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

The discovery of new small molecule-based inhibitors is an attractive field in medicinal chemistry. Structurally diversified heterocyclic derivatives have been investigated to combat multi-drug resistant bacterial infections and they offers several mechanism of action. Methicillin-resistant Staphylococcus aureus (MRSA) is becoming more and more deadly to humans because of its simple method of transmission, quick development of antibiotic resistance, and ability to cause hard-to-treat skin and filmy diseases. The sulfur (SVI) particularly sulfonyl and sulfonamide based heterocyclic moieties, have found to be good anti-MRSA agents. The development of new nontoxic, economical and highly active sulfur (SVI) containing derivatives has become hot research topics in drug discovery research. Presently, more than 150 FDA approved Sulfur (SVI)-based drugs are available in the market, and they are widely used to treat various types of diseases with different therapeutic potential. The present collective data provides the latest advancements in Sulfur (SVI)-hybrid compounds as antibacterial agents against MRSA. It also examines the outcomes of in-vitro and in-vivo investigations, exploring potential mechanisms of action and offering alternative perspectives on the structure-activity relationship (SAR). Sulfur (SVI)-hybrids exhibits synergistic effects with existing drugs to provide antibacterial action against MRSA.

Fluorinated azoles as effective weapons in fight against methicillin-resistance staphylococcus aureus (MRSA) and its SAR studies.

The rapid spread of Methicillin-resistant Staphylococcus aureus (MRSA) and its difficult-to-treat skin and filmsy diseases are making MRSA a threat to human life. The most dangerous feature is the fast emergence of MRSA resistance to all recognized antibiotics, including vancomycin. The creation of novel, effective, and non-toxic drug candidates to combat MRSA isolates is urgently required. Fluorine containing small molecules have taken a centre stage in the field of drug development. Over the last 50 years, there have been a growing number of fluorinated compounds that have been approved since the clinical usage of fluorinated corticosteroids in the 1950 s and fluoroquinolones in the 1980 s. Due to its advantages in terms of potency and ADME (absorption, distribution, metabolism, and excretion), fluoro-pharmaceuticals have been regarded as a potent and useful tool in the rational drug design method. The flexible bioactive fluorinated azoles are ideal candidates for the development of new antibiotics. This review summarizes the decade developments of fluorinated azole derivatives with a wide antibacterial activity against diverged MRSA strains. In specific, we correlated the efficacy of structurally varied fluorinated azole analogues including thiazole, benzimidazole, oxadiazole and pyrazole against MRSA and discussed different angles of structure-activity relationship (SAR).

A key review on oxadiazole analogs as potential methicillin-resistant Staphylococcus aureus (MRSA) activity: Structure-activity relationship studies.

Methicillin-resistant Staphylococcus aureus (MRSA) is becoming dangerous to human beings due to easy transmission mode and leading to the difficult-to-treat situation. The rapid resistance development of MRSA to many approved antibiotics is of major concern. There is a lot of scope to develop novel, efficient, specific, and nontoxic drug candidates to fight against MRSA isolates. The interesting molecular structure and adaptable feature of oxadiazole moiety which are bioisosteres of esters and amides, and these functional groups show improved resistance to esterases mediated hydrolytic cleavage, attracting researchers to develop required novel antibiotics based on oxadiazole core. This review summarizes the developments of oxadiazole-containing derivatives as potent antibacterial agents against multidrug-resistant MRSA strains and discussing the structure-activity relationship (SAR) in various directions. The current survey is the highlight of the present scenario of oxadiazole hybrids on MRSA studies, covering articles published from 2011 to 2020. This collective information may become a good platform to plan and develop new oxadiazole-based small molecule growth inhibitors of MRSA with minimal side effects.

Catalytic pyrolysis of ulva lactuca macroalgae: Effects of mono and bimetallic catalysts and reaction parameters on bio-oil up-gradation.

Catalytic pyrolysis of ulva lactuca (UL) macroalgae was studied over a series of ZrO2 supported metal such as Co, Ni and Co-Ni metal catalysts at temperature range of 300-500 °C. Highest bio-oil yield (47.8 wt%) was found with Co-Ni/ZrO2 (10 wt%) catalyst while non-catalytic yielded 42.5 wt% bio-oil. Moreover with increases the metal amount to 15 wt%, the bio-oil yield slightly increased (49.2 wt%). The bio-oil quality significantly improved with using the catalysts compared to the non-catalytic pyrolysis. Catalytic pyrolysis also revealed that introducing Co-Ni into the ZrO2 could result in higher surface area and which increased active sites. Catalytic bio-oils were consisted of mainly long chain hydrocarbon in the range of C6-C16. Moreover, the catalytic bio-oils were showed the higher 'high heating value' (HHV) 38.1 MJ/kg as compare to non-catalytic bio-oils (29.4 MJ/kg). Catalysts have been showed excellent recyclability on bio-oil yield and compounds selectivity.

Pyrazole-based analogs as potential antibacterial agents against methicillin-resistance staphylococcus aureus (MRSA) and its SAR elucidation.

Methicillin-resistant Staphylococcus aureus (MRSA) is becoming lethal to humanity due to easy transmission and difficult-to-treat skin and flimsy diseases. The most threatening aspect is the rapid resistance development of MRSA to any approved antibiotics, including vancomycin. The development of new, efficient, and nontoxic drug candidate to fight against MRSA isolates is the need of the hour. The intriguing molecular structure and versatile bioactive pyrazole core attracting to development required novel antibiotics. This review presents the decade developments of pyrazole-containing derivatives with a broad antibacterial movement against diverged bacterial strains. In specific, we correlated the efficacy of structurally diversified pyrazole analogs against MRSA and discussed different angles of structure-activity relationship (SAR). The current survey highlights pyrazole hybrids' present scenario on MRSA studies, covering articles published from 2011 to 2020. This collective information may become an excellent platform to plan and develop new pyrazole-based small MRSA growth inhibitors with minimal side effects.

Anti-tuberculosis activity and its structure-activity relationship (SAR) studies of oxadiazole derivatives: A key review.

With the increasing number of cases of inactive and drug-resistance tuberculosis, there is an urgent need to develop new potent molecules set for fighting this brutal disease. Medicinal chemistry concerns the discovery, the development, the identification, and the interpretation of the mode of action of biologically active compounds at the molecular level. Molecules bearing oxadiazoles are one such class that could be considered to satisfy this need. Oxadiazole regioisomers have been investigated in drug discovery programs for their capacity to go about as powerful linkers and as pharmacophoric highlights. Oxadiazoles can go about as bioisosteric substitutions for the hydrazide moiety which can be found in first-line anti-TB drugs, and some have been likewise answered to cooperate with more current anti-TB targets. This present review summarizes the current innovations of oxadiazole-based derivatives with potential antituberculosis activity and bacteria discussing various aspects of structure-activity relationship (SAR).

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

The rise of drug-resistance has made the deserted clinical requirement to improve of new classes of antibiotics agents. The development of antibacterial agents with the novel method of activity stays a high need worldwide. The treatment of bacterial infections remains a test in light of developing irresistible sicknesses and the expanding number of multidrug-resistance microbial pathogens. Therefore, there is a need for powerful activities to think of new successful therapeutic agents, and it is dire to find novel synthetic analogs against bacterial targets. The improvements of new, less harmful, minimum side-effort, and extremely dynamic sulfonyl or sulfonamide-bearing analogs are hot research topics in medicinal chemistry. This present review summarizes the current innovations of sulfonyl or sulfonamide-based derivatives with potential antibacterial activities against various Gram-positive and Gram-negative bacterial strains and discussing its various aspects of structure-activity relationship (SAR).