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Heterocycles in Drugs and Drug Discovery
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Heterocycles in Drugs and Drug Discovery

A special issue of Molecules (ISSN 1420-3049). This special issue belongs to the section "Medicinal Chemistry".

Deadline for manuscript submissions: closed (30 November 2022) | Viewed by 4897

Special Issue Editor

Prof. Dr. Julio Álvarez-Buílla

E-Mail Website
Guest Editor
Department of Organic Chemistry and Inorganic Chemistry, University of Alcalá, 28871 Alcala de Henares, Madrid, Spain
Interests: new heterocyclic drugs; heterocyclic moieties used as prodrugs; new heterocyclic PET reagents

Special Issue Information

Dear Colleagues,

Heterocycles are moieties used often as part of active pharmaceutical ingredients (APIs). The reasons for this are varied: heterocyclic fragments add to the API molecule a variety of functionalities, heteroatoms, aromatic or nonaromatic rings, and differences in basicity or hydrophobicity, all properties which can be easily modulated by the correct functionalization of every heterocyclic ring.

text

Scheme 1. Heterocyclic and nonheterocyclic APIs launched in the international market.

As shown in Scheme 1, which lists most of the APIs launched in the international market since 1994, more than 70% of the products bear heterocycles in their molecules. Biotech drugs have been counted as nonheterocyclic. The present Special Issue will be devoted to this field, focusing on how heterocycles can be used to develop new APIs. Original research (communications, full papers, and reviews) that discusses drug development of heterocyclic drugs would therefore be welcome.

Prof. Julio Álvarez-Buílla
Guest Editor

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. Molecules is an international peer-reviewed open access semimonthly 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 2700 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.

Keywords

  • medicinal chemistry
  • heterocyclic chemistry
  • drug design
  • heterocycles
  • π-excedent heterocycles
  • π-deficient heterocycles

Published Papers (2 papers)

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Research

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12 pages, 1758 KiB  
Article
Antifungal Activity of Amphiphilic Perylene Bisimides
by Vicky C. Roa-Linares, Ana C. Mesa-Arango, Ramón J. Zaragozá and Miguel A. González-Cardenete
Molecules 2022, 27(20), 6890; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules27206890 - 14 Oct 2022
Cited by 2 | Viewed by 1060
Abstract
Perylene-based compounds, either naturally occurring or synthetic, have shown interesting biological activities. In this study, we report on the broad-spectrum antifungal properties of two lead amphiphilic perylene bisimides, compounds 4 and 5, which were synthesized from perylene-3,4,9,10-tetracarboxylic dianhydride by condensation with spermine [...] Read more.
Perylene-based compounds, either naturally occurring or synthetic, have shown interesting biological activities. In this study, we report on the broad-spectrum antifungal properties of two lead amphiphilic perylene bisimides, compounds 4 and 5, which were synthesized from perylene-3,4,9,10-tetracarboxylic dianhydride by condensation with spermine and an ammonium salt formation. The antifungal activity was evaluated using a collection of fungal strains and clinical isolates from patients with onychomycosis or sporotrichosis. Both molecules displayed an interesting antifungal profile with MIC values in the range of 2–25 μM, being as active as several reference drugs, even more potent in some particular strains. The ammonium trifluoroacetate salt 5 showed the highest activity with a MIC value of 2.1 μM for all tested Candida spp., two Cryptococcus spp., two Fusarium spp., and one Neoscytalidium spp. strain. Therefore, these amphiphilic molecules with the perylene moiety and cationic ammonium side chains represent important structural features for the development of novel antifungals. Full article
(This article belongs to the Special Issue Heterocycles in Drugs and Drug Discovery)
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Review

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23 pages, 8368 KiB  
Review
Quinazolinones, the Winning Horse in Drug Discovery
by Aishah M. Alsibaee, Hanan M. Al-Yousef and Huda S. Al-Salem
Molecules 2023, 28(3), 978; https://0-doi-org.brum.beds.ac.uk/10.3390/molecules28030978 - 18 Jan 2023
Cited by 21 | Viewed by 3028
Abstract
Quinazolines are nitrogen-containing heterocycles that consist of a benzene ring fused with a pyrimidine ring. Quinazolinones, oxidized quinazolines, are promising compounds with a wide range of biological activities. In the pharmaceutical field, quinazolinones are the building blocks of more than 150 naturally occurring [...] Read more.
Quinazolines are nitrogen-containing heterocycles that consist of a benzene ring fused with a pyrimidine ring. Quinazolinones, oxidized quinazolines, are promising compounds with a wide range of biological activities. In the pharmaceutical field, quinazolinones are the building blocks of more than 150 naturally occurring alkaloids isolated from different plants, microorganisms, and animals. Scientists give a continuous interest in this moiety due to their stability and relatively easy methods for preparation. Their lipophilicity is another reason for this interest as it helps quinazolinones in penetration through the blood–brain barrier which makes them suitable for targeting different central nervous system diseases. Various modifications to the substitutions around the quinazolinone system changed their biological activity significantly due to changes in their physicochemical properties. Structure–activity relationship (SAR) studies of quinazolinone revealed that positions 2, 6, and 8 of the ring systems are significant for different pharmacological activities. In addition, it has been suggested that the addition of different heterocyclic moieties at position 3 could increase activity. In this review, we will highlight the chemical properties of quinazolinones, including their chemical reactions and different methods for their preparation. Moreover, we will try to modify some of the old SAR studies according to their updated biological activities in the last twelve years. Full article
(This article belongs to the Special Issue Heterocycles in Drugs and Drug Discovery)
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