China
Africa
Explore chapters and articles related to this topic
Operations at the Philadelphia Laboratory
Published in George Winston Smith, Medicines for the Union Army, 2014
Because it was a residual salt that remained in the “mother liquor” after quinia and quinidia had crystallized, cinchonia had accumulated in the possession of the manufacturers. Compared to quinine it had been overlooked, and even in 1863 sold for as little as forty-two cents per pound. When the supply table went through its revision in 1862, Hammond added it to the list. The manufacturers were then able to dispose of their supplies of it at a considerable profit, but doubtless it tended to hold down the price of quinine sulfate.181 Late in the war there was still a large supply of cinchonia sulfate available, although it too began to rise in price.182 From a theoretical viewpoint, cinchonia sulfate seemed to win quick acceptance. The apothecary of the Pennsylvania Hospital declared that the three cinchona alkaloids (quinidia, quinia, and cinchonia) were “used indiscriminately and in the same doses” in that hospital.183 In India, three medical commissions appointed to assess the effectiveness of the cinchona alkaloids discovered that a mixture of the three alkaloids provided a drug just as effective as quinine sulfate, and “poor man’s quinine” came into being.184 The Madras Commission’s analysts, however, found cinchonia to be considerably inferior to the other alkaloids.185 During the Civil War, some physicians insisted that larger doses of it were necessary to get comparable results, and that it was “more variable and less reliable than the quinia salt.”186 Cinchonia sulfate was officinal in the fourth revision of the United States Pharmacopoeia,187 although quinidia sulfate—which Pepper and other outstanding practitioners prescribed in the same or smaller doses than quinine sulfate188—was not.
Synthesis, kinetic studies and in-silico investigations of novel quinolinyl-iminothiazolines as alkaline phosphatase inhibitors
Published in Journal of Enzyme Inhibition and Medicinal Chemistry, 2023
Muhammad Naeem Mustafa, Pervaiz Ali Channar, Muhammad Sarfraz, Aamer Saeed, Syeda Abida Ejaz, Mubashir Aziz, Fatmah Ali Alasmary, Hanadi Yaqob Alsoqair, Hussain Raza, Song Ja Kim, Asad Hamad
In the quest for safe drug therapy, researchers are striving for development of novel and specific medication for APs associated malignancies. Among various heterocyclic compounds, the quinolone and thiazolines possessed a wide range of biological and pharmacological activities including anti-cancer, anti-fungal, analgesic, antihypertensive and antibiotic activities. Specifically, quinoline has displayed an broad spectrum of biological applications such as anti-fungal, antimalarial, anticonvulsant, analgesic, anti-bacterial, cardiotonic anthelmintic, and anti-inflammatory activities19. Several pharmacologically active substances and natural products (Cinchona Alkaloids) possess quinoline nucleus20. The most famous quinoline based drug chloroquine I (Figure 1) resulted in eradication and control of malaria for the decades. This type of drugs influence parasite’s life cycle during blood stages21.
Improvement of solubility, dissolution and stability profile of artemether solid dispersions and self emulsified solid dispersions by solvent evaporation method
Published in Pharmaceutical Development and Technology, 2018
Muhammad Tayyab Ansari, Muhammad Sohail Arshad, Altaf Hussain, Zeeshan Ahmad
Over the years various treatments have been proposed for the eradication of malaria. These include various drug types such as sulfonamides and cinchona alkaloids. However, the emergence of malarial resistance toward conventional treatments has led to persistent risk of infection5. The more recent anti-malarial agent “artemether,” belongs to the Artemisinins family and is an active constituent of Chinese herbs known as qinghao, also termed Artemisia annua. Artemether is metabolized into de-methylated derivative dihydroartemisinin in the liver. Both artemether and its metabolite possess a 1,2,4-trioxane ring, which is an active pharmacophore responsible for anti-malarial properties6 and exhibits efficient schizontocidal action against P. falciparum7,8. However, the poor water solubility of artemether poses obstacles in the development of oral formulations. Although this issue is partly resolved when administered as an intramuscular injection, the development of oral formulations is much preferred, providing greater patient compliance and economical benefits. Solubility enhancement approaches such as solid dispersions (SDs) in water soluble polymers, SESDs, micronization and complex formation with cyclodextrins are expected to yield novel strategies and therapeutic effects9,10.
Dealing with frequent hitters in drug discovery: a multidisciplinary view on the issue of filtering compounds on biological screenings
Published in Expert Opinion on Drug Discovery, 2019
Rafael Ferreira Dantas, Tereza Cristina Santos Evangelista, Bruno Junior Neves, Mario Roberto Senger, Carolina Horta Andrade, Sabrina Baptista Ferreira, Floriano Paes Silva-Junior
In a subsequent study by the same group, the BIOS approach was also applied, this time to quinidine as a cinchona alkaloid [27]. The synthesis methodology allows the direct transformation of the quinidine structure into the oxazatwistane portion, allowing the generation of 50 new compounds from late stage C-H functionalization and metal-catalyzed coupling reactions (Figure 4(c)). The compounds were screened with target-agnostic phenotypic assays, and some of them showed to have the capacity to act as inhibitors of starvation-induced autophagy in the submicromolar range. The results from the study showed that the new inhibitors represent a new class of autophagy modulators, once their guiding NPs do not exhibit this inhibitory activity at the same tested conditions.