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Pharmaceuticals
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Pyrazole and Thiazole Derivatives in Medicinal Chemistry
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Pyrazole and Thiazole Derivatives in Medicinal Chemistry

A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: 25 June 2024 | Viewed by 3194

Special Issue Editors

Dr. Dimitris Matiadis

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Guest Editor
1. Department of Biomedical Sciences, University of West Attica, Egaleo Park Campus, 12243 Athens, Greece
2. Institute of Biosciences and Applications, National Centre for Scientific Research “Demokritos”, 15310 Athens, Greece
Interests: heterocyclic and medicinal chemistry; organic synthesis; antimicrobial agents; structure–activity relationships of bioactive compounds; curcuminoids; tetramic acids; pyrazolines
Special Issues, Collections and Topics in MDPI journals
Dr. Antonella Messore

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Guest Editor
Department of Pharmaceutical Chemistry and drug Technology \"Sapienza\", University of Rome, Rome, Italy
Interests: drug design; synthesis of new potential bioactive compounds in the field of anticancer, antiviral and antiparasitic agents; structure–activity relationship study; organic synthesis
Special Issues, Collections and Topics in MDPI journals
Dr. Nicolas Primas

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Guest Editor
Faculté de Pharmacie, Aix Marseille University, 27 Boulevard Jean Moulin, CS30064, CEDEX 05, 13385 Marseille, France
Interests: cross coupling; medicinal chemistry; heterocyclic compound synthesis; organic synthesis; synthetic organic chemistry; medicinal and pharmaceutical chemistry; heterocyclic compounds

Special Issue Information

Dear Colleagues,

Five-membered heterocyclic compounds that contain two heteroatoms are amongst the most prominent scaffolds in medicinal chemistry. Especially, pyrazole and thiazole derivatives are two exceptional classes of bioactive compounds that have received particular attention for their chemical and biological properties.

Pyrazoles (2H-pyrazoles) are aromatic five-membered heterocycles that contain two adjacent nitrogen atoms. Along with their aromatic isomers, including indazoles and isoindazoles, as well as their non-aromatic isomers, namely 3H-pyrazoles, isopyrazoles or 4H-pyrazoles, 1-, 2- or 3-pyrazolines, pyrazolidines and pyrazolones, they are versatile molecules with distinct pharmacological profiles. Moreover, they are found in many commercialized drugs, such as the synthetically derived crizotinib (anticancer) and celecoxib (anti-inflammatory), in addition to naturally occurring products, such as pyrazofurin (antitumor; antiviral).

On the other hand, thiazoles and their derivatives are aromatic heterocycles that contain both an electron-donating group (sulfur) and an iminic electron-accepting group. They are known for their broad spectrum of biological properties, including antibacterial, antifungal, anticancer and antiviral activities. This privileged scaffold is present in many FDA-approved commercially available drugs, ranging from simple structured molecules, such as clomethiazole (sedative and hypnotic) and sulfathiazole (antibiotic), to complex molecules, such as alpelisib (anticancer) and cobicistat (anti-HIV).

For the Special Issue “Pyrazole and Thiazole Derivatives in Medicinal Chemistry”, we welcome the submission of research articles related to one or more of the following topics: the design, synthesis and/or biological evaluation of the aforementioned heterocyclic motifs, including their isomers, conjugates or functionalized derivatives.

Dr. Dimitris Matiadis
Dr. Antonella Messore
Dr. Nicolas Primas
Guest Editors

Manuscript Submission Information

Manuscripts should be submitted online at www.mdpi.com by registering and logging in to this website. Once you are registered, click here to go to the submission form. Manuscripts can be submitted until the deadline. All submissions that pass pre-check are peer-reviewed. Accepted papers will be published continuously in the journal (as soon as accepted) and will be listed together on the special issue website. Research articles, review articles as well as short communications are invited. For planned papers, a title and short abstract (about 100 words) can be sent to the Editorial Office for announcement on this website.

Submitted manuscripts should not have been published previously, nor be under consideration for publication elsewhere (except conference proceedings papers). All manuscripts are thoroughly refereed through a single-blind peer-review process. A guide for authors and other relevant information for submission of manuscripts is available on the Instructions for Authors page. Pharmaceuticals is an international peer-reviewed open access monthly journal published by MDPI.

Please visit the Instructions for Authors page before submitting a manuscript. The Article Processing Charge (APC) for publication in this open access journal is 2900 CHF (Swiss Francs). Submitted papers should be well formatted and use good English. Authors may use MDPI's English editing service prior to publication or during author revisions.

Published Papers (2 papers)

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23 pages, 11785 KiB  
Article
The Synthesis, In Vitro Bio-Evaluation, and In Silico Molecular Docking Studies of Pyrazoline–Thiazole Hybrid Analogues as Promising Anti-α-Glucosidase and Anti-Urease Agents
by Yousaf Khan, Shoaib Khan, Rafaqat Hussain, Aneela Maalik, Wajid Rehman, Mohamed W. Attwa, Rafia Masood, Hany W. Darwish and Hazem A. Ghabbour
Pharmaceuticals 2023, 16(12), 1650; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16121650 - 25 Nov 2023
Cited by 1 | Viewed by 1110
Abstract
In the present work, a concise library of benzothiazole-derived pyrazoline-based thiazole (1–17) was designed and synthesized by employing a multistep reaction strategy. The newly synthesized compounds were screened for their α-glucosidase and urease inhibitory activities. The scaffolds (1 [...] Read more.
In the present work, a concise library of benzothiazole-derived pyrazoline-based thiazole (1–17) was designed and synthesized by employing a multistep reaction strategy. The newly synthesized compounds were screened for their α-glucosidase and urease inhibitory activities. The scaffolds (1–17) were characterized using a combination of several spectroscopic techniques, including FT-IR, 1H-NMR, 13C-NMR, and EI-MS. The majority of the synthesized compounds demonstrated a notable potency against α-glucosidase and urease enzymes. These analogues disclosed varying degrees of α-glucosidase and urease inhibitory activities, with their IC50 values ranging from 2.50 to 17.50 μM (α-glucosidase) and 14.30 to 41.50 (urease). Compounds 6, 7, 14, and 12, with IC50 values of 2.50, 3.20, 3.40, and 3.50 μM as compared to standard acarbose (IC50 = 5.30 µM), while the same compounds showed 14.30, 19.20, 21.80, and 22.30 comparable with thiourea (IC50 = 31.40 μM), respectively, showed excellent inhibitory activity. The structure−activity relationship revealed that the size and electron-donating or electron-withdrawing effects of substituents influenced the enzymatic activities such as α-glucosidase and urease. Compound 6 was a dual potent inhibitor against α-glucosidase and urease due to the presence of -CF3 electron-withdrawing functionality on the phenyl ring. To the best of our knowledge, these synthetic compounds were found to be the most potent dual inhibitors of α-glucosidase and urease with minimum IC50 values. Moreover, in silico studies on most active compounds, i.e., 6, 7, 14, and 12, were also performed to understand the binding interaction of most active compounds with active sites of α-glucosidase and urease enzymes. Full article
(This article belongs to the Special Issue Pyrazole and Thiazole Derivatives in Medicinal Chemistry)
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17 pages, 1781 KiB  
Article
2-Substituted-3-(5-Substituted-1,3,4-oxadiazol/thiadiazol-2-yl) Thiazolidin-4-one Derivatives: Synthesis, Anticancer, Antimicrobial, and Antioxidant Potential
by Davinder Kumar, Navidha Aggarwal, Harsh Kumar, Garima Kapoor, Aakash Deep, Shabana Bibi, Aastha Sharma, Hitesh Chopra, Rakesh Kumar Marwaha, Abdulrahman Alshammari, Metab Alharbi and Abdul Hayee
Pharmaceuticals 2023, 16(6), 805; https://0-doi-org.brum.beds.ac.uk/10.3390/ph16060805 - 29 May 2023
Cited by 1 | Viewed by 1406
Abstract
In this innovative research, a novel series of thiazolidin-4-one analogues having a 1,3,4-oxadiazole/thiadiazole moiety were derived and the structures of all the newly obtained molecules were established using different physicochemical and analytical means (1H-NMR, FTIR, mass spectra, and elemental analyses). The [...] Read more.
In this innovative research, a novel series of thiazolidin-4-one analogues having a 1,3,4-oxadiazole/thiadiazole moiety were derived and the structures of all the newly obtained molecules were established using different physicochemical and analytical means (1H-NMR, FTIR, mass spectra, and elemental analyses). The synthesized molecules were then investigated for their antiproliferative, antimicrobial, and antioxidant potential. The cytotoxicity screening studies revealed that analogues D-1, D-6, D-15, and D-16 possessed comparable efficacy, within the IC50 range (1 to 7 μM), when taking doxorubicin as a reference drug (IC50 = 0.5 μM). The antimicrobial activity was assessed using different Gram-(+) and Gram-(−) bacterial and fungal strains and the results revealed that molecules D-2, D-4, D-6, D-19, and D-20 possessed potent activity against selective strains of microbes with MIC ranges of 3.58 to 8.74 µM. The antioxidant evaluation was performed using the DPPH assay and the screening results revealed that analogue D-16 was the most potent derivative (IC50 = 22.3 µM) when compared with the positive control, ascorbic acid (IC50 = 111.6 µM). Structure–activity relationship (SAR) studies of the synthesized novel derivatives revealed that para-substituted halogen and hydroxy derivatives have remarkable potential against the MCF-7 cancer cell line and antioxidant potential. Similarly, electron-withdrawing groups (Cl/NO2) and -donating groups at the para position possess moderate to promising antimicrobial potential. Full article
(This article belongs to the Special Issue Pyrazole and Thiazole Derivatives in Medicinal Chemistry)
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