5-(2-(4-pyridinyl)vinyl)-6-chloro-3-(1-methyl-2-(S)-pyrrolidinylmethoxy)pyridine (1b) exhibited high affinity for nicotinic acetylcholine receptors in the in vitro competition binding assays, with a Kd value in the low picomolar range, performed at room temperature and at physiological temperatu...

In order to explore the viability and generality of a recently uncovered [4+1] cycloaddition based strategy for the preparation of pyrazolo[3,4-c]pyridine derivatives, members of a series of 5-arylazo-2,3,6-trisubstituted pyridines were prepared by reactions of 3-oxo-2-arylhydrazonopropanals wit...

An oxadiazole-based chemosensor (sensor 1) for Fe3+/Fe2+ was successfully designed and synthesized. Sensor 1 displayed fluorescence quenching response towards both Fe3+ and Fe2+ in THF:H2O (4:1, v/v) solvent with high selectivity and sensitivity over all other competitive metal ions. Job's ...

A symmetrical oxadiazole derivative (OXD) containing two pyrazole moieties was synthesized successfully and characterized by single crystal X-ray diffraction, nuclear magnetic resonance and mass spectrometry. The synthesized compound displayed “On-Off” fluorescent sensing towards Cu2+ with hig...

Structure–activity relationship studies in a series of diarylpyrazolyl thiadiazoles identified cannabinoid-1 receptor antagonists with excellent potency and selectivity. Based on its exceptional in vivo efficacy in animal models and its favorable pharmacokinetic and toxicological profiles, 2-(4...

Histamine H3 receptor (H3R) is largely expressed in the CNS and modulation of the H3R function can affect histamine synthesis and liberation, and modulate the release of many other neurotransmitters. Targeting H3R with antagonists/inverse agonists may have therapeutic applications in neurodegene...

A series of1,2,4- and 1,3,4-oxadiazole derivatives were synthesized and evaluated for their anticancer activity. Halogenated 1,2,4-oxadiazoles were obtained from benzonitrile and coupled either lipophilic amines or with aminoalcohols. Lipophilic 1,3,4-oxadiazole derivatives were obtained through...

A total synthesis of (+)-spatol (1) was achieved which depends upon a novel stereospecific transformation of trans-2,3-epoxy-1,4-diols to generate the sensitive allylic vicinal cis-diepoxide in 1.

The first total synthesis of (+)-spatol (1) with natural configuration is described. The important step utilizes the carbon-carbon bond formation with simultaneous epoxide formation by the reaction of optically pure sulfonium ylide (4) and optically pure epoxy aldehyde (5).

Total synthesis of optically pure spatol (+)-1 was achieved by employing asymmetric (2+2) photocycloaddition of the optically pure butenolide 12 with cyclopentenone ethylene ketal. The two major photocycloadducts 14, 15 were separately converted into the cis,anti,cis-tricyclo-[5.3.0.0.2,6]decane...

An α-lithio epoxide intermediate provides a highly stereocontrolled synthesis of the spatol allylic diepoxide, a functional array that is uniquely effective at inhibiting mitosis.

Xenon oscillation is caused by imbalance of xenon distribution in nuclear reactors. Procedures have been developed in the past to dampen these oscillations. One of the procedures is known as quite simple and effective, which uses several constants obtained from reactor modeling codes in the anal...

Induction of acquired resistance activates defense-related genes. Current study aimed to (a) initiate potato acquired resistance to the Early Blight disease caused by Alternaria solani through treating potato plants with low and repetitive doses of 2,4-dichlorophenoxy acetic acid (2,4-D), abscis...

A series of kojic acid-derived compounds 6a-p bearing aryloxymethyl-1H-1,2,3-triazol-1-yl moiety were designed by modifying primary alcoholic group of kojic acid as tyrosinase inhibitors. The target compounds 6a-p were synthesized via click reaction. All compounds showed very potent anti-tyrosin...

In glasshouse tests against the soil-borne disease potato common scab (Streptomyces scabies), foliar sprays (0 · 9 mm) of several compounds inhibited symptom development as effectively as 3,5-D (3,5-dichlorophenoxyacetic acid). These compounds were of two main types: (1) compounds very similar ...

Treatment of tissue disks from chicory root with 10−5 M solutions of the highly active plant growth regulator 2,4-dichlorophenoxyacetic acid (2,4-d) results in a very large water uptake. This is accompanied by extensive hydrolysis of oligosaccharides and a very marked increase in hydrolase and i...

This research has provided the most active 5-HT6R agents among 1,3,5-triazine derivatives investigated to date and has also identified the world's first selenium-containing 5-HT6R ligands. The studies are focused on design, synthesis, biological evaluation and docking-supported SAR analysis...

Nine molecular co-crystals containing 2,3-, 2,5-, 2,6- and (3,5-dichlorophenoxy)acetic acid have been prepared and studied using single-crystal X-ray diffraction techniques. The free acid structure of (2,3-dichlorophenoxy)acetic acid is also reported. The bases used to prepare the adducts were 2...

Two series of ω-phenoxy contained acylhydroxamic acids as novel urease inhibitors were designed and synthesized. Biological activity evaluations revealed that ω-phenoxypropinoylhydroxamic acids were more active than phenoxyacetohydroxamic acids. Out of these compounds, 3-(3,4-dichlorophenoxy)p...

Some novel 2-oxo-acetamidines were synthesized via one-pot three-component reaction of acetophenones, secondary amines and anilines in presence of CuI as catalyst. The reaction involved in a oxidation process of C (sp3)H bonds of acetophenones in presence of air followed by aminations, and produ...