An isoquinolone derivative, methyl-2-(4-aminophenyl)-1,2-dihydro-1-oxo-7-(2-pyridinylmethoxy)-4-(3,4,5-trimethoxyphenyl)-3-isoquinoline carboxylate sulfate (T-1032), was found to be a novel potent inhibitor of cyclic GMP (cGMP)-binding cGMP-specific phosphodiesterase (PDE5). We investigated the ...

A new type of catalytic cascade pseudo four-component reaction has been found. The simple and facile pseudo four-component reaction of salicylaldehydes and cyclic or heterocyclic ketones with two molecules of malononitrile catalyzed by sodium acetate at ambient temperature results in the formati...

Three cyclic peptides were synthesized by first assembling the amino acid sequences on polystyrene resin derivatized with 4-(4-hydroxymethyl-3-methoxyphenoxy)-butyric acid (HMBA), cleaving the protected peptides from the solid support, and then cyclizing in solution.

Inosine 5′-monophosphate dehydrogenase (IMPDH, EC 1.1.1.205) catalyzes a crucial step in guanine nucleotide biosynthesis, thereby governing cell proliferation. In contrast to mammalian IMPDHs, microbial IMPDHs are relatively less explored as potential targets for antimicrobial drug discovery. I...

DPP-IV inhibitors have been immersed as promising pathway to treat Type 2 diabetes. Here we have reported designing of coumarin derivatives as DPP-IV inhibitors. Designed compounds have been studied for their binding with DPP-IV enzyme through molecular docking followed by synthesis. All synthes...

The first online method with 1s time resolution for Geometric Surface Area (GSA) measurement of aerosol nanoparticles and the corresponding instrumentation prototype were proposed and developed in this study. This developed method consists of one diffusion charger, followed by two electrostatic ...

Low- and high-resolution nuclease mapping of in vivo transcripts, and in vitro transcription reactions using purified RNA polymerase, were used to analyse transcription of and around the mmr gene, which specifies resistance of Streptomyces coelicolor A3(2) to methylenomycin (Mm) and is located i...

Oxidation of the α-alkylthio-substituted phosphonate carbanions was found to give the corresponding carbonyl compounds. A new synthesis of 1,4-dicarbonyl systems involving the oxygenation of phosphonate carbanions as a key step is described. Total synthesis of dihydrojasmone and allethrone and ...

The gas flow thermolyses of 1-isobutenyl alkynyl and 2-methylphenyl alkynyl ketones were found to lead to phenols and to cyclopentenones. The results are explained by a 5-ring carbene process (the known α-alkynone cyclization) and a 6-ring as well as a 5-ring addition process. The latter two (n...

A concise and efficient synthesis of the new compound—(+)-didesmethylmethylenomycin A methyl ester from chiral building block 4 has been achieved.

Previous studies had localised the gene (mmr) for resistance to methylenomycin A (Mm) to a 2.5-kb PstI fragment in the middle of a cluster of Mm biosynthetic genes from the Streptomyces coelicolor plasmid SCP1. In this paper, the gene has been more precisely located by sub-cloning, and the nucle...

A new synthesis of methylenomycin B (1) has been accomplished in four steps starting with a NI(CO)4 promoted cyclocondensation reaction of allyl chloride and 2-butyn-1-ol in MeOH, followed by hydrogenolysis of the resulting mixture to 2,3-dimethyl-5-methyl-oxycarbonylmethyl-2-cyclopentenone (3),...

Methylenomycin B (3a) has been prepared in ∼55% yield by SET catalyzed cyclization of enyone 1a. Mechanistic studies indicate that initial electron donation takes place at C-3 in enolized intermediates of type 2a

[±]-Deepoxy-4,5-didehydromethylenomycin A methyl ester 8 and [±]-methylenomycin A methyl ester 9 are synthesized from anthracene adduct 2 via a common intermediate 13. Flash vacuum pyrolysis of adduct 13 gives 8, while stereospecific epoxidation of 13 followed by pyrolysis yields 9.

Natural (−)-botryodiplodin(1) has been synthesized from an antibiotic methylenomycin A (2). The absolute configurations of (−)-botryodiplodin(1 and methylenomycin A (2) have also been established as shown in 1 and 2 respectively.

A new series of 3-hydroxyflavones (1–46) were synthesized according to the Claisen-Schmidt followed by Algar-Flynn-Oyamada reactions (AFO) in one step. The synthesized flavonoids were characterized by 1H NMR, 13C NMR and DCI-HRMS. All the synthesized compounds were tested in vitro for their 15-...

Some trimethyl-substituted antimony(V) compounds containing Sb-O bonds such as trimethylantimony dicarboxylates, dinitrate or oxybis(trimethylantimony) dinitrate, were prepared. From the infrared spectroscopic investigation, both in the solid and in solution, and cryoscopic molecular weight dete...

Ionization and appearance potentials determined with a time-of-flight mass spectrometer are reported for the principal positive ions in the mass spectra of dimethylzinc, trimethylaluminum, and trimethylantimony. The heats of formation, deduced by the application of the experimentally determined ...

Infrared and Raman spectra of trimethylantimony dichloride, dibromide and their deuterated analogs have been determined between 600 and 33 cm−1. Assignments of the skeletal modes were made on the basis of a D3h model by comparing data obtained on the deuterated and nondeuterated compounds. A gen...

The compounds bis(diorganomonothiophosphinato)trimethylantimony(V), Me3Sb(OSPR2)2, where R = Me, Et and Ph, have been prepared and characterized by IR, multinuclear (1H, 13C, 31P) NMR spectroscopy and mass spectrometry. The structure of Me3Sb(OSPPh2)2 has been determined by single-crystal X-ray ...