Pharmaceutical and medicinal significance of sulfur (SVI)-Containing motifs for drug discovery: A critical review

Review: 294 refs.

A comprehensive review in current developments of benzothiazole-based molecules in medicinal chemistry.

Pharmaceutical significance of azepane based motifs for drug discovery: A critical review

Carbonic anhydrase: chemistry, physiology, and inhibition.

Antibacterial activities of sulfonyl or sulfonamide containing heterocyclic derivatives and its structure-activity relationships (SAR) studies: A critical review

Welcome to the first issue of 2012 of Cardiovascular & Hematological Agents in Medicinal Chemistry. I hope everyone has had a wonderful holiday season and I want to wish everyone a wonderful New Year. As you are aware, our journal aims to cover the latest and outstanding developments in medicinal chemistry, rational drug design for the discovery of novel cardiovascular and hematological agents and discusses such therapies in clinical practice. Each issue contains a series of timely in-depth reviews, original research articles and drug clinical trial studies written by leaders in the field covering a range of current topics in cardiovascular and hematological sciences. I feel that Cardiovascular & Hematological Agents in Medicinal Chemistry is an essential journal for every medicinal chemist, clinician and healthcare provider who wishes to be kept informed and up-to-date with the latest and most important developments in cardiovascular and hematological drug discovery and their clinical uses. In the coming issues of the journal, we will discuss several important topics pertinent to medicinal chemists and clinicians in the cardiovascular and hematology field such as evidence for the use of adrenaline in the treatment of neonatal hypotension, use of selective Inhibitors of plasma kallikrein, potential cardiotoxic effect of clozapine, novel antiplatelets agents in cardiovascular medicine among others. Cardiovascular medicine and hematology are both very dynamic fields with rapid advances and we will continue to strive to keep you up to date on new advances and therapies. I would also take this opportunity to invite our readers and experts to contribute hot topics and general articles in their respective fields to our journal. The journal is in its tenth successful year of publication, and is indexed by all major indexing media including Chemical Abstracts, EMBASE/Excerpta Medica, Index Medicus/MEDLINE, BIOSIS Previews, BIOSIS Reviews Reports and Meetings, Google, Google Scholar, Genamics JournalSeek, MediaFinder®-Standard Periodical Directory and Scopus and remains a valuable resource for chemists and clinicians.

since the 1970s, over 200 studies with acetazolamide have shown it safe and 60–80% effective in acute mountain sickness (AMS). Despite much investigation, our understanding of its action in AMS remains incomplete and more complicated than generally taught. This should come as no surprise

Sulfur (SⅥ)-containing heterocyclic hybrids as antibacterial agents against methicillin-resistant Staphylococcus aureus (MRSA) and its SAR

Epilepsy is one of the common diseases seriously threatening life and health of human. More than 50 million people are suffering from this condition and anticonvulsant agents are the main treatment. However, side effects and intolerance, and a lack of efficacy limit the application of the current anticonvulsant agents. The search for new anticonvulsant agents with higher efficacy and lower toxicity continues to be the focus and task in medicinal chemistry. Numbers of triazole derivatives as clinical drugs or candidates have been frequently employed for the treatment of various types of diseases, which have proved the importance of this heterocyclic nucleus in drug design and discovery. Recently many endeavours were made to involve the triazole into the anticonvulsants design, which have brought lots of active compounds. This work is an attempt to systematically review the research of triazole derivatives in the design and development of anticonvulsant agents during the past two decades.

Generics and Biosimilars: Barriers and Opportunities

PROTACs is an emerging technique that addresses the disease causing proteins by targeting protein degradation. PROTACs molecules are bifunctional small molecules that simultaneously bind to the protein of interest (POIs) and an E3 ligase followed by ubiquitination and degradation of the protein of interest by the proteasome. PROTACs technology offers many advantages over classical inhibition such as PROTACs molecules can target intracellular proteins regardless of their function and have good tissue distribution. They are capable to target mutated and overexpressed proteins, thus potent molecules with the high degradation selectivity can be designed. Moreover, PROTACs molecules can target the undruggable proteome which makes up almost 85% of human proteins. Several PROTACs-based compounds have exhibited high therapeutic potency and some of them are currently under clinical trials. Current article gives a comprehensive overview of the current development of PROTACs-based anticancer compounds along with the structure-activity relationship of the reported molecules. The development of PROTACs-based compounds and related research regarding medicinal chemistry is one of the most active and hot topics for research. It is believed that the current review article can be helpful to understand the logical design of more efficacious PROTACs-based molecules with less toxicity and more selectivity.

""Abstract: Lactoferrin is an iron binding protein belonging to the transferrin superfamily. Its main function is the protection. towards infections. In a previous article (Leboffe et al., Anti-Infective Agents in Medicinal Chemistry, 2009), we. have reviewed the antifungal and antiparasitic activity of lactoferrin. In the present updated review we focused the attention. on the newly discovered antifungal properties of lactoferrin and its derived peptides in clinical, diagnostic and biotechnological. applications. In particular, we discuss the new findings on diagnosis of fungal infections utilizing Lf and on. emerging pharmacological treatments exploiting combined effects of Lf and classical antifungal drugs. We also reported. recent studies on the use of Lf antifungal activity for food and beverage preservation. These new properties have found. applications both “in vitro” and “in vivo”, opening new scenarios about the use of this protein as an antinfective agent. both in translational medicine and biotechnology""

Imidazole ring is an important five-membered aromatic heterocycle widely present in natural products and synthetic molecules. The unique structural feature of imidazole ring with desirable electron-rich characteristic is beneficial for imidazole derivatives to readily bind with a variety of enzymes and receptors in biological systems through diverse weak interactions, thereby exhibiting broad bioactivities. The related research and developments of imidazole-based medicinal chemistry have become a rapidly developing and increasingly active topic. Particularly, numerous imidazole-based compounds as clinical drugs have been extensively used in the clinic to treat various types of diseases with high therapeutic potency, which have shown the enormous development value. This work systematically gives a comprehensive review in current developments of imidazole-based compounds in the whole range of medicinal chemistry as anticancer, antifungal, antibacterial, antitubercular, anti-inflammatory, antineuropathic, antihypertensive, antihistaminic, antiparasitic, antiobesity, antiviral, and other medicinal agents, together with their potential applications in diagnostics and pathology. It is hoped that this review will be helpful for new thoughts in the quest for rational designs of more active and less toxic imidazole-based medicinal drugs, as well as more effective diagnostic agents and pathologic probes.

Two exemplary contributions of organometallics in medicinal chemistry, ferroquine and ferrocifen, which exhibit excellent anti-plasmodial and anti-cancer activities, respectively, have opened a new field called medicinal organometallic chemistry. This field has been gaining significant interest due to the recent upsurge in ferrocene-linked organic frameworks with promising biological potential. The success of ferrocene is due to the sustained efforts by organic medicinal chemists and its inherent stability in air, heat and light, low toxicity, low cost and reversible redox properties. The replacement of the aryl/heteroaryl core with a ferrocene nucleus in organic molecules imparts a significant change not only in their molecular properties, such as solubility and hydro-/lipophilicity, but also improves the activities of bioactive compounds. Ferrocifen (ferrocene analogue of hydroxytamoxifen) possesses the remarkable feature of being anti-proliferative against both the MCF-7 (hormone dependent) and MDA-MB-231 (hormone independent) breast cancer cell lines. Accordingly, this review article is aimed at updating researchers on the recent developments (2014-18) on the synthesis and evaluation of ferrocene-containing bio-active pharmacophores with emphasis on their structure-activity relationship and mechanism of action.

Coumarin compounds represent an important type of naturally occurring and synthetic oxygen-containing heterocycles with typical benzopyrone framework. This type of special benzopyrone structure enables its derivatives readily interact with a diversity of enzymes and receptors in organisms through weak bond interactions, thereby exhibit wide potentiality as medicinal drugs. So far, some coumarin-based drugs such as anticoagulant and antineurodegenerative agents have been extensively used in clinic. Coumarin-containing supramolecular medicinal agents as a new increasing expansion of supramolecular chemistry in pharmaceutical science have also been actively investigated in recent years. Coumarin-derived artificial ion receptors, fluorescent probes and biological stains are growing quickly and have a variety of potential applications in monitoring timely enzyme activity, complex biological events as well as accurate pharmacological and pharmacokinetic properties. This review provides a systematic summary and insight of the whole range of medicinal chemistry in the current developments of coumarin compounds as anticoagulant, antineurodegenerative, anticancer, antioxidative, antibacterial, antifungal, antiviral, antiparasitic, antiinflammatory and analgesic, antidiabetic, antidepressive and other bioactive agents as well as supramolecular medicinal drugs, diagnostic agents and pathologic probes, and biological stains. Some rational design strategies, structure-activity relationships and action mechanisms are discussed. The perspectives of the future development of coumarinbased medicinal chemistry are also presented.