β-lactam antibiotics are considered the safest bactericides, and upon wide clinical use of benzyl penicillin G in 1945, outbreaks of resistance came out. The frequent semi-synthetic strategies revealed β-lactam generations that are of broad-spectrum activity. The new agents as well as their concomitant use with known inhibitors of β-lactamases potentiate their effectiveness versus higher numbers of resistant pathogens. However, the extremely resistant pathogens are still representing a burden. Efforts had been continued to find more inhibitors of β-lactamases to combine with β-lactams to provide good management of infections by extremely resistant microbes. The purpose of this work is to overview the conventional and the recently introduced β-lactamases in clinical applications, as well as some reported effective inhibitors of β-lactamases. The review pinpoints the inhibitors that can be mixed and/or merged with the beta-lactam antibiotics to effectively treat the microbial infections producing resistant-β-lactamases. ClogP for these drugs and candidate inhibitors is introduced as suggestions to open a door for developers to admix derivatives with suitable pharmacokinetics.
Pesticides have become an essential component of Indian agriculture. Increasing concentrations of these chemicals per hectare have led to many environmental and health risks. Nanotechnology, a new era of science, has led to the invention of nanopesticides, which have both advantages and disadvantages. Many formulations, such as nanoemulsions, nanosuspensions, nanoencapsulated and nanoparticles, have been produced by the research community. The chemicals' smaller size allows them to more effectively diffuse across the insect's and host's surfaces, providing a better effect than conventional pesticides. Nanopesticide significantly reduces the dose of chemical pesticides and hence is a promising scientific development that offers many benefits, including increased efficacy, durability, and reduced amount of active ingredient (AI) used to protect crops from diseases, insects, and weeds.
4-Aminoquinazoline analogs have been identified as a new class of cancer chemotherapeutic agents with significant therapeutic efficacy against solid tumors. They are potent and highly selective inhibitors of tyrosine kinase (TK) and epidermal growth factor receptor (EGFR). Till date various 4-aminoquinazoline analogs have been synthesized and evaluated for anticancer activity. This review is an attempt to compile the medicinal chemistry of various synthesized 4-aminoquinazoline analogs. Keywords: 4-Aminoquinazoline, antitumor, apoptosis, cytotoxic, epidermal growth factor receptor, tyrosine kinase.
Abstract: Chromenes are an important class of oxygen-containing heterocyclic compounds with intriguing biological activity, a simple structure with mild adverse effects. Chromenes are abundantly found in nature in the form of alkaloids, tocopherols, flavone, and anthocyanins. The Chromene nucleus is an important moiety for the discovery of new drug candidates. Chromene derivatives have shown various pharmacological activities like antiviral, anticancer, anti-inflammatory, antitumour, antimicrobial, antiproliferative, anticholinesterase, EPR-1 (Effector cell Protease Receptor-1) antagonist and MAO (Mono-Amine Oxidase) inhibitors. In SAR (Structure Activity Relationship) studies with chromene nucleus, it was found that 4-aryl moiety, 3-cyano group, and 2-amino group are essential for the cytotoxic activity. Substitution at the 7th position with electron donating group enhances the pharmacological activity whereas the electron withdrawing group decreases the pharmacological activity. Structural modifications at the chromene ring, middle aliphatic portion, and terminal aromatic ring yielded more potential 5-HT1A (5-Hydroxytryptamine 1A) receptor affinity and antidiabetic activity. Chromenes with cyclic secondary amine and 4-hydroxy phenyl substituents yielded potent antimicrobial compounds. This review summarizes the importance of chromenes in rational drug design and the development of novel molecules with a variety of pharmacological activities.
Abstract: In response to the escalating issue of antibiotic-resistant bacteria adhering to and thriving on medical equipment, scientists are pioneering innovative "intelligent" materials and coatings. These advancements entail the targeted release of antimicrobial substances, specifically activated when bacteria are detected. The next section discusses three revolutionary substances: hydrogels, nanoparticles, and thin films. Furthermore, intelligent antibacterial materials are divided into 2 groups based on the triggering source: those that react to biological stimuli and those that react to non-biological ones, like temperature and electric cues associated with bacterial presence, such as pH shifts or bacterial enzyme discharge. Moreover, because of their simple construction technique, outstanding biocompatibility, and robust antibacterial characteristics derived from polyphenols and metal ions, metallic-polyphenolic nanoparticles (MPNs) have obtained substantial interest in tackling antimicrobial infections. This article presents an introduction to several MPN-centered biomaterials (like nanoparticles, coatings, capsules, and hydrogels) and highlights the latest advancements in research in its applications for addressing microbial threats in the field of biomedicine. Furthermore, the usage of smart materials is classified based on their application domains, encompassing medical implants, waste reduction, and nano-engineered systems.
Trichosanthes dioica R. (T. dioica) is an easily available common plant. The plant belongs to family Cucurbitaceae which has given us many important medicinal plants like Momordica charantia, Citrullus colocynthis etc. from which important pharmacological activities and markers like charantin and Cucurbitacin have been reported and isolated. In the present study T. dioica was evaluated for anti-inflammatory activity using carrageenan induced acute inflammation model in rats. It was concluded that leaves of T. dioica possess moderate anti-inflammatory activity.
Trichosanthes dioica seeds are mentioned in various traditional texts as a drug used for vermicidal anthelmintic, insecticidal, sedative, diuretic, demulcent, and expectorant purpose ethnopharmacologically. The studies were taken up to evaluate pharmacognostic, physicochemical and phytochemical standard for Trichosanthes dioica seeds. The objective of present study is to evaluate the morphological, microscopical, phytochemical and physicochemical properties of various bioactive compounds present in Trichosanthes dioica seeds. Preliminary phytochemical screening was done and HPTLC studies were carried out. CAMAG HPTLC system equipped with Linomat V applicator, TLC scanner, and WIN CATS-4 software were used. The microscopical studies of T. dioica seeds have showed mucilaginous epidermis made up of long thin trichomes, Innermost layer of parenchyma cells and sclerotic endodermal layer. Testa is 17-23 cells thick on the sides on the seeds. Exotesta: a layer shortly columnar pulpy cells, much elongate on the sides of micropyle thin walled but with fine fibrillar thickenings (not lignified) on the radial and inner wall, the outer wall thickened and slightly lignified, first filled with starch grains. Physico-chemical studies of T. dioica seeds have set the some standard i.e. Ether soluble extractive value 16.15%w/w, alcohol soluble extractive value 10.11% w/w, water soluble extractive value 9.22% w/w, Total Ash value 6.21 w/w, acid insoluble ash value 1.32% w/w, water soluble ash value 4.29% and loss on drying 24.33% w/w etc. were found out. Preliminary phytochemical screening was done then TLC and HPTLC studies were carried out. All the findings will be useful towards establishing pharmacognostic standards on identification, purity, quality and classification of the plant, which is gaining relevance in plant drug research for the identification and preparation of monograph of plant.
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