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Article ; Online: Recent Trends in Enzyme Inhibition and Activation in Drug Design

Athina Geronikaki

Molecules, Vol 26, Iss 17, p

2021 Volume 17

Abstract: It is known that enzymes are involved in many pathological conditions, such as inflammation, diabetes, microbial infections, HIV, neoplastic, neglected diseases and others [.] ...

Abstract	It is known that enzymes are involved in many pathological conditions, such as inflammation, diabetes, microbial infections, HIV, neoplastic, neglected diseases and others [.]
Keywords	n/a ; Organic chemistry ; QD241-441
Language	English
Publishing date	2021-12-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Enzymes and Enzyme Inhibitors—Applications in Medicine and Diagnosis

Athina Geronikaki / Phaedra T. Eleutheriou

International Journal of Molecular Sciences, Vol 24, Iss 5245, p

2023 Volume 5245

Abstract: This is the first part of a Special Issue on enzymes and enzymes inhibitors and their applications in medicine and diagnosis [.] ...

Abstract	This is the first part of a Special Issue on enzymes and enzymes inhibitors and their applications in medicine and diagnosis [.]
Keywords	n/a ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
Language	English
Publishing date	2023-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Thiazole Ring—A Biologically Active Scaffold

Anthi Petrou / Maria Fesatidou / Athina Geronikaki

Molecules, Vol 26, Iss 3166, p

2021 Volume 3166

Abstract: Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, ... ...

Abstract	Background: Thiazole is a good pharmacophore nucleus due to its various pharmaceutical applications. Its derivatives have a wide range of biological activities such as antioxidant, analgesic, and antimicrobial including antibacterial, antifungal, antimalarial, anticancer, antiallergic, antihypertensive, anti-inflammatory, and antipsychotic. Indeed, the thiazole scaffold is contained in more than 18 FDA-approved drugs as well as in numerous experimental drugs. Objective: To summarize recent literature on the biological activities of thiazole ring-containing compounds Methods: A literature survey regarding the topics from the year 2015 up to now was carried out. Older publications were not included, since they were previously analyzed in available peer reviews. Results: Nearly 124 research articles were found, critically analyzed, and arranged regarding the synthesis and biological activities of thiazoles derivatives in the last 5 years.
Keywords	thiazoles ; antimicrobial ; neglected ; anticonvulsant ; anti-inflammatory ; carbonic anhydise ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2021-05-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Book ; Online: In Silico Evaluation of the Effectivity of Approved Protease Inhibitors against the Main Protease of the Novel SARS-CoV-2 Virus

Phaedra Eleftheriou / Dionysia Amanatidou / Anthi Petrou / Athina Geronikaki

Molecules ; Volume 25 ; Issue 11

2020

Abstract: The coronavirus disease, COVID-19, caused by the novel coronavirus SARS-CoV-2, which first emerged in Wuhan, China and was made known to the World in December 2019 turned into a pandemic causing more than 126,124 deaths worldwide up to April 16th, 2020. ... ...

Abstract	The coronavirus disease, COVID-19, caused by the novel coronavirus SARS-CoV-2, which first emerged in Wuhan, China and was made known to the World in December 2019 turned into a pandemic causing more than 126,124 deaths worldwide up to April 16th, 2020. It has 79.5% sequence identity with SARS-CoV-1 and the same strategy for host cell invasion through the ACE-2 surface protein. Since the development of novel drugs is a long-lasting process, researchers look for effective substances among drugs already approved or developed for other purposes. The 3D structure of the SARS-CoV-2 main protease was compared with the 3D structures of seven proteases, which are drug targets, and docking analysis to the SARS-CoV-2 protease structure of thirty four approved and on-trial protease inhibitors was performed. Increased 3D structural similarity between the SARS-CoV-2 main protease, the HCV protease and α -thrombin was found. According to docking analysis the most promising results were found for HCV protease, DPP-4, α -thrombin and coagulation Factor Xa known inhibitors, with several of them exhibiting estimated free binding energy lower than − 8.00 kcal/mol and better prediction results than reference compounds. Since some of the compounds are well-tolerated drugs, the promising in silico results may warrant further evaluation for viral anticipation. DPP-4 inhibitors with anti-viral action may be more useful for infected patients with diabetes, while anti-coagulant treatment is proposed in severe SARS-CoV-2 induced pneumonia.
Keywords	coronavirus ; SARS-CoV-2 ; protease inhibitors ; HCV protease inhibitors ; DPP-4 inhibitors ; a-thrombin inhibitors ; docking ; covid19
Subject code	540
Language	English
Publishing date	2020-05-29
Publisher	Multidisciplinary Digital Publishing Institute
Publishing country	ch
Document type	Book ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: In Silico Evaluation of the Effectivity of Approved Protease Inhibitors against the Main Protease of the Novel SARS-CoV-2 Virus

Phaedra Eleftheriou / Dionysia Amanatidou / Anthi Petrou / Athina Geronikaki

Molecules, Vol 25, Iss 2529, p

2020 Volume 2529

Abstract	The coronavirus disease, COVID-19, caused by the novel coronavirus SARS-CoV-2, which first emerged in Wuhan, China and was made known to the World in December 2019 turned into a pandemic causing more than 126,124 deaths worldwide up to April 16th, 2020. It has 79.5% sequence identity with SARS-CoV-1 and the same strategy for host cell invasion through the ACE-2 surface protein. Since the development of novel drugs is a long-lasting process, researchers look for effective substances among drugs already approved or developed for other purposes. The 3D structure of the SARS-CoV-2 main protease was compared with the 3D structures of seven proteases, which are drug targets, and docking analysis to the SARS-CoV-2 protease structure of thirty four approved and on-trial protease inhibitors was performed. Increased 3D structural similarity between the SARS-CoV-2 main protease, the HCV protease and α-thrombin was found. According to docking analysis the most promising results were found for HCV protease, DPP-4, α-thrombin and coagulation Factor Xa known inhibitors, with several of them exhibiting estimated free binding energy lower than −8.00 kcal/mol and better prediction results than reference compounds. Since some of the compounds are well-tolerated drugs, the promising in silico results may warrant further evaluation for viral anticipation. DPP-4 inhibitors with anti-viral action may be more useful for infected patients with diabetes, while anti-coagulant treatment is proposed in severe SARS-CoV-2 induced pneumonia.
Keywords	coronavirus ; SARS-CoV-2 ; protease inhibitors ; HCV protease inhibitors ; DPP-4 inhibitors ; a-thrombin inhibitors ; Organic chemistry ; QD241-441 ; covid19
Subject code	540
Language	English
Publishing date	2020-05-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: Heterocycle Compounds with Antimicrobial Activity.

Fesatidou, Maria / Petrou, Anthi / Athina, Geronikaki

Current pharmaceutical design

2020 Volume 26, Issue 8, Page(s) 867–904

Abstract: Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of ... ...

Abstract	Background: Bacterial infections are a growing problem worldwide causing morbidity and mortality mainly in developing countries. Moreover, the increased number of microorganisms, developing multiple resistances to known drugs, due to abuse of antibiotics, is another serious problem. This problem becomes more serious for immunocompromised patients and those who are often disposed to opportunistic fungal infections. Objective: The objective of this manuscript is to give an overview of new findings in the field of antimicrobial agents among five-membered heterocyclic compounds. These heterocyclic compounds especially five-membered attracted the interest of the scientific community not only for their occurrence in nature but also due to their wide range of biological activities. Methods: To reach our goal, a literature survey that covers the last decade was performed. Results: As a result, recent data on the biological activity of thiazole, thiazolidinone, benzothiazole and thiadiazole derivatives are mentioned. Conclusion: It should be mentioned that despite the progress in the development of new antimicrobial agents, there is still room for new findings. Thus, research still continues.
MeSH term(s)	Anti-Bacterial Agents/pharmacology ; Anti-Infective Agents/pharmacology ; Heterocyclic Compounds/pharmacology
Chemical Substances	Anti-Bacterial Agents ; Anti-Infective Agents ; Heterocyclic Compounds
Language	English
Publishing date	2020-02-05
Publishing country	United Arab Emirates
Document type	Journal Article ; Review
ZDB-ID	1304236-1
ISSN	1873-4286 ; 1381-6128
ISSN (online)	1873-4286
ISSN	1381-6128
DOI	10.2174/1381612826666200206093815
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Article ; Online: Synthesis, Biological and In Silico Studies of Griseofulvin and Usnic Acid Sulfonamide Derivatives as Fungal, Bacterial and Human Carbonic Anhydrase Inhibitors

Andrea Angeli / Anthi Petrou / Victor Kartsev / Boris Lichitsky / Andrey Komogortsev / Clemente Capasso / Athina Geronikaki / Claudiu T. Supuran

International Journal of Molecular Sciences, Vol 24, Iss 2802, p

2023 Volume 2802

Abstract: Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO 2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho-/physiological conditions. A series of griseofulvin and usnic acid ... ...

Abstract	Carbonic anhydrases (CAs, EC 4.2.1.1) catalyze the essential reaction of CO 2 hydration in all living organisms, being actively involved in the regulation of a plethora of patho-/physiological conditions. A series of griseofulvin and usnic acid sulfonamides were synthesized and tested as possible CA inhibitors. Since β- and γ- classes are expressed in microorganisms in addition to the α- class, showing substantial structural differences to the human isoforms they are also interesting as new antiinfective targets with a different mechanism of action for fighting the emerging problem of extensive drug resistance afflicting most countries worldwide. Griseofulvin and usnic acid sulfonamides were synthesized using methods of organic chemistry. Their inhibitory activity, assessed against the cytosolic human isoforms hCA I and hCA II, the transmembrane hCA IX as well as β- and γ-CAs from different bacterial and fungal strains, was evaluated by a stopped-flow CO 2 hydrase assay. Several of the investigated derivatives showed interesting inhibition activity towards the cytosolic associate isoforms hCA I and hCA II, as well as the three γ-CAs and Malassezia globosa (MgCA) enzyme. Six compounds ( 1b – 1d , 1h, 1i and 1j ) were more potent than AAZ against hCA I while five ( 1d , 1h , 1i , 1j and 4a ) showed better activity than AAZ against the hCA II isoform. Moreover, all compounds appeared to be very potent against MgCA with a Ki lower than that of the reference drug. Furthermore, computational procedures were used to investigate the binding mode of this class of compounds within the active site of human CAs.
Keywords	griseofulvin derivatives ; usnic acid derivatives ; carbonic anhydrase inhibitors ; stopped-flow CO 2 hydrase assay ; in silico studies ; Biology (General) ; QH301-705.5 ; Chemistry ; QD1-999
Subject code	540
Language	English
Publishing date	2023-02-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
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Article ; Online: Antimicrobial Activity of Some Steroidal Hydrazones

Maia Merlani / Nanuli Nadaraia / Lela Amiranashvili / Anthi Petrou / Athina Geronikaki / Ana Ciric / Jasmina Glamoclija / Tamara Carevic / Marina Sokovic

Molecules, Vol 28, Iss 1167, p

2023 Volume 1167

Abstract: Twelve steroid based hydrazones were in silico evaluated using computer program PASS as antimicrobial agents. The experimental evaluation revealed that all compounds have low to moderate antibacterial activity against all bacteria tested, except for B. ... ...

Abstract	Twelve steroid based hydrazones were in silico evaluated using computer program PASS as antimicrobial agents. The experimental evaluation revealed that all compounds have low to moderate antibacterial activity against all bacteria tested, except for B. cereus with MIC at a range of 0.37–3.00 mg/mL and MBC at 0.75–6.00 mg/mL. The most potent appeared to be compound 11 with MIC/MBC of 0.75/1.5 mg/mL, respectively. The evaluation of antibacterial activity against three resistant strains MRSA, E. coli and P. aeruginosa demonstrated superior activity of compounds against MRSA compared with ampicillin, which did not show bacteriostatic or bactericidal activities. All compounds exhibited good antifungal activity with MIC of 0.37–1.50 mg/mL and MFC of 1.50–3.00 mg/mL, but with different sensitivity against fungi tested. According to docking studies, 14-alpha demethylase inhibition may be responsible for antifungal activity. Two compounds were evaluated for their antibiofilm activity. Finally, drug-likeness and docking prediction were performed.
Keywords	hydrazones ; ketosteroids ; antimicrobial activity ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2023-01-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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Article ; Online: 5-Membered Heterocyclic Compounds as Antiviral Agents.

Tratrat, Christophe / Petrou, Anthi / Fesatidou, Maria / Haroun, Michelyne / Athina, Geronikaki / Venugopala, Katharigatta / Sreeharsha, Nagaraja / Chemali, Jad

Current topics in medicinal chemistry

2023 Volume 23, Issue 7, Page(s) 520–538

Abstract: Viral infections range from self-limiting to more serious and fatal infections; therefore, some viral infections are of great public health concern worldwide, e.g., Hepatitis B virus, Hepatitis C virus, and HIV. Recently, the world faced a new infection ... ...

Abstract	Viral infections range from self-limiting to more serious and fatal infections; therefore, some viral infections are of great public health concern worldwide, e.g., Hepatitis B virus, Hepatitis C virus, and HIV. Recently, the world faced a new infection due to the coronavirus, COVID-19, which was announced as a pandemic in early 2020. This virus infected more than 500 million people, killing around 6 million people worldwide. On the other hand, the increase in drug-resistant strains is also creating serious health problems. Thus, developing new selective antiviral agents with a different mode of action to fight against mutated and novel viruses is a primary goal of many researchers. Taking into account the role of heterocyclic compounds in drug discovery as a key structural component of most of the bioactive molecules; herein, we report an extensive review of the antiviral activity of five-membered heterocyclic compounds reported from 2015 to date. In this review, the antiviral activities of the agents containing the specified ring systems thiadiazoles, triazoles, oxadiazoles, and thiazoles are discussed.
MeSH term(s)	Humans ; Antiviral Agents/chemistry ; COVID-19 ; Virus Diseases/drug therapy ; Heterocyclic Compounds/pharmacology ; Heterocyclic Compounds/therapeutic use ; Thiadiazoles/chemistry
Chemical Substances	Antiviral Agents ; Heterocyclic Compounds ; Thiadiazoles
Language	English
Publishing date	2023-04-17
Publishing country	United Arab Emirates
Document type	Review ; Journal Article
ZDB-ID	2064823-6
ISSN	1873-4294 ; 1568-0266
ISSN (online)	1873-4294
ISSN	1568-0266
DOI	10.2174/1568026623666230325153927
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Article ; Online: Thiazoles and Thiazolidinones as COX/LOX Inhibitors

Konstantinos Liaras / Maria Fesatidou / Athina Geronikaki

Molecules, Vol 23, Iss 3, p

2018 Volume 685

Abstract: Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of ... ...

Abstract	Inflammation is a natural process that is connected to various conditions and disorders such as arthritis, psoriasis, cancer, infections, asthma, etc. Based on the fact that cyclooxygenase isoenzymes (COX-1, COX-2) are responsible for the production of prostaglandins that play an important role in inflammation, traditional treatment approaches include administration of non-steroidal anti-inflammatory drugs (NSAIDs), which act as selective or non-selective COX inhibitors. Almost all of them present a number of unwanted, often serious, side effects as a consequence of interference with the arachidonic acid cascade. In search for new drugs to avoid side effects, while maintaining high potency over inflammation, scientists turned their interest to the synthesis of dual COX/LOX inhibitors, which could provide numerous therapeutic advantages in terms of anti-inflammatory activity, improved gastric protection and safer cardiovascular profile compared to conventional NSAIDs. Τhiazole and thiazolidinone moieties can be found in numerous biologically active compounds of natural origin, as well as synthetic molecules that possess a wide range of pharmacological activities. This review focuses on the biological activity of several thiazole and thiazolidinone derivatives as COX-1/COX-2 and LOX inhibitors.
Keywords	thiazole ; thiazolidinone ; COX ; LOX ; anti-inflammatory ; Organic chemistry ; QD241-441
Subject code	540
Language	English
Publishing date	2018-03-01T00:00:00Z
Publisher	MDPI AG
Document type	Article ; Online
Database	BASE - Bielefeld Academic Search Engine (life sciences selection)

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