Current Bioactive Compounds - Volume 14, Issue 3, 2018

Background: A large number of scientific researches have been reported for isatin and its Schiff base metal complexes, but there is no detailed compilation of these isatin Schiff base metal complexes with their biological properties. This review may help scientist to develop new drugs with more potent activity and specificity in their action. Method: This review is designed according to the different metal complexes of differe Read More

In 1863, Diphenylamine (DPA) was prepared by Hoffmann by the destructive distillation of different triphenylmethane dyes. DPA are naturally occurring compounds, present in onions, leaves of black and green tea and peel of citrus fruits. DPA derivatives belong to the category of Non Steroidal Anti-inflammatory Drugs (NSAIDs). Diclofenac, chemically called 2-(2,6-dichloranilino) phenylacetic acid, is a well-known NSAID Read More

Background: Considering the fact that many nitrogenated aromatic derivatives such as pyrazoles, hydrazones, pyrazolo[1,5-a]-pyrimidines and pyrazolo [3,4-b]-pyridine have shown antiparasitic properties, the current study was carried out to analyze the in vitro antileishmanial and antitrypanosomal potential of some derivatives, synthesize from 6-substituted-3-formylcromone. Method: The pyrazoles (4a-c), hydrazo Read More

Background: Novel oximinoethers of indanones / aryloxy indanones were designed, synthesized and evaluated in vitro as antileishmanials against Leishmania donovani. Most of the synthesized compounds (5-12) exhibited 100% inhibition at 10 μg/mL against promastigotes and six compounds (5, 6, 7, 9, 11 and 12) exhibited 100% inhibition at 10 μg/mL with an IC50 in the range of 1.65-4.98 μg/mL against amastigotes. Among al Read More

Background: 4-substituted pyroglutamates have found use in the synthesis of ACE inhibitors e.g. Fosinopril, conformationally constrained peptides as well as bioactive natural products. Such versatile applications associated with 4-substituted Pyroglutamates encouraged researchers to study the Lienolate derived alkylation of pyroglutamate with electrophiles. Though several reports are available on Li-enolate derived reactions of Read More

Background: Prevalence of lung cancer and breast cancer is increasing worldwide. Current therapies have certain limitations for the treatment of lung cancer and breast cancer. We herewith report a series of novel 2-((1H-1,2,3-triazol-1-yl)methyl)-3-phenylquinazolin-4(3H)-ones as anticancer agents for the treatment of lung cancer and breast cancer. Method: Synthesis of 2-((1H-1,2,3-triazol-1-yl)methyl)-3-phenylquinazolin-4(3 Read More

Objective: In the present work, we aim to investigate the acute toxicity and to evaluate the antioxidant, anti-inflammatory, analgesic, and antipyretic activities of the methanol extract (UDME) of Urospermum dalechampii (L.) Scop. ex F.W.Schmidt. Methods: Total phenolics, total flavonoids, and condensed tannins content were estimated by colorimetric methods. The antioxidant activity was evaluated by various a Read More

Background: Thiabendazole (TBZ; 4-(1H-benzimidazol-2-yl)-1,3-thiazole) is a well known anti-fungal and anti-helminthic agent. It has been observed that substitution pattern by different alkyl, aryl or heterocyclic functionalities at the various positions of benzimidazole as well as thiazole nucleus markedly influence the biological efficacy. In this study, we synthesized a novel series of TBZ derivatives with structure modifications inv Read More

Background: We developed Multicomponent synthesis for novel Mannich products with biologically active quinoline nucleolus under solvent free condition. This methodology provided us good amount of yield with the exception of chromatographic separation. The structure of novel compounds (4d1-d13) was characterized by elemental, mass, 1H-NMR, 13C-NMR and IR spectroscopic analysis. In vitro antimicrobial stu Read More

Background: Several synthesized chromones derivatives have been found to promote intense vasodilation and antihypertensive activity. 2 hydroxymethylchromone (2HMC) is a benzopyrane derivative that vasodilator effect on small arteries has not yet been investigated. This study describes its synthesis, examines any vasodilator effect observed, and clarifies its mechanism of action in rat mesenteric arterial bed (M Read More

Background: Breast cancer is the most common invasive cancer in female worldwide. Indole scaffold represents an important class of therapeutic agents in medicinal chemistry. Many indole derivatives are reported as potent anticancer agents. This study aims to design, and synthesize anti-breast cancer potential of new bisindole derivatives. Method: The target molecules were prepared by reacting cyano acetyl indoles with Read More

Objective: The objective of this study was to synthesize a series of 1,3,4-thiadiazole derivative and evaluate their possible in vitro and in vivo anticancer activity. Method: Compounds 7a-f have been synthesized by chlorination of 2-[bis(2-hydroxyethyl)amino]-N-[5- substituted phenyl)-1,3,4-thiadiazol-2-yl]acetohydrazide with phosphorous oxychloride and phosphorous pentachloride. Synthesis of the targeted compounds was Read More