Three new 2-methoxy acetylenic acids (1-3) and a known derivative (4), in addition to three new natural pyrazole alkaloids (5-7) were isolated from an Indonesian marine sponge of the genus Cinachyrella. Compounds 5 and 6 have previously been reported as synthetic compounds. The structures of the new compounds were established on the basis of one- and two-dimensional NMR spectroscopy as well as ...

In the title 2H-pyrazolo-[4,3-c]pyridine derivative, C(32)H(27)Cl(2)N(3), the dihydro-pyrazole ring adopts an envelope conformation and the piperidine fused ring a twisted-chair conformation. Two short intra-molecular C-H⋯Cl contacts are observed. The crystal packing is characterized by dimeric C-Cl⋯π inter-actions involving the 5-benzyl ring, with Cl⋯centroid and closest atomic Cl⋯π distances ...

Several pyrazolo [1, 5-a] pyrimidines derivative were prepared by the condensation of substituted of α, βunsaturated carbonyl compounds (chalcones) with substituted 5-amino pyrazole as an alternative polyethylene glycol (PEG-400) as green reaction medium. The reaction is clean with excellent yield, shorter reaction time. The entire synthesized products were characterized by spectral analysis. F...

Cryptosporidium inosine 5'-monophosphate dehydrogenase (CpIMPDH) has emerged as a therapeutic target for treating Cryptosporidium parasites because it catalyzes a critical step in guanine nucleotide biosynthesis. A 4-oxo-[1]benzopyrano[4,3-c]pyrazole derivative was identified as a moderately potent (IC50 = 1.5 μM) inhibitor of CpIMPDH. We report a SAR study for this compound series resulting in...

Novel tetrasubstituted pyrazole derivatives bearing a nitro substituent on their A-phenol ring were synthesized and their binding affinity towards the estrogen receptor (ER) subtypes ERalpha and ERbeta was determined. Among compounds tested, the 2-nitrophenol derivative 5c was found to bind satisfactorily to both estrogen receptor subtypes (RBAalpha=5.17 and RBAbeta=3.27). In general, the intro...

A case of gangrene of the hand following inadvertent intra-arterial injection of a pyrazole derivative (Tomanol) is presented. Gangrene of the hand and superficial sloughing of the distal arm necessitated a forearm amputation. Because of the serious sequelae, precautions must be taken to avoid inadvertent intra-arterial injections and due consideration must be given to the anatomical variation ...

In the title compound, C(21)H(15)F(2)N(3)O(2), a pyrazole derivative bearing three aromatic substituents, the central five-membered heterocyclic ring makes dihedral angles of 1.77 (14), 3.68 (13) and 72.15 (14)° with the three benzene rings. In the crystal, C-H⋯O and C-H⋯F inter-actions connect the mol-ecules into double layers parallel to the bc plane.

Recently described biphenyl analogues of the antituberculosis drug PA-824 displayed improved potencies against M. tuberculosis but were poorly soluble. Heterobiaryl analogues of these, in which the first phenyl ring was replaced with various 5-membered ring heterocycles, were prepared with the aim of identifying potent new candidates with improved aqueous solubility. The compounds were construc...

Department of Pharmaceutical technology, Meerut Institute of Engineering and Technology, Meerut. ABSTRACT Pyrazole and pyrimidine derivatives attracted organic chemists due to their various biological and chemotherapeutic significance. Pyrazolopyrimidines and related fused heterocycles are of important as probable bioactive molecules. The heterocyclic fusion of pyrimidine ring and pyrazole ring...

The extensive pharmacological applications of the pyrazole-based compounds stimulated us to synthesize highly functionalized, pyrazolylmalonyl diisothiocyanate derivative (2) via treating 2-((1,3-diphenyl-1H-pyrazol-4-yl)methylene)malonyl dichloride (1) with ammonium thiocyanate in acetonitrile at room temperature. 2 was subsequently conducted a double molar ratio different nitrogen nucleophile...