Immunopharmacological Drugs

Vardanyan, Ruben; Hruby, Victor J.

doi:10.1016/b978-0-12-411492-0.00029-8

Cited by 3 publications

(3 citation statements)

References 102 publications

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“…XX w. wykorzystywano je w zwalczaniu białaczki u dzieci. Jedną z najstarszych pochodnych jest azatiopryna, analog purynowy zaburzający syntezę DNA (Gertrude Elion i George Hitchings, którzy odkryli ją na fali poszukiwań analogu 6-merkaptopuryny w metabolicznie aktywnej, ale zamaskowanej formie) [112][113].…”

Section: Linkozamidyunclassified

Zarys historii syntezy leków ze szczególnym uwzględnieniem leków przeciwnowotworowych i przeciwbakteryjnych

Warguła¹

2022

pps

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W pracy przedstawiono zarys historyczny rozwoju leków od czasów najdawniejszych do czasów obecnych, starając się uwzględnić zarówno drogę jaką przebyto od poznania właściwości leczniczych surowca, przez wskazanie konkretnych związków aktywnych z niego wyizolowanych, po identyfikację celu biologicznego. Na przykładzie syntezy pierwszych chemicznych środków leczniczych wskazano kierunki badań i tok rozumowania ówczesnych naukowców. Omawiając historię środków przeciwbakteryjnych, nakreślono drogę, jaką przebyto od przypadkowego odkrycia Fleminga, po organiczną syntezę związków o innej niż przeciwdrobnoustrojowa aktywności biologicznej. Fakt ten zazębia się z historią rozwoju leków przeciwnowotworowych, którą zarysowano z uwzględnieniem głównych mechanizmów działania.

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Section: Linkozamidyunclassified

Zarys historii syntezy leków ze szczególnym uwzględnieniem leków przeciwnowotworowych i przeciwbakteryjnych

Warguła¹

2022

pps

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“…It is a 31-membered macrolide immunosuppressant member having some antiproliferation effects on lymphoid and non-lymphoid cells (5). It is classified as xenobiotic immunosuppressant which are produced via endogenic processes and derived from microbes with antiproliferation effect on lymphocytes (6). RAPA was traditionally used to prevent kidney transplantation rejection, also used in treatment of rheumatoid arthritis and some types of cancers (7).…”

Section: Introductionmentioning

confidence: 99%

“…RAPA was traditionally used to prevent kidney transplantation rejection, also used in treatment of rheumatoid arthritis and some types of cancers (7). RAPA is one of the two clinically used mTOR (mammalian target of rapamycin) inhibitors, rapamycin and everolimus, approved by Food and Drug Administration (FDA) in clinical use (6). RAPA inhibits proliferation of splenic Tand B-cells (8).…”

Section: Introductionmentioning

confidence: 99%

Rapamycin and Filgrastim effect on Regulation of Peripheral and Splenic Tissue B- and T-lymphocytes in TAA-Induced Splenic Injury in Rats

Keshta

Abdelfatah

Abdelrahman

2022

Biochemistry Letters

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Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

et al. 2022

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The basic configuration of glucocorticoid consists of four-fused rings associated with one cyclohexadienone ring, two cyclohexane rings, and one cyclopentane ring. The ways the structure and dynamics of five glucocorticoids (prednisone, prednisolone, prednisolone acetate, methylprednisolone, and methylprednisolone acetate) are altered because of the substitution of various functional groups with these four-fused rings are studied thoroughly by applying sophisticated solid-state nuclear magnetic resonance (NMR) methodologies. The biological activities of these glucocorticoids are also changed because of the attachment of various functional groups with these four-fused rings. The substitution of the hydroxyl group (with the C11 atom of the cyclohexane ring) in place of the keto group enhances the potential of the glucocorticoid to cross the cellular membrane. As a result, the bioavailability of prednisolone (the hydroxyl group is attached with the C11 atom of the cyclohexane ring) is increased compared to prednisone (the keto group is attached with the C11 atom of cyclohexane rings). Another notable point is that the spin–lattice relaxation rate at crystallographically distinct carbon nuclei sites of prednisolone is increased compared to that of the prednisone, which implies that the motional degrees of freedom of glucocorticoid is increased because of the substitution of the hydroxyl group in place of the keto group of the cyclohexane ring. The attachment of the methyl group with the C6 atom of cyclohexane rings further reduces the spin–lattice relaxation time at crystallographically distinct carbon nuclei sites of glucocorticoid and its bioactivity is also increased. By comparing the spin–lattice relaxation time and the local correlation time at crystallographically different carbon nuclei sites of three steroids prednisone, prednisolone, and methylprednisolone, it is observed that both the spin–lattice relaxation time and the local correlation time gradually decrease at each crystallographically distinct carbon nuclei sites when we move from prednisone to prednisolone to methyl-prednisolone. On the other hand, if we compare the same for prednisolone, prednisolone acetate, and methylprednisolone acetate, then we also observe that both the spin–lattice relaxation time and the local-correlation time gradually decrease from prednisolone to prednisolone acetate to methylprednisolone acetate for all chemically different carbon nuclei. It is also noticeable that both the spin–lattice relaxation time and the local-correlation time gradually decrease from prednisone to prednisolone to prednisolone acetate to methylprednisolone to methylprednisolone acetate for most of the carbon nuclei sites. From in silico analysis, it is also revealed that the bioavailability and efficacy of the glucocorticoid increase from prednisone to prednisolone to prednisolone acetate to methylprednisolone to methylprednisolone acetate. Hence, it can be concluded that the biological activity and the motional degrees of freedom of the glu...

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Immunopharmacological Drugs

Cited by 3 publications

References 102 publications

Zarys historii syntezy leków ze szczególnym uwzględnieniem leków przeciwnowotworowych i przeciwbakteryjnych

Zarys historii syntezy leków ze szczególnym uwzględnieniem leków przeciwnowotworowych i przeciwbakteryjnych

Rapamycin and Filgrastim effect on Regulation of Peripheral and Splenic Tissue B- and T-lymphocytes in TAA-Induced Splenic Injury in Rats

Investigation of the Influence of Various Functional Groups on the Dynamics of Glucocorticoids

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