Abstract

Murrayanine is the most highly explored molecule fromMurraya koenigiiL., known popularly as Indian curry plant (familyRutaceae) which demonstrates carminative, astringent, stomachic, purgative, febrifuge, anti-anemic, and anthelminthic.Thiadiazole is a scaffold of prime importance in medicinal chemistry. It has often been observed that thiadiazoleson hybridization with other heterocyclic scaffolds, demonstrates synergistic activity. Based on this fact, a hybrid of1,3,4-thiadiazole was planned to fabricate with murrayanine and also to explore its synergistic potentials in a specificdirection based on the available text information. The present study involved the synthesis of murrayanine-thiadiazolehybrids using a previously reported starting material (E)-2-((1-methoxy-9H-carbazol-3-yl)methylene)thiosemicarbazide and exploring the anti-inflammatory activity of the produced novel compounds. The compound 4c, containing 3-OCH 3 and 4-OH substituents displayed the highest edema reducing activity after 3 hrs. The enhanced activity may be due tothe interaction of the hydrophilic moiety, via oxygen moiety with the active site of the inflammation causing elementslike Cyclooxygenase (COX) and Lipoxygenase (LOX). We tried to establish a crystal clear structure-activity relationship,but due to mixed results, a true relationship cannot be predicted. Rather, an assumption was made based on the availableinteracting groups with the active sites of the chemical mediator. This research will definitely motivate global researchersin rationally designing of natural product-based heterocyclic hybrids which will have great perspective as therapeuticagents in future with reduced side-effects.

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