Leishmaniasis and microbial infections are two of the major contributors to global mortality and morbidity rates. Hence, development of novel, effective and safer antileishmanial and antimicrobial agents having reduced side effects are major priority for researchers. Two series of N-substituted indole derivatives i.
View Article and Find Full Text PDFBepotastine (BPT) is a H-receptor antagonist. It is used as a besilate salt in ophthalmic solution for allergic conjunctivitis and orally for the treatment of allergic rhinitis and urticaria/pruritus. Its systematic forced degradation study is unreported.
View Article and Find Full Text PDFA serendipitous discovery of [1,3]-sulfonyl migration has been made in the two-component reaction of azomethine imine and allenoates. Current methodology involving N-S bond cleavage and C-S bond formation provided easy access to biologically important arylsulfonylmethyl substituted pyrazolo[1,5-c]quinazolines. Subsequently, a one-pot sequential protocol has been developed from the easily available starting material.
View Article and Find Full Text PDFJ Pharm Biomed Anal
January 2020
The present study was to investigate the degradation profile of sorafenib tosylate (SORA), a potent oral multi-kinase inhibitor under various stress conditions as per ICH (Q1A (R2)) guidelines. Separation of SORA and its degradation products (DP-1-DP-5) was achieved on Acquity UPLC BEH C18 (100 mm × 2.1 mm × 1.
View Article and Find Full Text PDFAzines are organic molecules which bear the C[double bond, length as m-dash]N-N[double bond, length as m-dash]C functional unit. In the recent past, azines have received increased attention due to the recognition of their biological, chemical and materials properties. Azines have been conventionally synthesised by the condensation of hydrazine with ketones and aldehydes, and many alternate routes are also available.
View Article and Find Full Text PDFWe herein report for the first time an unusual decomposition of 2-nitrophenyl-substituted -formyl pyrazolines under Bechamp reduction condition employed to yield 2-aryl quinolines exclusively instead of pyrazolo[1,5-]quinazolines. The reaction investigation suggests acid-mediated cleavage of followed by a retro-Michael addition, and a subsequent in situ intramolecular reductive cyclization through a modified Friedlander mechanism afforded 2-aryl quinolines () in good yields. The proposed mechanistic pathways were supported via experimental evidence and density functional theory studies.
View Article and Find Full Text PDFThe present study focused upon the forced degradation behaviour of fosamprenavir (FPV), an antiretroviral drug. A total of six degradation products (DPs) were separated on a non-polar stationary phase by high performance liquid chromatography (HPLC). For the characterization, comprehensive mass fragmentation pathway of the drug was initially established using high resolution mass spectrometry (HRMS) and multi-stage tandem mass spectrometry (MS) data.
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