The central role of lipophilicity in drug discovery is emphasized. Amine basicity is discussed as a function of fluorination patterns focusing on additivity effects, conformation, and specific noncovalent interactions. Modulation of effective and intrinsic lipophilicity is explored for simple pa...

A new intact glucosinolate Cinnamoyl derivative [6'-O-trans-(4″- hydroxy cinnamoyl)-4-(methylsulphinyl) butyl glucosinolate] (A) has been isolated from Broccoli (Brassica oleracea L. var. italica) florets. The compound was isolated and characterized by LC, MS-ESI, FTIR, 1H and 13C NMR as w...

Cinnamoyl alginate, cinnamoyl Pluronic F127 and cinnamoyl poly(ethylene glycol) were self-assembled into nanogel in aqueous phase. The size of nanogel was 100 nm–200 nm on TEM photos. When 1 ml of human growth hormone (hGH) solution (5 mg/ml, pH3.0) was mixed with 4 ml of the nanogel suspension...

New lanthanide complexes of 4-chloroquinoline-1-oxide (CQNO) and 5-chloroisoquinoline-2-oxide (CIQNO) were synthesized. CQNO gave two sets of complexes, one set soluble in acetone with the formulae [Ln(CQNO)8](ClO4)3, where LnNd to Yb, and [La(CQNO)10](ClO4)3, and the other insoluble in aceton...

A facile and microwave accelerated reaction of 1-chloro-3-(4-chlorophenyl)isoquinoline with various heterocyclic amines, catalyzed by Pd, in the presence of BINAP additive and sodium carbonate as the base, leads to the formation of 3-(4-chlorophenyl)-1-(1H-1,2,3-triazol-1-yl)isoquinoline, 3-(4-c...

An efficient, copper-free Sonogashira coupling reaction of 1-chloroisoquinolines and terminal alkynes, catalyzed by Pd(OAc)2/Ruphos, in the presence of Et3N and tetrahydrofuran leads to the formation of 1-alkynyl-3-substituted isoquinolines in good yields.

Sequential treatment of a (3-substituted-1-thioxo-1,2,3,4-tetrahydroisoquinolin-4-ylidene)acetic acid with thionyl chloride and a nucleophile did not give the expected ester or amide, but a derivative of 2-(3-substituted-1-chloroisoquinolin-4-yl)acetic acid, constituting a simple procedure for t...

Our study presents the synthesis and structure-activity relationship (SAR) of novel N-substituted nipecotic acid derivatives closely related to DDPM-1457 [(S)-2a], a chemically stable analog of (S)-SNAP-5114 (1), in the pursuit of finding new and potent mGAT4 selective inhibitors. Iminium ion ch...

A novel series of 3-acetamido-4-methyl benzoic acid derivatives designed on the basis of vHTS hit ZINC02765569 were synthesized and screened for PTP1B inhibitory activity. The most potent compounds 3-(1-(5-methoxy-1H-benzo[d]imidazol-2-ylthio)acetamido)-4-methyl benzoic acid (10c, IC50 8.2 μM) ...

Pyrolysis results for a variety of compounds are presented in this chapter. This include esters such as esters of alcohols that have or do not have a β-hydrogen, esters with additional functional groups, esters between alcohols with β-hydrogen and simple monocarboxylic acids, esters of alcohol...

This chapter deals the chemistry, structural and reactivity aspects of saturated, and unsaturated five membered monocyclic and benzene fused heterocycles with mono nitrogen, oxygen and sulfur heteroatom such as pyrrole, pyrrolidine, indole, isoindole, indolizine, carbazole, furan, reduced furan,...

STAT3 has been extensively studied as a potential antitumor target. Though studies on regulating STAT3 mainly focus on the inhibition of STAT3 phosphorylation at Tyr705 residue, the phosphorylation at Ser727 residue of STAT3 protein is also closely associated with the mitochondrial import of STA...

A Lewis acid-catalyzed [3 + 3] cycloaddition reaction of donor‒acceptor aziridines with N,N-dialkyl-3-vinylanilines has been developed for the stereoselective synthesis of tetrahydroisoquinolines (THIQs). The reaction performed using Gd(OTf)3 as the Lewis acid catalyst was tolerant to various N-...

This review aimed to document the publications concerning 4-hydroxycoumarin, its synthesis, chemical reactivity and reactions during the period from 1996 up to now.

This article describes the synthesis of some novel sulfonamides having biologically active pyridine 21–28. Starting with 4-(1-(2-(2-cyanoacetyl)hydrazono)ethyl)-N-ethyl-N-methylbenzenesulfonamide (2), which was prepared from condensation of acetophenone derivative 1 with 2-cyanoacetohydrazide. ...

A novel solvatochromic l-(4-dimethylaminophenyl)-2-(5H-phenanthridine-6-ylidene)-ethanone (6-KMPT) dye was synthesized and characterized by means of NMR, IR, mass spectroscopies. Also, it was studied using UV–vis and fluorescence spectroscopic methods in a broad range of solvents. UV–vis resul...

A series of novel hybrids β-carboline-4-thiazolidinones were synthesized and evaluated for their in vitro antitumor activity against human cancer cell lines and for antiviral activity towards Herpes simplex virus type-1 (HSV-1). From the N′-(2-ylidene-4-thiazolidinone)-β-carboline-3-carbohydr...

The title compound 6-chloro-7-hydroxy-4-methyl-2H-chromen-2-one, a coumarin derivative was synthesized and characterized by using spectroscopic tools such as mass spectra, NMR (1H and 13C) and finally the structure was confirmed by the single crystal X-ray diffraction studies. The title compound...

Of twenty-one nicotinic acid analogs assayed against tri-o-cresyl phosphate-induced ataxia in hens, five provided partial relief of the syndrome. These were nicotinamide, nikethamide, phenyl nicotinate, 3-picoline, and 3-acetylpyridine. Almost all of those assayed in mice against tri-n-butyl pho...

1-(1-alkenyl)-(1a-g) and 1-(1-cycloalkenyl)cycloalkyl esters (acetate, tosylate, mesylate) (4a-d) underwent palladium(0) catalyzed hydrogenolysis by sodium formate or n-butylzinc chloride as hydride sources. The regioselectivity of the reduction can be monitored either by ring strain, silyl subs...