2017 MMCS 2017 - 44 articles
Barcelona, Spain | 8 September 2017
Issue Editor: Diego Muñoz-Torrero, University of Barcelona, Spain
Libraries of compounds containing heteroaromatic rings and other nitrogen heterocycles were [...]
The Medicinal Chemistry section of the MDPI journal Molecules organized, for the first time, the [...]
It has recently been demonstrated, from a number of antimalarial and antituberculosis drug discovery programmes, that phenotypic whole cell screening can uncover cell permeable and active drug leads with potentially novel modes of action. In this re...
The rapid increase of multiple drug resistant bacteria and fungi poses a serious threat to society. [...]
The development of nifurtimox-eflornithine combination therapy (NECT) has been a major and emboldening advance towards more effective and simple medications in the field of neglected tropical diseases (NTD) caused by Trypanosomatids. [...]
Topoisomerase inhibitors initiate the cell killing process by either stabilizing or increasing the amount of the covalent complex formed between the enzyme and cleaved DNA. [...]
Tuberculosis (TB) is the biggest global killer in history. One of the main objectives for fighting TB is to find a shorter treatment and also to target multidrug-resistant (MDR) and extensively drug-resistant XDR strains. [...]
Antibiotic resistance is a daunting challenge for public health systems worldwide. [...]
Reverse transcriptase (RT), the key enzyme in the HIV life cycle of HIV, is one of the main targets for the antiretroviral chemotherapy. [...]
Tuberculosis (TB) remains a major global health problem. [...]
Nitric oxide (NO) therapy is the newest approach to the treatment of socially important diseases all over the world. [...]
New, safe, well tolerated, and versatile anti-trichomonal agents for oral and topical use are needed to combat spreading resistance of Trichomonas vaginalis to metronidazole (MTZ). [...]
We disclose a reaction discovery approach, based on novel multicomponent reactions (MCRs) upon heterocyclic substrates, especially azines, that yields a variety of scaffolds amenable to straightforward diversification. [...]
The efficacy of some of the available antiretroviral drugs is very limited against HIV-2 and, most importantly, none of the current drugs effectively prevents entry into the cells. [...]
Libraries of compounds containing unnatural amino acids or amino acid analogues were prepared from inexpensive substrates using sustainable processes [1–3]. [...]
Antimicrobial peptides (AMPs) have been used by animals and plants for millions of years for defence against pathogens, and present important advantages as potential drugs, such as a broad spectrum of activity, no induction of resistances, and synerg...
Antibiotic resistance which was expedited by the use of antimicrobial drugs has been a significant global challenge for public health [1]. [...]
Edelfosine (ET-18-OCH3) is an alkylphospholipid with an analogous structure to miltefosine. Both molecules are active against kinetoplastids (Leishmania spp., Trypanosoma cruzi and Trypanosoma brucei). [...]
The incidence of infection from opportunistic and pathogenic fungi has continued to rise in recent years. [...]
The rate of invasive fungal infections has increased since the 1980s, particularly in the vast populace of immunocompromised patients as well as those hospitalized with serious underlying disease [1]. [...]
Lanosterol 14α-demethylase (CYP51) is an essential enzyme in the fungal life cycle and also an important target for antifungal drug development. Selective inhibition of the enzyme would cause depletion of ergosterol and accumulation of lanosterol and...
During the last few years, there has been an increased awareness of morbidity and mortality related to invasive and systemic fungal disease because of resistant fungi and immunocompromised infections, for instance, AIDS. [...]
The azole pharmacophore is still regarded as a viable lead structure for the synthesis of more effective antifungal agents [1–3]. [...]
Protozoan infections (Plasmodium spp., Leishmania spp., and Trypanosoma spp.) remain one of the most pressing global health concerns, affecting billions of people and producing unsustainable economic burdens [1]. [...]
Molecules that block virus entry by interfering with the actions of viral fusion proteins are of primary concern in the search for antiviral drugs. [...]
The present study is focused on the chemometric QSAR analysis of antifungal and antibacterial activity of novel 2-morpholinoquinoline analogs and their molecular structure described by in silico molecular descriptors. [...]
Malaria is a devastating disease affecting millions of people each year yet, surprisingly, apart from the Artemisinin Combination Therapies (ACTs) there are relatively few effective treatments for Plasmodium falciparum and only one complete treatment...
Malaria is a mosquito-borne infectious disease caused by parasitic protozoans of the genus Plasmodium. [...]
Chagas disease (CD) or American trypanosomiasis is a widespread parasitic disease throughout the world. [...]
Chagas disease and Leishmaniasis are trypanosomatid diseases considered as neglected tropical diseases by the WHO. [...]
Chagas disease (CD) is a neglected tropical disease caused by the parasite Trypanosoma cruzi [1]. [...]
Benzimidazole derivatives have a great deal of interest in terms of antimicrobial therapy. [...]
Antimicrobial peptides (AMPs) have been used on animals for millions of years. [...]
Menaquinone is one of the essential components of the electron transport chain in many pathogens and consequently enzymes in its biosynthesis pathway are potential drug targets for the development of novel antibacterial agents. [...]
The emergence of multidrug resistant bacteria has a direct impact on global public health due to the reduced potency of existing antibiotics against pathogens [1]. [...]
We have been preparing new dipeptidyl inhibitors against parasitic cysteine proteases cruzain (related to Chagas disease) and rhodesain (related to Sleeping Sickness disease), and against human cathepsins. [...]
Modern advances in Chemical Biology include the improvement of screening methods, the introduction of bioinformatic methods to unravel biological pathways, and the generation of highquality chemical libraries. [...]
Reverse transcriptase (RT), the key enzyme in the HIV life cycle of HIV, is one of the main targets for the antiretroviral chemotherapy. [...]
There currently exists a dire need for safe and inexpensive new antimalarial drugs, which are effective against multiple life cycle stages of Plasmodium falciparum, and act through mechanisms that differ from those of the available drugs to prevent d...
Chagas disease is caused by the insect-transmitted protozoan Trypanosoma cruzi, and is the most important parasitic infection in Latin America. [...]
Benznidazole and nifurtimox, the currently available drugs for the specific treatment of Chagas disease, show limited effectiveness and high toxicity that prompt the identification of therapeutic alternatives. [...]
Similarities between parasites and cancer have prompted parasitologists to take advantage of several approaches enabled by cancer research to identify antiparasitic agents [1]. [...]
Antimicrobial peptides offer a new class of therapeutic agents to which bacteria may not be able to develop genetic resistance, since they act on the lipid component of the cell membranes [1]. [...]
The increasing prevalence of antibacterial resistance is a worrying health concern. [...]
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