The discovery and utilization of novel metabolites from natural sources are gaining momentum
in the present era. The drug discovery programs have witnessed a remarkable shift from conventional
medicines to exploiting natural products and their “value addition”, for treating lifethreatening
diseases. The global outbreak of life-threatening diseases namely Ebola,
SARS,including infections of the bloodstream (bacteremia), heart valves (endocarditis), lungs
(pneumonia), and brain (meningitis) and AIDS calls for a more targeted approach to effectively
combat the emerging diseases.
In the present scenario, natural products and their extracts are being explored extensively for
the treatment of various life threatening diseases. In this thematic issue, several review articles contributed by the scientist
and researchers in the different areas of medicinal chemistry, synthetic chemistry, new emerging multi-drug targets were
collected.
This issue begins with a review article on the “Chemistry and Pharmacology of Natural Catechins from Camellia sinensis
as anti-MRSA agents” by Gaur et al. and focuses on the spread of MRSA strains is of great concern because of limited treatment
options for staphylococcal infections, since these strains are resistant to the entire class of β-lactam antibiotics. In addition,
MRSA exhibits resistance to other classes of antimicrobial agents such as fluoroquinolones, cephalosporins, aminoglycosides,
macrolide and even glycopeptides (vancomycin and teicoplanine), leading to the emergence of resistant strains such as
glycopeptide intermediate (GISA) and resistant strain (GRSA) of S. aureus. In this review, chemical constituents responsible
for the anti-MRSA activity of tea are explored [1].
The next article of this issue is a review article on the “Recent Advancements in the Synthesis and Chemistry of Benzofused
Nitrogen- and Oxygen-based Bioactive Heterocycles” by Sharma et al. which focuses on medicinal importance of these
bioactive benzo-fused heterocycles; special attention has been given to their synthesis as well as medicinal/pharmaceutical
properties in detail [2].
“Trends in pharmaceutical design of Endophytes as anti-infective,” by Tiwari et al., is the third article in this issue. The
review focused on the meta-analysis of bioactive metabolite production from endophytes, extensively discussing the bioprospection
of natural products for pharmaceutical applications. In light of the emerging importance of endophytes as antiinfective
agents, an exploration of the pharmaceutical design of novel chemical entities and analogues has enabled efficient
and cost-effective drug discovery programs. However, bottlenecks in endophytic biology and research requires a better understanding
of endophytic dynamics and mechanism of bioactive metabolite production towards a sustainable drug discovery
program [3].
The last article of this issue is also research article on “Recent development of tetrahydro-quinoline/isoquinoline based
compounds as anticancer agents” by Yadav et al. The article reported the synthesis of potent tetrahydroquinoline/isoquinoline
molecules of the last 10 years with their anticancer properties in various cancer cell lines and stated their half-maximal inhibitory
concentration (IC50). In addition, we also considered the discussion of molecular docking and structural activity relationship
wherever provided to understand the possible mode of activity an target involved and structural features responsible for
the better activity, so the reader can directly find detail for designing new anticancer agents. [4].
Finally I would like to thank all authors who contributed to this issue, titled “Recent advances on small molecule medicinal
chemistry to treat human diseases”.
A Review of Study Designs and Outcomes of Phase I Clinical Studies of Nanoparticle Agents Compared with Small-Molecule Anticancer Agents