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Projektowanie, synteza i aktywność przeciw HIV analogów kurkuminy

Projektowanie, synteza i aktywność przeciw HIV analogów kurkuminy

Mohamed Jawed Ahsan / Sachin Kumar Sharma

58,96 €
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Editorial:
KS OmniScriptum Publishing
Año de edición:
2025
Materia
Farmacología
ISBN:
9786209361012
58,96 €
IVA incluido
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Seria 11 analogów kurkuminy została poddana prognozowaniu właściwości molekularnych i podobieństwa do leków za pomocą oprogramowania Molinspiration i MolSoft, a także parametrów lipofilowości i rozpuszczalności za pomocą programu ALOGPS 2.1. Związki zgodne z „zasadą pięciu' Lipinskiego zostały zsyntetyzowane w celu przeprowadzenia badań przesiewowych pod kątem działania przeciw HIV jako leki/związki wiodące dostępne w postaci doustnej. Następnie struktura zsyntetyzowanych związków została potwierdzona analizami spektralnymi (IR, NMR i masowymi), a związki (3a-k) zostały ocenione pod kątem działania przeciw HIV zgodnie ze standardowym protokołem. Maksymalny wynik modelu podobieństwa do leku (1.1.0) uzyskano dla 3,5-bis(4-hydroksy-3-metylostyrylo)-N-(4-chlorofenylo)-1H-pirazol-1-karboksamidu (3b). Stwierdzono, że związek 3b wykazuje aktywność przeciwko HIV z IC50 >3,71 µM i CC50 3,71 µM, jednak aktywność ta była mniejsza niż w przypadku standardowego leku zydowudyny.

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