Synthesis and characterization of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl]ethylidene) benzenamine derivatives as potent antifungal agents.

In the present study, a series of (Z)-N-(1-[2-{3-[(dimethylamino)methyl)]-2-methoxyphenyl}-5-(pyridin-4-yl)-1,3,4-oxadiazol-3(2H)-yl]ethylidene)benzenamine derivatives have been synthesized and characterized by IR, 1H NMR and 13C NMR spectra. All the synthesized compounds were evaluated for their antifungal activity and were compared with the standard drug, clotrimazole. The compounds demonstrated excellent to weak antifungal activity. Among the synthesized derivatives, 4f and 4h showed significant activity and 4c exhibited moderate activity against Candida albicans, Candida tropicalis and Aspergillus niger as compared with the standard antifungal agent - clotrimazole. The minimum inhibitory concentration of the compounds was in the range of 1.62-25 microg/mL against fungi. Furthermore, the substitution of chloro, nitro and methoxy groups at para position of benzene moiety play an important role in enhancing the antifungal activity of this class of compounds.

A novel G·G·T non-conventional intramolecular triplex formed by the double repeat sequence of Chlamydomonas telomeric DNA.

Competition among DNA non-canonical structures has been widely studied in repetitive DNA sequences. The factors affecting DNA structural polymorphism have always been an important area of research. The Chlamydomonas reinhardtii telomere (TTTTAGGG) n is found to be an exception to the general idea of forming a folded G-quadruplex by a few repeats in any telomeric sequence. Herein, using gel electrophoresis, UV thermal melting, UV thermal difference spectra (TDS), circular dichroism, and fluorescence and NMR spectroscopy. We demonstrated that the double repeat of the C. reinhardtii telomere (TTTTAGGG)2 (Chlm2) adopts an intramolecular non-conventional triplex structure in Na+ solution. We report that the co-existence of reverse Hoogsteen (G·G) and Wobble base pairing (G·T) stabilizes the triplex structure. To the best of our knowledge, such a non-conventional triplex structure formed by any telomeric sequence has not been reported to date.

Correction: A novel G·G·T non-conventional intramolecular triplex formed by the double repeat sequence of Chlamydomonas telomeric DNA.

[This corrects the article DOI: 10.1039/D2RA00861K.].

A mini review on central nervous system potential of isatin derivatives.

Isatin is a heterocyclic moiety which can be used for the synthesis of a large variety of heterocyclic compounds such as quinolines, indoles and as raw material for medicinal important drugs. This review gives an overview of the advances of isatin for the synthesis of various heterocyclic compounds and shows the various biological potentials such as anticonvulsant, sedative, hypnotic, monoamine oxidase inhibitors, antianxiety, antipsychoactives activity etc. Isatin derivatives displayed as potent anticonvulsant potential in a large variety of preclinical anticonvulsant models. Present review article is an attempt to compile the various central nervous system potential of synthesized isatin analogs which will serve as a valuable source of information for the researchers working in this field.

Cabazitaxel: a novel drug for hormone-refractory prostate cancer.

Cabazitaxel has recently been approved by FDA for the treatment of docetaxel resistant hormone-refractory prostate cancer. It has been developed by Sanofi-Aventis under the trade name of Jevtana. It is given in combination with prednisone/prednisolone and has passed the clinical trial over well-known drug mitoxantrone. This drug is a microtubule depolymerization inhibitor, which can penetrate blood brain barrier (BBB). The FDA granted fast track designation to this drug in November 2009 and thereafter, new drug application submission was done in March 2010. Priority review to this drug was granted in April 2010 and finally in July 2010 it was approved by FDA. It is available in the form of injection in the dose of 60 mg/1.5 mL, which should be diluted prior to its use by the diluents supplied along with the injection. It is a second-line drug and has proven to be effective in patients experiencing docetaxel based treatment failure.