Owing to ever-increasing bacterial and fungal drug resistance, we attempted to develop novel antitubercular and antimicrobial agents. For this purpose, we developed some new fluorine-substituted chalcone analogs (3, 4, 9–15, and 20–23) using a structure–activity relationship approach. Target compounds were evaluated for their antitubercular efficacy against Mycobacterium tuberculosis H37Rv and antimicrobial activity against five common pathogenic bacterial and three common fungal strains. Three derivatives (3, 9, and 10) displayed significant antitubercular activity with IC50 values of ≤16,760. Compounds derived from trimethoxy substituent scaffolds with monofluoro substitution on the B ring of the chalcone structure exhibited superior inhibition activity compared to corresponding hydroxy analogs. In terms of antimicrobial activity, most compounds (3, 9, 12–14, and 23) exhibited moderate to potent activity against the bacteria, and the antifungal activities of compounds 3, 13, 15, 20, and 22 were comparable to those of reference drugs ampicillin and fluconazole.
Fused pyrimidines, especially pyrazolo [3,4-d]pyrimidines, are among the most preferred building blocks for pharmacology studies, as they exhibit a broad spectrum of biological activity. In this study, new derivatives of pyrazolo [3,4-d]pyrimidine were synthesized by alkylation of the N1 nitrogen atom. We synthesized 3-iodo-1H-pyrazolo [3,4-d] pyrimidin-4-amine 2 from commercially available aminopyrazolopyrimidine 1 using N-iodosuccinimide as an iodinating agent. The synthesis of compound 2 started with nucleophilic substitution of 3-iodo-1H-pyrazolo [3,4-d]pyrimidin-4-amine with R-X (X:-OMs, -Br, -Cl), affording N-alkylated pyrazolo [3,4-d]pyrimidine. We performed this synthesis using a weak inorganic base and the mild temperature was also used for a two-step procedure to generate N-alkylated pyrazolo [3,4-d]pyrimidine derivatives. Also, all compounds were tested for their ability to inhibit acetylcholinesterase (AChE) and the human carbonic anhydrase (hCA) isoforms I and II, with K i values in the range of
The experiment was carried out under three seasons with 15 genotypes at Agricultural Research Station, Kunaram, Telangana state, India during rabi season (December to April) 2014–15 (E1), kharif season (July to November) 2015 (E2) and rabi season (December to April) 2015–16 (E3). The objective of the study was to assess the stability and adaptability of 15 rice genotypes of the various maturity groups over three seasons. The GGE biplot tool of these 15 rice genotypes of various maturity durations expressed a significant genotype, environment and G×E interaction for yield and days to 50% flowering. Genotype and environment interaction effect was responsible for the greatest part of the variation, followed by genotypes and environment effects for grain yield. Days to 50% flowering of genotypes was highly affected by environments followed by genotypes, and genotype and environment interaction. It also detected that rabi season 2014–15 (E1) was identified as the best suited season for the potential expression of the grain yield, while kharif season 2015 (E2) was the right season for the expression of reduced days to 50% flowering. Further, the what–won–where model indicated that short duration rice genotype G14 (KNM 1690) and medium duration genotype G9 (KNM 1632) in the environments rabi season 2014–15 (E1) and kharif season 2015 (E2), respectively and the early line G11 (KNM 1684) in the environment rabi season 2015–16 (E3) were the winning genotypes and suitable for their respective environments for grain yield. G7 (KNM 1616) was the vertex early genotype and closer to the ideal genotype expressed high yield and stability for all the environments. G13 (KNM 1689) and G14 (KNM 1690) were found to be stable for earliness across all the seasons and could be utilized for the development of early duration varieties. The rice genotype, G15 (BPT 5204) was found to be stable for lateness for all the seasons.
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