Synthesis and antiplasmodial evaluation of 1H-1,2,3-triazole grafted 4-aminoquinoline-benzoxaborole hybrids and benzoxaborole analogues.

A library of 1H-1,2,3-triazole-tethered 4-aminoquinoline-benzoxaborole hybrids as well as aryl substituted benzoxaborole analogues was synthesized and screened for their anti-plasmodial efficacy against both chloroquine-susceptibility 3D7 and chloroquine-resistant W2 strains of P. falciparum. The inclusion of quinoline core among the synthesized analogues resulted in substantial enhancement of anti-plasmodial activities. Further, the spacer of a flexible alkyl chain is marginally preferred over piperazyl-ethyl in inhibiting growth of P. falciparum. The most potent 4-aminoquinoline-benzoxaborole conjugate with ethyl as spacer exhibited IC50 values of 4.15 and 3.78 µM against 3D7 CQ-susceptible and W2 CQ-resistant strains of P. falciparum with lower cross resistance with Chloroquine. There was no difference in anti-plasmodial activities between the CQ-susceptible 3D7 and CQ-resistant W2 strains of P. falciparum for the benzoxaborole derivatives lacking a quinoline core.

Conversion of aldimines to secondary amines using iron-catalysed hydrosilylation.

Iron-catalyzed hydrosilylation of imines to amines using a well-defined iron complex is reported. This method employs relatively mild conditions, by reaction of imine, (EtO)3SiH in a 1 : 2 ratio in the presence of 1 mol% precatalyst ([BIAN]Fe(η6-toluene), 3, BIAN = bis(2,6-diisopropylaniline)acenaphthene) at 70 °C. A broad scope of imines was readily converted into the corresponding secondary amines without the need for precatalyst activators.

Amalgamating Isatin/Indole/Nitroimidazole with 7-chloroquinolines via azide-alkyne cycloaddition: Synthesis, anti-plasmodial, and cytotoxic evaluation.

The present paper describes the synthesis, anti-plasmodial, and cytotoxic evaluation of 7-chloroquinoline-based conjugates with isatins/indoles/ nitroimidazoles, obtained via Cu-promoted 1,3-dipolar cycloadditions. On contemplating SAR of the synthesized series, the inclusion of indole and nitroimidazole-core improved the anti-plasmodial activities while the isatin seemed to have a lesser effect. The conjugate with a nitroimidazole-core and hexyl chain length as a spacer between the two pharmacophores was found to be most potent among the synthesized series and displayed an IC50 of 0.12 µM and a selectivity index of 1748.

High Performance Fluorescent Turn-On Probe for Amitriptyline Based on Hybrid Nanoassembly of Organic-Inorganic Nanoparticles.

Fluorescence methods have gained enormous attention due to their ease in use, simplicity, selectivity and sensitivity. Fluorescent chemosensors respond instantly by converting molecular recognition to fluorescent signals. The consumption of pharmaceutical products by living beings is on great increase. The disposal of such compounds in the environment is a matter of great concern as these compounds enter aquatic environment and show accumulation in tissues of aquatic organisms. In the present study, we have utilized naphthalimide based receptors to fabricate organic nanoparticles (ONPs). These ONPs were used for the development of hybrid nanoassemblies, and the developed nanoassemblies were characterized with the help of transmission electron microscopy and dynamic light scattering studies. The photophysical studies were performed and the hybrid assembly developed using receptor 2 demonstrated a turn-on fluorescence emission behavior on binding with Amitriptyline. The present sensing system acted as promising candidate for determination of Amitriptyline among other contending drug molecules. The established system can recognize Amitriptyline up to a detection limit of 48 nM in aqueous medium. Electrochemical recognition studies show binding of hybrid nanoassembly of receptor 2 with Amitriptyline with limit of detection of 21 nM.

4-Aminoquinoline-chalcone/-N-acetylpyrazoline conjugates: Synthesis and antiplasmodial evaluation.

1H-1,2,3-triazole linked 4-aminoquinoline-chalcone/-N-acetylpyrazoline conjugates were synthesized and evaluated against cultured chloroquine (CQ) resistant strain. Antiplasmodial activities of the synthesized conjugates revealed dependence of activity on the length of the alkyl chain as well as on the presence of methoxy substituents on ring A/ring B of the chalcone. The most potent and non-cytotoxic conjugate showed comparable antiplasmodial activity with that of CQ, with an IC50 value of 53.7 nM.

Physicians of ancient India.

A survey of Indian medical historiography will reveal no dearth of work on the systems of medicine and medical literature of ancient India. However, the people who were responsible for the healing have not received much attention. This article traces the evolution of the physician as a professional in ancient India. This article reviews the secondary literature on healing and medical practice in India, specifically pertaining to the individual medical practitioner, drawing from varied sources. The healers of ancient India hailed from different castes and classes. They were well-respected and enjoyed state patronage. They were held to the highest ethical standards of the day and were bound by a strict code of conduct. They underwent rigorous training in both medicine and surgery. Most physicians were multi-skilled generalists, and expected to be skilled in elocution and debate. They were reasonably well-off financially. The paper also briefly traces the evolution of medicinal ideas in ancient India.

Physicians of colonial India (1757-1900).

The period of British rule from 1757 to 1900 is marked by major sociopolitical changes and scientific breakthroughs that impacted medical systems, institutions, and practitioners in India. In addition, historians have debated whether the colonial regime used Western medicine as a tool to expand and legitimize its rule. This paper reviews the secondary literature on this subject with emphasis on the individual physicians. During this period, the practice of "Doctory" or Western medicine gained momentum in India, buoyed with the support of the British as well as Western-educated Indians. Many Indians were trained in Western medicine and employed by the administration as "native doctors" in the subordinate medical service, and the superior medical service by and large comprised Europeans. The colonial regime gradually withdrew most of its patronage to the indigenous systems of medicine. The practitioners of these systems, the vaidyas and the hakims, suffered significant loss of prestige against Western medicine's claims of being a more rational "superior" system of medicine. Some of them became purists and defended and promoted their systems, while others adopted the methods and ideas of Western medicine into their education and practice. European doctors now rarely interacted with practitioners of Indian systems, but seriously pursued research into medicinal plants and tropical diseases. There is no mention of specialist physicians in this period, and all physicians and surgeons were generalists. Folk practitioners continued to be popular among the masses.

Synthesis and in vitro antiplasmodial evaluation of 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone conjugates.

The manuscript describes the synthesis of novel amide tethered 7-chloroquinoline-chalcone and 7-chloroquinoline-ferrocenylchalcone bifunctional hybrids and their evaluation as antimalarial agents against W2 resistant strain of Plasmodium falciparum. The antiplasmodial activity of 7-chloroquinoline-ferrocenylchalcones was found to be less than their corresponding simple chalcone conjugates. The presence of a methoxy substituent at para position of ring B on chalcones and longer alkyl chain length markedly improved the antiplasmodial profiles of the synthesized scaffolds with the most potent of the test compound exhibiting an IC50 value of 17.8 nM.