6-Oxy-(N-succinimidyl acetate)-9-(2′-methoxycarbonyl)fluorescein (SAMF), a new fluorescein-based amine-reactive fluorescent probe was well designed, synthesized and used as a pre-column derivatizing reagent for the determination of aliphatic amines in HPLC. It exhibited relatively pH-independen...
Vascular Adhesion Protein-1 (VAP-1) is a promising therapeutic target for the treatment of several inflammatory-related diseases including diabetic microvascular complication. We identified glycine amide derivative 3 as a novel structure with moderate VAP-1 inhibitory activity. Structure-activit...
The pharmacokinetic based optimisation of a novel series of indole-2-carboxamide antagonists of the cannabinoid CB1 receptor is disclosed. Compound 24 was found to be a highly potent and selective cannabinoid CB1 antagonist with high predicted human oral bioavailability.
Structure-based drug design and molecular modeling were employed to identify a new series of indole-2-carboxamides as potential anticancer agents. These compounds were synthesized and characterized with the aid of several spectroscopic techniques, such as FT-IR, NMR, and mass spectrometry as wel...
A series of substituted 1H-indole-2-carboxamides structurally related to compounds Org27569 (1), Org29647 (2) and Org27759 (3) were synthesized and evaluated for CB1 allosteric modulating activity in calcium mobilization assays. Structure–activity relationship studies showed that the modulation...
5-Chloro-3-ethyl-N-(4-(piperidin-1-yl)phenethyl)-1H-indole-2-carboxamide (ORG27569, 1) is a prototypical allosteric modulator for the cannabinoid CB1 receptor. Based on this indole-2-carboxamide scaffold, we designed and synthesized novel CB1 allosteric modulators that possess photoactivatable f...
A series of substituted indoloquinolinones were readily synthesized, via two steps, from indole-2-carboxylic acid and its derivatives: a 3-arylation of indole-2-carboxamides and a subsequent PIDA-mediated oxidative C–N bond formation. The underpinning strategy involves a Cu(I)-promoted C(sp2)–...
A series of novel compounds carrying pyrazino[1,2-a]indol-1(2H)-one scaffold (5a-g) and their reaction intermediates, indole-2-carboxamides, (3a-g) were synthesized and evaluated for their ability to inhibit reactive oxygen species (ROS) generation, antioxidant activity and anticancer activity a...
A novel series of 2-(4-sulfonamidophenyl)-indole 3-carboxamides was identified and optimized for activity against the HCV genotype 1b replicon resulting in compounds with potent and selective activity. Further evaluation of this series demonstrated potent activity across HCV genotypes 1a, 2a and...
A novel series of highly diverse indole-2-carboxamides was synthesized utilizing the isocyanide based multicomponent reaction (IMCR)-post modification approach and were identified as potential antileishmanial chemotype. Among the synthesized 18 analogues, 12 analogues exhibited better antileishm...
Current treatment regimens for non-tuberculous mycobacteria (NTM) and tuberculosis (TB) generally require long duration of therapy with multiple drugs, some of which are broad spectrum antibiotics. Despite some advances in antimicrobial compounds, there remains a need in therapy for antibiotics ...
The pharmacologically active dichloromethane extracts of dried woad leaves (Isatis tinctoria L.), and the methanol extracts of comparable fresh leaves of the same plants, were analyzed by LC-MSn. The fresh leaf metabolite profile revealed a complex pattern of indolic compounds. Besides the known...
In this paper, the effects of carboxylic substituent position on their electrodeposition, morphology and capacitance properties were investigated for the first time. The results indicated that three carboxylic group substituted polyindole derivatives nanowires, namely poly(indole-5-carboxylic ac...
A novel electrochromic material, poly(indole-6-carboxylic acid) (PIn), and its application in electrochromic devices (ECDs) are discussed. PIn was switched between yellow in the reduced state and green in the oxidized state. Electrochromic switching of PIn film shows that it has fast switching t...
A new cobalt(II) coordination polymer of indole‑3‑carboxylic acid (I3CAH2), [Co(I3CAH)2(H2O)]n has been synthesized and characterized using single-crystal X-ray diffraction, infrared spectroscopy and thermal (TGA/DTG analysis). The crystal structure is monoclinic, space group Cc, with a = 33.406...
We synthesized novel tetracyclic fused indole derivatives via the intramolecular Heck reaction of indole-containing Baylis–Hillman adducts in good to moderate yields.
Poly(indole-6-carboxylic acid) (PICA) was synthesized electrochemically over glassy carbon electrode (GCE) through potentiodynamic mode of polymerization. The resulting polymer was soluble in Tris–HCl buffer (pH 7.0). The processable polymer was cast over desired electrode surface along with or...
A simple and label-free electrochemical sensor for detection of DNA hybridization event was obtained based on a novel nanostructured conducting polymer, poly(indole-6-carboxylic acid). This precursor polymer with high electroactivity can be easily prepared by direct electrochemical polymerizatio...
A novel, highly sensitive amperometric biosensor for detection of organophosphorus (OP) compounds has been constructed, based on rat brain acetylcholinesterase (AChE) immobilized onto nanocomposite of ZnS-nanoparticles (ZnSNPs) and poly(indole-5-carboxylic acid) electrodeposited on Au electrode....
The glucose level measurement in the diabetic patient plays a vital role in identification of the treatments going on and it also provides the control over the diabetics. A new electrochemical sensing device was constructed for determination of glycated hemoglobin (HbA1c) in whole blood samples....
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