Article
Biochemistry & Molecular Biology
Elmas Begum Cakmak, Belma Zengin Kurt, Dilek Ozturk Civelek, Andrea Angeli, Atilla Akdemir, Fatih Sonmez, Claudiu T. Supuran, Mustafa Kucukislamoglu
Summary: Carbonic anhydrase (CA) IX and XII isoforms are highly expressed in various human tissues and cancers, with CA IX being a prominent target due to its overexpression in hypoxic tumors. A study synthesized and characterized twenty-seven novel compounds with inhibitory activities against CA I, CA II, CA IX, and CA XII isoforms, among which compound 2m showed the highest inhibition against hCA IX. Furthermore, compounds 3a, 3e, and 3f exhibited the most cytotoxic effects across different cell lines.
BIOORGANIC CHEMISTRY
(2021)
Article
Biochemical Research Methods
Amber R. Rose, Marianne E. Staretz, Monica Joshi, Matthew Wood, Thomas A. Brettell
Summary: This study optimized the separation of eight aminoindane analogues, determining their linear retention indices on four capillary columns. Based on the retention data, all eight aminoindanes were resolved on an Rxi (R)-624Sil MS column. Each aminoindane exhibited unique fragmentation ions in the mass spectra to distinguish between similar analogues.
RAPID COMMUNICATIONS IN MASS SPECTROMETRY
(2021)
Article
Biochemistry & Molecular Biology
Farhat Ramzan, Syed Ayaz Nabi, Mehak Saba Lone, Alessandro Bonardi, Aabid Hamid, Sameena Bano, Kalicharan Sharma, Syed Shafi, Mohammed Samim, Kalim Javed, Claudiu T. Supran
Summary: A series of newly designed (E)-1-(4-sulphamoylphenylethyl)-3-arylidene-5-aryl-1H-pyrrol-2(3H)-ones were synthesized and evaluated as inhibitors for four human isoforms of carbonic anhydrase (CA, EC 4.2.1.1) with pharmaceutical potential, namely hCA I, II, IX, and XII. These compounds exhibited varying potencies in the low to high nanomolar range against all isoforms. Introducing strong electron-withdrawing groups at the para position of the arylidene ring enhanced the enzyme binding affinity. Computational ADMET analysis demonstrated that all compounds possessed acceptable pharmacokinetic range and physicochemical characteristics. Density Functional Theory (DFT) calculations of 3n revealed the stability of the E isomer over the Z isomer by -8.2 kJ mol(-1). Our findings suggest that these molecules serve as promising leads in the search for new CA inhibitors.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2023)
Article
Chemistry, Inorganic & Nuclear
Bunyamin Aygun, Burak Alaylar, Akin Akincioglu, Bunyamin Alim, Ebu Talip Kocaman, Mehmet Karadayi, Mohammed Ibrahim Abu Al-Sayyed, Seyma Aksu, Erdem Sakar, Ozgur Firat Ozpolat, Suleyman Goksu, Medine Gulluce, Abdulhalik Karabulut
Summary: The study investigated the potential drug active substances with the ability to reduce the effects of radiation on human tissues and cells by synthesizing eight different types of sulfamide derivatives. The derivatives were found to have superior radiation absorption abilities compared to reference materials, and genotoxicity tests showed that they are safe at concentrations up to 5 mM. It is suggested that these derivative materials can be used as active substances for a drug to protect against both neutron and gamma radiation.
Article
Biochemistry & Molecular Biology
Micaela Tirri, Giorgia Corli, Raffaella Arfe, Beatrice Marchetti, Sabrine Bilel, Tatiana Bernardi, Federica Boccuto, Sara Odoardi, Serena Mestria, Sabina Strano-Rossi, Matteo Marti
Summary: Drug forums are important sources for the popularity of new psychoactive substances (NPS), especially for those not yet illegal. This study aims to evaluate the acute effects of NM2AI on mice. The results show changes in sensory and physiological functions, nociceptor sensitivity, grip strength, sensorimotor abilities, and mild hallucinogenic effects. The main active metabolite of NM2AI is 2-aminoindane (2AI). These effects are consistent with reports from networked users.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Health Care Sciences & Services
Mirabela Romanescu, Valentina Buda, Adelina Lombrea, Minodora Andor, Ionut Ledeti, Maria Suciu, Corina Danciu, Cristina Adriana Dehelean, Liana Dehelean
Summary: Studies show that there are differences in drug response between men and women, particularly in central nervous system drugs. Different genders significantly influence the pharmacokinetics and pharmacodynamics of drugs. Although many studies have conflicting results, there are certain sex-related differences in each drug class. There are differences in response to opioids, antidepressants, and antipsychotics between genders.
JOURNAL OF PERSONALIZED MEDICINE
(2022)
Article
Biochemistry & Molecular Biology
Reem Odi, David Bibi, Bella Shusterman, Natalia Erenburg, Chanan Shaul, Claudiu T. Supuran, Alessio Nocentini, Meir Bialer
Summary: The study demonstrated that both MBPC enantiomers exhibited anticonvulsant activity in the rat MES test, with (S)-MBPC showing slightly better brain permeability than (R)-MBPC, potentially contributing to its better anticonvulsant efficacy.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Review
Biochemistry & Molecular Biology
Marc-Michel Wilson, David C. Henshall, Susan M. Byrne, Gary P. Brennan
Summary: Epileptic encephalopathies are severe epilepsy syndromes caused by de novo mutations in the chromodomain helicase DNA binding protein 2 (CHD2) gene. Dysregulation of CHD2 leads to early onset epileptic encephalopathy, abnormal brain function, and intellectual disability.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Organic
Akin Akincioglu, Yusuf Akbaba, Leyla Polat Kose, Leyla Demirkol Akyuz, Sueleyman Goksu
Summary: We carried out racemic synthesis and asymmetric resolution of one 2-aminoindane and three 2-aminotertalins, which play crucial biological roles in the central nervous system (CNS). The desired (+/-)-2-aminoindane and (+/-)-2-aminotetralin derivatives were synthesized from appropriate reagents. Different methods were used to obtain enantio pure products.
Article
Medicine, General & Internal
Van Vo, Richard L. Tillett, Katerina Papp, Ching-Lan Chang, Anthony Harrington, Michael Moshi, Edwin C. Oh, Daniel Gerrity
Summary: This study leveraged spatial and temporal differences in wastewater WGS data to quantify the relative contributions of visitors to SARS-CoV-2 in southern Nevada. The results showed that on December 13, Omicron-specific mutations accounted for 48% of all genomes in the Las Vegas Strip manhole, while the proportion in facilities 2 and 3 was only 4.1%. The study concluded that visitors contributed more than 60% of the SARS-CoV-2 load in the sewershed serving the Las Vegas Strip, highlighting the importance of wastewater surveillance for estimating COVID-19 incidence.
Article
Biochemistry & Molecular Biology
Sarah Mazzotta, Judith Berastegui-Cabrera, Margarita Vega-Holm, Maria del Rosario Garcia-Lozano, Marta Carretero-Ledesma, Francesca Aiello, Jose Manuel Vega-Perez, Jeronimo Pachon, Fernando Iglesias-Guerra, Javier Sanchez-Cespedes
Summary: A new library of anti-adenovirus compounds based on 3-amino-1,2-propanediol skeleton was designed and synthesized, with seven compounds showing high anti-HAdV activity at low concentrations and low cytotoxicity. Mechanistic assays revealed that some compounds target specific processes in HAdV replication.
BIOORGANIC CHEMISTRY
(2021)
Article
Chemistry, Organic
Lu Lin, Peng Wang, Tao Dong, Gavin Chit Tsui, Saihu Liao
Summary: Here, we present a transition-metal-free and visible-light-mediated radical 1-fluorosulfonyl-2-heteroarylation of alkenes, which enables the synthesis of a variety of SO2F-containing quinoxalin-2(1H)-ones, a critical structural motif widely found in biologically active molecules. Furthermore, we demonstrate the application of this method in the modification of other heterocycles and drug molecules, as well as ligation chemistry via SuFEx click reactions.
Article
Hematology
Matthew J. Frigault, Jorg Dietrich, Kathleen Gallagher, Mark Roschewski, Justin T. Jordan, Deborah Forst, Scott R. Plotkin, Daniella Cook, Keagan S. Casey, Kevin A. Lindell, Gabriel D. Depinho, Katelin Katsis, Eva Lynn Elder, Mark B. Leick, Bryan Choi, Nora Horick, Frederic Preffer, Meredith Saylor, Steven McAfee, Paul O'Donnell, Thomas R. Spitzer, Bimalangshu Dey, Zachariah DeFilipp, Areej El-Jawahri, Tracy T. Batchelor, Marcela Maus, Yi-Bin Chen
Summary: This study conducted a clinical trial of tisagenlecleucel in highly refractory patients with primary central nervous system lymphoma (PCNSL). The results showed that most patients responded well to the treatment and there were no severe side effects. This suggests that tisagenlecleucel is safe and effective in this patient population.
Article
Biochemistry & Molecular Biology
Stanislav Kalinin, Alexander Kovalenko, Annika Valtari, Alessio Nocentini, Maxim Gureev, Arto Urtti, Mikhail Korsakov, Claudiu T. Supuran, Mikhail Krasavin
Summary: Hydrophilic derivatives of carbonic anhydrase inhibitors were designed, prepared, and profiled against a panel of carbonic anhydrase isoforms. Computational prediction showed that these hydrophilic derivatives predominantly enter the eye through conjunctival absorption rather than corneal absorption. The potentially reactive periphery of these compounds makes them suitable candidates for bioconjugation to polymeric drug carriers.
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
(2022)
Review
Veterinary Sciences
Maria M. Kotova, David S. Galstyan, Tatiana O. Kolesnikova, Murilo S. de Abreu, Tamara G. Amstislavskaya, Tatyana Strekalova, Elena V. Petersen, Konstantin B. Yenkoyan, Konstantin A. Demin, Allan V. Kalueff
Summary: Antimicrobial drugs can influence the central nervous system and gut microbiota, leading to changes in brain and behavior. Zebrafish models are useful for studying the effects of these drugs on the central nervous system. Recent research has revealed the impacts of a wide range of antimicrobial drugs on brain and behavior in zebrafish.
VETERINARY SCIENCES
(2023)
Article
Biotechnology & Applied Microbiology
Bunyamin Ozgeris
Summary: A series of thioureas were synthesized from various amines and nicotinic acid, exhibiting antimicrobial and antioxidant properties. These compounds showed moderate activity against bacteria causing nosocomial infections with acquired resistance to antibiotics, along with strong antioxidant properties. Thus, they have the potential to be developed as agents for treating bacterial infections and health issues related to aging such as cancer and neurodegenerative diseases.
JOURNAL OF ANTIBIOTICS
(2021)
Article
Chemistry, Medicinal
Nihal Gok, Akin Akincioglu, Edanur Erumit Binici, Hulya Akincioglu, Namik Kilinc, Suleyman Goksu
Summary: A series of novel dopamine analogs were synthesized incorporating urea and sulfonamide functional groups, exhibiting anticholinergic and antioxidant effects. Compound 13 showed inhibition for both acetylcholinesterase and butyrylcholinesterase, while compounds 16 and 18 demonstrated higher reducing power and better radical scavenging activity.
ARCHIV DER PHARMAZIE
(2021)
Article
Chemistry, Organic
B. Ozgeris
Summary: Thiourea-based scaffolds, particularly with phenethylamine derivatives, have shown promising antimicrobial activity against bacteria resistant to multiple antibiotics and strong antioxidant properties. This highlights their potential as antibacterial and antioxidant agents for treating bacterial infections and age-related health issues.
RUSSIAN JOURNAL OF ORGANIC CHEMISTRY
(2021)
Article
Biochemistry & Molecular Biology
Fevzi Topal, Kadir Aksu, Ilhami Gulcin, Ferhan Tumer, Suleyman Goksu
Summary: This study identified a series of symmetric sulfamide compounds that exhibited good inhibitory effects against human carbonic anhydrase I and II isoenzymes, with compound 11 showing the best performance. Acetazolamide, used as the standard, displayed higher IC50 values. Additionally, in silico ADME-Tox study showed good oral bioavailability for all synthesized compounds according to Jorgensen's rule of three and Lipinski's rule of five.
CHEMISTRY & BIODIVERSITY
(2021)
Article
Chemistry, Multidisciplinary
Fatma Betul Ozgeris, Bunyamin Ozgeris
Summary: This study reveals the synthesis and biological evaluation of novel phenethylamine-based urea derivatives in cancer cell lines and antioxidant properties. Some compounds exhibited comparable or even higher cytotoxicity than cisplatin, suggesting their potential for anticancer treatment.
MONATSHEFTE FUR CHEMIE
(2021)
Article
Chemistry, Organic
Yasin Cetinkaya, Ahmet Maras, Suleyman Goksu
Summary: This study investigates intramolecular interactions in (1S(R),2S(R))-2-azidocycloalk-3-en-1-ols and (1S(R),2S(R))-2-azidocycloalk-3-en-1-yl acetates consisting of six-to eight-membered rings through molecular spectroscopy and density functional theory calculations. The results show that the allylic azides stabilized by intramolecular interactions do not cause the known rearrangement reactions.
Article
Biology
Akin Akincioglu, Suleyman Goksu, Ali Naderi, Hulya Akincioglu, Namik Kilinc, Ilhami Gulcin
Summary: Novel substituted benzylamines derived from dihydrochalcones exhibit potent inhibitory actions against carbonic anhydrase and cholinesterases, making significant contributions to the treatment of global diseases such as Alzheimer's and glaucoma.
COMPUTATIONAL BIOLOGY AND CHEMISTRY
(2021)
Article
Chemistry, Inorganic & Nuclear
Bunyamin Aygun, Burak Alaylar, Akin Akincioglu, Bunyamin Alim, Ebu Talip Kocaman, Mehmet Karadayi, Mohammed Ibrahim Abu Al-Sayyed, Seyma Aksu, Erdem Sakar, Ozgur Firat Ozpolat, Suleyman Goksu, Medine Gulluce, Abdulhalik Karabulut
Summary: The study investigated the potential drug active substances with the ability to reduce the effects of radiation on human tissues and cells by synthesizing eight different types of sulfamide derivatives. The derivatives were found to have superior radiation absorption abilities compared to reference materials, and genotoxicity tests showed that they are safe at concentrations up to 5 mM. It is suggested that these derivative materials can be used as active substances for a drug to protect against both neutron and gamma radiation.
Article
Toxicology
Veysel Parlak, Bunyamin Ozgeris, Arzu Ucar, Asli Cilingir Yeltekin, Fatma Betul Ozgeris, Ozge Caglar, Gonca Alak, Hasan Turkez, Muhammed Atamanalp
Summary: This study evaluated the hematological, oxidative, and genotoxic damage potentials of 3-Benzoylpyridine (3BP) on rainbow trout. The results showed that 3BP caused hematological and oxidative alterations as well as genotoxic damage in rainbow trout.
TOXICOLOGY MECHANISMS AND METHODS
(2022)
Article
Chemistry, Multidisciplinary
Yusuf Akbaba, Fatma Necmiye Kaci, Suleyman Goksu
Summary: Multi-target drug discovery is crucial in the treatment of carcinogenesis. In this study, a series of new urea derivatives were synthesized and their anti-cancer and antimicrobial properties were investigated. One synthesized urea derivative exhibited the best anti-cancer activity against HeLa cancer cells, with less toxicity against non-cancerous cells. Some urea derivatives also showed antibacterial activities against multiple bacterial strains.
Article
Chemistry, Organic
Akin Akincioglu, Yusuf Akbaba, Leyla Polat Kose, Leyla Demirkol Akyuz, Sueleyman Goksu
Summary: We carried out racemic synthesis and asymmetric resolution of one 2-aminoindane and three 2-aminotertalins, which play crucial biological roles in the central nervous system (CNS). The desired (+/-)-2-aminoindane and (+/-)-2-aminotetralin derivatives were synthesized from appropriate reagents. Different methods were used to obtain enantio pure products.
Article
Chemistry, Multidisciplinary
Akin Akincioglu, Yusuf Akbaba, Leyla Polat Kose, Suleyman Goksu
Summary: Compounds with 1-aminoindane motif have important biological activities in the central nervous system. This study focused on synthesizing new compounds with this structure and obtaining them in high enantiopurity. Novel substituted 1-aminoindane derivatives were synthesized and their asymmetric resolutions were carried out. The resulting asymmetric amines with high enantio-purity were obtained through a series of reactions.
Article
Chemistry, Multidisciplinary
Ali Naderi, Akin Akincioglu, Ahmet Cagan, Suleyman Goksu, Parham Taslimi, Ilhami Gulcin
Summary: A series of novel sulfamides were synthesized and tested for their inhibition properties on hCA I and II, AChE, and BChE enzymes. The majority of the compounds were more effective against AChE than tacrine, while some were also more effective against BChE. The most potent compounds against cholinesterase enzymes were N,N-dimethyl-[3-(2,4-dimethoxyphenyl)propyl]sulfamide and two other sulfamide derivatives.
STUDIA UNIVERSITATIS BABES-BOLYAI CHEMIA
(2023)
Article
Chemistry, Applied
Fatma Betul Ozgeris, Fatma Necmiye Kaci, Bunyamin Ozgeris, Arzu Gormez
Summary: This study synthesized urea derivatives containing substituted phenethylamine rings and found that while the compound was inactive against bacterial strains, it exhibited remarkable anti-cancer and antioxidant activities. The unsymmetrical urea compound showed significant anticancer activity, particularly against the HeLa cell line, with potential as an anticancer and antioxidant agent for treating cancer and related diseases.
BIOINTERFACE RESEARCH IN APPLIED CHEMISTRY
(2022)
Article
Chemistry, Multidisciplinary
Bunyamin Ozgeris
MONATSHEFTE FUR CHEMIE
(2020)
Article
Chemistry, Organic
Dilek Isik Tasgin, Irem Bayraktar
Summary: We present a synthetic method for pyrrolizine-3-one derivatives and investigate their photophysical properties. These compounds are prepared through a series of reactions involving substituted pyrroles in one-pot, two-step oxidation, and intramolecular cyclization processes. The photophysical properties of the synthesized compounds are studied using UV-Vis and fluorescence spectroscopy in various solvents. The introduction of pyrrolyl substituents has a significant impact on Stokes shifts and quantum yield values.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Satish Kumar Burra, Vaikunta Rao Lakinani, Raghunadh Akula, Chiranjeevi Yankkanti
Summary: A novel and green strategy for the construction of biologically relevant substituted indolyl-4H-chromenes scaffolds is reported, using L-proline as a catalyst and water as a promoter solvent. This catalytic system offers wider applicability, shorter reaction times, and high yields, making it an ideal condition for green chemistry.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Abouelhaoul El Alami, Amine El Maraghi, Fatima Youssoufi, Assiya Atif, Hamid Sdassi
Summary: Nitrobenzimidazoles have become increasingly important in the design of new compounds in medicinal, therapeutic and chemical fields. This review provides an overview of the synthesis strategies and biological activities of nitrobenzimidazole derivatives.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Nilesh Raghunath Khedkar, Alex Joseph, Milind Sindkhedkar
Summary: In this study, a new library of 3-(2-(pyrimidin-5-yl)thiazol-4-yl)-1,2,4-oxadiazole compounds was designed and synthesized as potential anticancer agents using in silico fragment-based drug design. The compounds were tested for their anticancer activity in vitro, and one compound exhibited excellent activity against multiple cancer cell lines.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Terungwa H. Iorkula, Bryce A. Tolman, Scott R. Burt, Matt A. Peterson
Summary: A new method for synthesizing C-6 substituted products has been discovered in this study, which utilizes lower doses of fluoride and CsF as a catalyst, with high reaction yields and cost-effectiveness under suitable conditions.
SYNTHETIC COMMUNICATIONS
(2024)
Review
Chemistry, Organic
Ranjana Aggarwal, Swati Sharma
Summary: This review article mainly focuses on the synthesis of 3(5)-trifluoromethylpyrazoles via condensation reaction of trifluoromethyl-beta-diketones with hydrazines. It emphasizes the importance of fluorine-containing compounds and pyrazoles in the field of biology. The literature reported condensation reactions of trifluoromethyl-beta-diketones with hydrazines are covered.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
F. M. Alshareef, Sami A. Al-Harbi, Esam S. Allehyani, Omeima Abdullah, Magdy A. Ibrahim
Summary: This study aimed to construct a novel category of linear annulated chromeno[3',2':5,6]pyrido[2,3-d][1,3]thiazolo[3,2-a]pyrimidines. The chemical reactivity of the synthesized compounds was investigated, and they showed significant antimicrobial activity against various strains.
SYNTHETIC COMMUNICATIONS
(2024)
Article
Chemistry, Organic
Preethi Dhanapal, S. L. Manju
Summary: Thiazole based Schiff base scaffolds have become an integral part of drug development in recent years, playing a versatile role as building blocks for lead drug molecules. This study presents a facile one pot synthetic method for producing novel 4-aryl thiazoles with high yield, shorter reaction time, and milder conditions, without the need for catalysts or purification techniques.
SYNTHETIC COMMUNICATIONS
(2024)