Orhan
TOXICOLOGY LETTERS
(2021)
Article
Biochemistry & Molecular Biology
Hanif Shirinzadeh, Eddy Neuhaus, Elif Ince Erguc, Alev Tascioglu Aliyev, Hande Gurer-Orhan, Sibel Suzen
BIOORGANIC CHEMISTRY
(2020)
Article
Chemistry, Physical
Hanif Shirinzadeh, Esra Dilek
JOURNAL OF MOLECULAR STRUCTURE
(2020)
Article
Pharmacology & Pharmacy
Hanif Shirinzadeh, Mohammed Ghalia, Alev Tascioglu, Ferial Intissar Adjali, Gulsen Gunesacar, Hande Gurer-Orhan, Sibel Suzen
BRAZILIAN JOURNAL OF PHARMACEUTICAL SCIENCES
(2020)
