Frequency: Quarterly E- ISSN: 0976-3821 P- ISSN: IBI Factor: 4,26, Global Impact Factor 0.87 Abstracted/ Indexed in: CAS database (a division of the American Chemical Society), Ulrich's International Periodical Directory, Google Scholar, SCIRUS, Genamics Journal Seek, PSOAR, getCITED, JOURNAL directory, InfoBase Index, EBSCO Information Services
Quarterly published in print and online "Inventi Rapid: Med Chem" publishes high quality unpublished as well as high impact pre-published research and reviews catering to the needs of researchers and professionals. The journal covers all the areas under medicinal and pharmaceutical chemistry. It welcomes articles pertaining to design, synthesis, and biological evaluation of novel biologically active compounds, diagnostic agents, or ligands employed as pharmaceutical tools; molecular modifications of reported series leading to improved understanding of SAR; structural biological studies of relevant ligands and targets; computational chemistry methods; effect of molecular structure on biopharmaceutics, etc.
Thiadiazole, an important heterocyclic ring system, have recently attracted medical science to a great extent because of its diversified biological activities such as anti microbial, anti fungal, anti cancer, anti tubercular, anti HIV, anti convulsant, anti viral, anti inflammatory, anti depressant, anti leishmanial, anti oxidant and many more. In this review we have focused on diversified biological activities and different synthetic routes of 1,3,4-thiadiazole nucleus....
Oxadiazole a five membered heterocycles has been found with enormous biological activities with the suitable modifications in the structure. The present review is an attempt made to direct the attention of the researchers towards the oxadiazole ring for the development of newer chemical entities. Which are quite useful in the treatment of various life threatening diseases and disorders? Along with the development in the various methods used for the environmentally benign synthesis of oxadiazoles with profound biological activities....
With the suitable modifications in the structure 1,4-dihydropyrazol-5-one a five membered heterocycle has been found with enormous biological activities. The present review is an attempt made to direct the attention of the researchers towards the 1,4-dihydropyrazol-5-one moity for the development of newer chemical entities which will be quite useful in the treatment of various life threatening diseases and disorders. Along with the development in the various methods used for synthesis of 1,4-dihydropyrazol-5-one with profound biological activities one can proceed with newer area of Medicinal chemistry....
A set of ten substituted pyrazole derivative with anti-inflammatory activity was subjected to 2D-QSAR studies. Quantitative structure activity relationship (QSAR) analysis was performed on a series of pyrazole-based cyclooxygenase derived prostaglandin synthesis inhibitors for their anti-inflammatory activity by using VLife MDS 4.0software. QSAR models were generated based on various statistical methods like Multiple Regression, Principal Component Regression, and Partial Least Squares Regression etc. QSAR studies revealed that sulphur count, kappa3, chiV3, Oxygen count are primarily responsible for anti-inflammatory activity. The best QSAR model (r2 = 0.99, Fisher test value F=387.79, r2 se = 0.00) has acceptable statistical quality and predictive potential as indicated by the value of cross validated squared correlation coefficient (q2= 0.98). This model was obtained from Multiple Regression method with good predictive ability. The results obtained from QSAR studies could be used in designing better anti-inflammatory agents among the congeners in future....
Some novel compounds of 3-[3-chloro-2-(4-sustituted)-4-oxoazetidin-1-yl] 2-phenyl disubstituted quinazolin-4(3H)-one, 3-{[2-(3-chloro-4-substituted 2-oxoazetidin-1-yl)-1,3-thiazol-4-yl] amino}-2-phenyl disubstituted quinazolin-4(3H)-one were screened for their antifungal activity against fungi Candida albicans. These compounds have showed moderate and very good antifungal activity. The quantitative structure activity-relationships (QSAR) study on the quinazolin-4(3H)-one series was made using lipophilic, electronic and steric parameters. Several statistical expressions were developed and best models were validated. The studies confirm that the antifungal activity is dependent on selected lipophilic and electronic parameters. The study suggests that substitution on R1 group with increasing lipophilic nature and decreasing electronic factor favorable for antifungal activity. The QSAR study provides important structural insights in designing of potent antifungal agents....
Hetrocyclic compounds are indispensable structural units for both the chemists and the biochemists. There are vast numbers of pharmacologically active heterocyclic compounds in regular clinical use. Oxadiazole are the major compounds of heterocyclic nucleus for the development of new drugs and the drugs of oxadiazole were the first effective chemotherapeutic agent to be employed systemically for prevention and cure of bacterial-infection. This review provides an overview of anticancer activity of oxadiazole ring fused with heterocycles as reported over the past decades. Various cell lines used for anticancer activities are PC3, BGC823 and Bcap-37 cell, A431 human epidermoid cells. Oxadiazole ring have been explored in the past years and is still used for future development of new drugs against many more pathological conditions. Oxadiazole is an important pharmacophore in modern drug discovery....
As one third of the world’s population is infected with M. tuberculosis along with this new and relapse cases of tuberculosis are reported every year. The emergence of new cases, increased incidence of multi-drug resistant strains of M. tuberculosis and the side effects of existing first- and second-line antituberculosis drugs have led to hope of discovering new antitubercular drug molecules. The increase in demand for the synthesis of new antitubercular agents is due to the developing resistance towards existing drugs. The present review explores active triazole, thiazolidine, pyridine, oxazolidinone derivatives having antitubercular activity published during the last 10 years. Also, critical aspects of structure activity relationship with respect antitubercular activity have been encompassed. The present endeavor will of cognitive importance for further research on the potential use of said heterocyclic nucleus towards anti-tubercular activity....
A series of novel flavanone incorporated semicarbazide derivatives (Y2a–Y2j) was synthesized and characterized by elemental analyses, 1H NMR, IR and mass spectral studies. All the newly synthesized compounds (Y2a- Y2j) were screened for anti-phlogistic (anti-inflammatory) and anti-nociceptive activities against paw edema method, cotton pellet-induced granuloma, formalin induced paw edema in rats and acetic acid-induced writhing test respectively and compared with the standard drug diclofenac sodium and aspirin and compounds Y2c (o-NO2), Y2f (p-OH), Y2g (p-N(CH3)2) and Y2j (p-OH,-m-(OCH3)) having more anti-inflammatory and analgesic effect as compare to Y2a (p-Chloro), Y2b (o-Chloro), Y2d (m-NO2), Y2e (p-NO2), Y2h and Y2i (o-OH) and antimicrobial activity were also tested for their anti bacterial activity against gram positive bacteria S. aureus and B. antracis while gram negative bacteria P. aeruginosa and E. coli. And same compounds were tested for their anti fungal activity against C. albicans and A. Niger using cup plate method. Streptomycin, erythromycin, fluconazole and ketoconazole were used as a reference compound. The entire compounds shown good activity against gram positive and gram negative bacteria. The compounds Y2a (p-Chloro), Y2b (o-Chloro), Y2d (m-NO2), Y2e (p-NO2), Y2h and Y2i (o-OH) show moderate activity while Y2c (o-NO2), Y2f (p-OH), Y2g (p-N(CH3)2) and Y2j (p-OH,-m-(OCH3)) show good anti fungal and anti bacterial activities....
Molecular Modeling provides an array of valuable tools for drug design and analysis. Simple Visualization of molecules and easy access to structural databases has become essential component on the desktop of the medicinal chemist. Commercial software continues to expand upon the core user interface. New algorithms from industry and academia are quickly incorporated into the high end. Public domain takers are become more stable and offering functionality that rivals some of the commercial offerings. Computers continue to double in speed every year and a half while graphic displays become more sophisticated and intuitive. All of these elements make molecular modeling and integral part of the drug design....
Hydrazides and hydrazones are present in many of the bioactive heterocyclic compounds that are of wide interest because of their diverse biological and clinical applications. This created interest in researchers who have synthesized variety of hydrazide and hydrazone derivatives and screened them for their various biological activities viz. anticancer, antifungal, antimycobacterial, anti-inflammatory, trypanocidal, selective cox-2 inhibitors activity, antimicrobial, antiproliferative activity as well antimalarial activities....
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