Introduction. Les effets indésirables médicamenteux sont devenus un défi important de la médecine moderne ; ils sont classés entre les quatrièmes et sixièmes causes principales de décès. Selon une étude conduite par Novotny et coll., les antibiotiques sont responsables de 16 % des effets indésirables enregistrés. Cette étude a pour objectifs de détecter, évaluer et d’analyser les effets indésirables liés à l’utilisation des antibiotiques au CHU de Sidi Bel-Abbès. Méthodes. Une étude prospective portant sur les malades du CHU de Sidi Bel-Abbès qui ont développé des effets indésirables liés à l’utilisation des antibiotiques pendant cinq mois (du 1er janvier au 30 mai 2014). Résultats. Un total de 73 effets indésirables a été signalé au cours de la période d'étude avec une prédominance masculine (53,42%) et le groupe d'âge gériatrique. Les organes les plus affectés étaient le système gastro-intestinal (34,24 %) et la peau (26,02 %). Les classes d'antibiotiques principalement comptabilisées étaient les céphalosporines (35,61 %), suivie par les fluoroquinolones (30,50 %) et (61,64 %) des effets indésirables étaient prévisibles. L'évaluation de la gravité a révélé que la plupart d'entre eux étaient modérés (65,75%), suivis par des réactions légères et graves. Conclusion. L'étude a conclu que le taux des effets indésirables est assez élevé, d’où la nécessité de la création d’un service de pharmacovigilance qui veille à la surveillance de ces effets et la mise en œuvre de directives d’antibiotiques à usage hospitalier afin d’assurer leur usage rationnel
In mammalian cells, proliferation is controlled by the cell cycle, where cyclin-dependent kinases regulate critical checkpoints. CDK4 is considered highly validated anticancer drug target due to its essential role regulating cell cycle progression at the G1 restriction point. Our objective is designing novel CDK4 inhibitors using Structure-Based Drug Design and Quantitative Structure-Activity Relationship techniques. We used bioinformatics tools and biological databases. QSAR study of CDK4 inhibitors has given us an idea on the physicochemical features of studied compounds and their correlation with the IC50 activity. The docking study has helped to highlight the molecule key elements to refine in order to get a more potent compound of CDK4.The Molecule under the code 21366124 which has the low IC50= 3 nmole shows the most binding affinity with score value of ΔG=-9,8 kcal/mol. As prospects, it would be very interesting to synthesize this drug candidate and to test its inhibitory activity on cell culture of breast cancer
In mammalian cells, proliferation is controlled by the cell
cycle, where cyclin-dependent kinases regulate critical
checkpoints. CDK4 is considered a highly validated anticancer
drug target due to its essential role in regulating cell cycle
progression at the G1 restriction point. Our objective is
to design novel CDK4 inhibitors using Structure-Based Drug
Design and Quantitative Structure-Activity Relationship
techniques. We used bioinformatics tools and biological
databases. QSAR study of CDK4 inhibitors has given us an
idea of the physicochemical features of studied compounds
and their correlation with the IC50 activity. The docking study
has helped to highlight the molecule key elements to refine
in order to get a more potent compound of CDK4.The
Molecule under the code 21366124 which has the low IC50=
3 nmole shows the most binding affinity with a score value of
ΔG=-9,8 kcal/mol. As prospects, it would be very interesting
to synthesize this drug candidate and to test its inhibitory
activity on cell culture of breast cancer.
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