The 2-aminothiazole compounds are medicinally important agents due to their broad spectrum of biological activities. This study aims to design new 2-aminothiazole derivatives, docking, and synthesis via several steps and identified d concerning their The bioactivities of the synthesized compounds were evaluate using physical and spectroscopic techniques. Escherichia , Enterobact aerogenes were screened against five bacterial strains, antimicrobial activities against Candida and two types of fungal strain Pseudomonas aeruginosa, Staphylococcus aureus , Enterococcus faecalis , coli . Cryptococcus neoformans var. grubii and albicans K albicans. C.
Poor drug solubility with the consequent low bioavailability represents one of the main obstacles to the introduction of new drugs into the market. Several approaches were tried to improve drugs poor solubility and low bioavailability, one of these feasible approaches is by using co-crystallization technology which depends on co-crystal formation by joining the drug with another active pharmaceutical former which could alter the parent drug physicochemical properties. This review tries to highlight the main points in co-crystallization technology including co-crystals design, methods of preparation, the different ways of characterizations and diverse cocrystal applications in product development. Co-crystal design could be facilitated by different software programs like Cambridge structure database, which may aid in prediction of the cocrystal production. Various techniques were used in preparation of co-crystal including classical methods (dry grinding, wet grinding and solvent evaporation) and green methods (ultrasonic and microwave-assisted techniques). The characterization of cocrystal is a corner stone in this field. The developed co-crystal could be identified by their structure, thermal behavior and morphology. Different aspects for co-crystal applications in improving solubility, stability, taste, bioavailability and formulation performance of solid dosage forms were discussed. Indeed, co-crystal could improve flowability and compressibility of powder and consequently will help in production of tablet dosage form. Moreover, multi-drugs co-crystals have succeeded in reaching the market with great advantages in reducing the required dose to perform the pharmacological action in a synergistic performance with another pharmacological agent.
This study introduces the know-how of preparing a multiple injection form atropine sulphate solution. An injectable aqueous solution of atropine sulphate at a concentration of 0.1%. was prepared under aseptic conditions in dark glass bottles each containing 50 ml. The preparation was intended for animal use only. It contained 1g atropine sulphate, 9 g sodium chloride as a normal saline, benzyl alcohol 15 ml as a preservative and water for injection up to 1000 ml. The pH of the solution was adjusted to 4.2 (range 3.0-6.5). The preparation of 0.1% atropine sulphate solution was clear colorless solution free from undesired particles. It complied with the requirements for injectable solutions. Further, the preparation was safe when used under laboratory conditions in chicks, rats and donkeys. It was also effective in preventing dichlorvos (an organophosphate insecticide)-induced poisoning in chicks in a manner comparable to a commercial preparation of 0.1% atropine sulphate. In conclusion, the knowhow of a preparation of 0.1% atropine sulphate solution is presented for veterinary use.
The most traditional and popular agents are non-steroidal anti-inflammatory drugs (NSAIDs). However, due to their side effects on different organs. In this review, several compounds created as acetamide derivatives to maintain their anti-inflammatory properties, selective COX-II inhibitors, are discussed. Numerous literature reviews have highlighted the significance of these anti-inflammatory heterocyclic compounds in treatments, taking into consideration the significance of this pharmacological class. Cyclooxygenase-II (COX-II) inhibitors can be used in a wide variety of applications thanks to the prodrug method. It plays a big part in drug development. Many researchers have created different prodrugs using acetamide molecules to adjust pharmacokinetic parameters, enhance organoleptic qualities, or increase chemical properties. A huge quantity of amide derivatives belonging to different classes of compounds exhibit cyclooxygenase-II inhibitors and mainly to treat arthritis, pain, menstrual camps, and colonic polyps, they used for relief of pain, fever, swelling, and tenderness. Finally, the nanoparticles of cyclooxygenase (II) inhibitors were used for improving the efficacy.
Background: 1,3-oxazolidinones are an important class of antibiotics that are recognized with higher activities against Gram-positive bacteria. linezolid, tedizolid phosphate, and radezolid are important examples of this group. Aim: The aim of this review is to study the effect of 1,3-oxazolidinone derivatives as Gram-positive antibacterial agents. Results: There are many methods for preparing the oxazolidinone derivatives. Many patents Three new antibacterial oxazolidinones are linezolid, tedizolid phosphate, and radezolid. They differ in the side chain according to their structure-activity relationship. Conclusion: Study the structure-activity relationship (SAR) of oxazolidinone derivatives as new antibacterial agents.
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